Associate Professor Laurence Wakelin

Associate Professor Laurence Wakelin

Honorary Associate Professor

BSc.(Hons) 1st Class Chemistry, University of Kent, UK, 1971.

PhD Pharmacology, Clare College, University of Cambridge, UK, 1975.

Science
School of Chemistry

Education

University of Kent, United Kingdom, BSc(Hons) 1st Class Chemistry 1971.

University of Cambridge, United Kingdom, PhD Pharmacology 1975.

Employment

Department of Pharmacology, University of Cambridge, Science Research Council Fellow 1975-1977.

Department of Pharmacology, University of Cambridge, Medical Research Council Fellow, 1978-1980.

Senior Scientist, Peter MacCallum Cancer Institute, Melbourne, 1981-1989.

Professor of Cancer Research, University College Dublin, 1990-1997.

Visiting Fellow, School of Chemistry, UNSW, 1998.

Associate Professor, School of Medical Sciences, UNSW, 1999-2019.

Appointed Honorary Associate Professor, School of Chemistry, UNSW, April 2019. 

Mobile
+61414286217
Location
School of Chemistry, Dalton Building, UNSW Sydney, NSW 2052, Australia,
  • Book Chapters | 2011
    Wolf S; Wakelin L; Catchpoole DR, 2011, 'Considerations for Treatment Development in Rhabdomyosarcoma: In Vitro Assessment of Novel DNA Binding Drugs', in Derbel F (ed.), Soft Tissue Tumors, edn. 1st, InTech, November, 2011, pp. 3 - 30
    Book Chapters | 1991
    Wakelin L, 1991, 'On creating targets in DNA designed to be 'hot-spots' for radiation damage.', in Seymour C; Mothersill C (ed.), New Developments in Fundamental and Applied Radiobiology, Taylor and Francis, London, pp. 269 - 274, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1991BT29Y00038&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Book Chapters | 1991
    Wickham G; Wakelin L; Palmer B; Lee H; Johnson P; Baguley BC; Denny WA; McFadyen DW, 1991, 'Cis-diammine platinum (II) complexes tethered to DNA-affinic ligands: antitumour activity and DNA-binding properties', in Howell SB (ed.), Proceedings of the Sixth International Symposium on Platinum and Other Metal Co-ordination Compounds in Cancer Chemotherapy, Plenum, New York, pp. 51 - 60, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1991BV14L00005&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Book Chapters | 1990
    Wakelin L; Denny WA, 1990, 'Kinetic and equilibrium binding studies of a series of intercalating agents that bind by threading a sidechain through the DNA helix', in Pullman B; Jortner J (ed.), Molecular Basis of Specificity in Nucleic Acid-Drug Interactions, edn. JERUSALEM SYMPOSIA ON QUANTUM CHEMISTRY AND BIOCHEMISTRY, Kluwer Academic Publishers, Dordrecht, pp. 191 - 206, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1990BT67J00014&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Book Chapters | 1990
    Wakelin L; Waring M, 1990, 'DNA intercalating agents', in Hansch C; Sammes PG; Taylor JB (ed.), Comprehensive Medicinal Chemistry, The Rational Design, Mechanistic Study, and Therapeutic Application of Chemical Compounds, edn. Volume 2, Pergamon Press, Oxford, UK, pp. 703 - 724
    Book Chapters | 1988
    Denny WA; Wakelin L, 1988, 'Tricyclic carboxamides: relationships between antitumour activity and geometry and kinetics of binding to DNA.', in Sarma RH; Sarma MH (ed.), Structure and Expression: DNA and Its Drug Complexes, edn. Volume 2, Adenine Press, USA, pp. 329 - 337
  • Journal articles | 2022
    Chen J; Campbell AP; Wakelin LPG; Finch AM, 2022, 'Characterisation of bis(4-aminoquinoline)s as α1A adrenoceptor allosteric modulators', European Journal of Pharmacology, 916, http://dx.doi.org/10.1016/j.ejphar.2021.174659
    Journal articles | 2022
    Constable GEO; Jung J; Read RW; Wakelin LPG; Bhadbhade MM; Hunter L, 2022, 'Synthesis of phenazine-2,8-dicarboxylates', ARKIVOC, pp. 46 - 57, http://dx.doi.org/10.24820/ark.5550190.p011.616
    Journal articles | 2022
    Zihlif M; Catchpoole DR; Stewart BW; Wakelin LPG, 2022, 'Withdrawn: Variations in Altered Global Gene Expression caused by Topoisomerase II Poisons Assessed with Reference to Differences in DNA Binding.', Curr Mol Pharmacol, http://dx.doi.org/10.2174/1874467215666220301115946
    Journal articles | 2021
    Rowell KN; Thomas DS; Ball GE; Wakelin LPG, 2021, 'Molecular dynamic simulations of diacridine binding to DNA: Indications that C6 diacridine can bisintercalate spanning two base pairs', Biopolymers, 112, pp. e23409, http://dx.doi.org/10.1002/bip.23409
    Journal articles | 2020
    Serobian A; Pracey CP; Thomas DS; Denny WA; Ball GE; Wakelin LPG, 2020, 'Structures and dynamics of DNA complexes of the desmethyl analog of the cytotoxin MLN944: Insights into activity when a methyl isn't futile', Journal of Molecular Recognition, 33, http://dx.doi.org/10.1002/jmr.2843
    Journal articles | 2017
    Campbell AP; Wakelin LPG; Denny WA; Finch AM, 2017, 'Homobivalent conjugation increases the allosteric effect of 9-aminoacridine at the α1-adrenergic receptors', Molecular Pharmacology, 91, pp. 135 - 144, http://dx.doi.org/10.1124/mol.116.105874
    Journal articles | 2014
    Chen J; Campbell AP; Urmi KF; Wakelin LPG; Denny WA; Griffith R; Finch AM, 2014, 'Human α1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines', Bioorganic and Medicinal Chemistry, 22, pp. 5910 - 5916, http://dx.doi.org/10.1016/j.bmc.2014.09.017
    Journal articles | 2014
    Drwal MN; Marinello J; Manzo SG; Wakelin LPG; Capranico G; Griffith R, 2014, 'Novel DNA topoisomerase iia inhibitors from combined ligand- and structure- based virtual screening', PLoS ONE, 9, pp. e114904, http://dx.doi.org/10.1371/journal.pone.0114904
    Journal articles | 2014
    Serobian A; Thomas DS; Ball GE; Denny WA; Wakelin LPG, 2014, 'The solution structure of bis(phenazine-1-carboxamide)-DNA complexes: MLN 944 binding corrected and extended', Biopolymers, 101, pp. 1099 - 1113, http://dx.doi.org/10.1002/bip.22513
    Journal articles | 2013
    Chen J; Murad AK; Wakelin L; Denny WA; Griffith R; Finch AM, 2013, 'a1-Adrenoceptor and serotonin 5-HT1A receptor affinity of homobivalent 4-aminoquinoline compounds: An investigation of the effect of linker length', Biochemical Pharmacology, 85, pp. 1534 - 1541, http://dx.doi.org/10.1016/j.bcp.2013.03.010
    Journal articles | 2011
    Malgorzata ND; Agama K; Wakelin L; Pommier Y; Griffith R; Drwal M, 2011, 'Exploring DNA Topoisomerase I Ligand Space in Search of Novel Anticancer Agents', PLoS One, 6, pp. 1 - 12, http://dx.doi.org/10.1371/journal.pone.0025150
    Journal articles | 2011
    Wolf S; Huynh T; Bryce NS; Hambley TW; Wakelin L; Stewart BW; Stewart D, 2011, 'Intracellular Trafficking as a Determinant of AS-DACA Cytotoxicity in Rhabdomyosarcoma Cells', BMC Cell Biology, 12, pp. 1 - 11, http://dx.doi.org/10.1186/1471-2121-12-36
    Journal articles | 2010
    He Z; Lai D; Wakelin L, 2010, '[Co(III)(cyclen)Cl2]Cl is selectively cytotoxic to human leukaemia cells', European Journal of Pharmacology, 637, pp. 11 - 15, http://dx.doi.org/10.1016/j.ejphar.2010.03.047
    Journal articles | 2010
    Zihlif M; Catchpoole DR; Stewart BW; Wakelin L, 2010, 'Effects of DNA minor groove binding agents on global gene expression', Cancer Genomics and Proteomics, 7, pp. 323 - 330
    Journal articles | 2010
    Zihlif MA; Wakelin LPG; Catchpoole D; Stewart B, 2010, 'Determining the mechanism of action of novel bisintercalating agents using the cDNA microarray technology', CANCER RESEARCH, 70, http://dx.doi.org/10.1158/1538-7445.AM10-744
    Journal articles | 2009
    Majid AA; Smythe GA; Denny WA; Wakelin L, 2009, 'Mass spectrometry studies of the binding of the minor groove-directed alkylating agent alkamin to AT-Tract Oligonucleotides', Chemical Research in Toxicology, 22, pp. 146 - 157
    Journal articles | 2009
    Wolf S; Wakelin L; He Z; Stewart BW; Catchpoole DR, 2009, 'In vitro assessment of novel transcription inhibitors and topoisomerase poisons in rhabdomyosarcoma cell lines', Cancer Chemotherapy and Pharmacology, 64, pp. 1059 - 1069
    Journal articles | 2009
    Zihlif M; Catchpoole DR; Stewart BW; Wakelin L, 2009, 'Effects of DNA threading bis(9-aminoacridine-4-carboxamides) on global gene expression', Cancer Genomics and Proteomics, 6, pp. 317 - 323
    Journal articles | 2008
    He Z; Bu X; Eleftheriou A; Zihlif M; Qing Z; Stewart BW; Wakelin L, 2008, 'DNA threading bis(9-aminoacridine-4-carboxamides): Effects of piperidine sidechains on DNA binding, cytotoxicity and cell cycle arrest', Bioorganic and Medicinal Chemistry, 16, pp. 4390 - 4400, http://dx.doi.org/10.1016/j.bmc.2008.02.063
    Journal articles | 2007
    Majid A; Smythe GA; Denny WA; Wakelin L, 2007, 'Structure of the d( CGCGAATTCGCG)(2) complex of the minor groove binding alkylating agent alkamin studied by mass spectrometry', Molecular Pharmacology, 71, pp. 1165 - 1178
    Journal articles | 2007
    Majid A; Smythe GA; Denny WA; Wakelin L, 2007, 'Structure of the d(CGCGAATTCGCG)(2) complex of the minor groove binding alkylating agent alkamin studied by mass spectrometry (vol 71, pg 1165, 2007)', Molecular Pharmacology, 72, pp. 485 - 485
    Journal articles | 2005
    Edwards GL; Black DS; Deacon G; Wakelin L, 2005, 'Effect of charge and surface area on the cytotoxicity of cationic metallointercalation reagents', Canadian Journal of Chemistry - Revue Canadienne de Chimie, 83, pp. 969 - 979
    Journal articles | 2005
    Edwards GL; Black DS; Deacon G; Wakelin L, 2005, 'In vitro and in vivo studies of neutral cyclometallated complexes against murine leukaemias', Canadian Journal of Chemistry - Revue Canadienne de Chimie, 83, pp. 980 - 989
    Journal articles | 2004
    Adams A; Guss JM; Denny WA; Wakelin L, 2004, 'Structure of 9-amino-[N-(2-dimethylamino)propyl]acridine-4-carboxamidebound to d(CGTACG)(2): a comparison of structures of d(CGTACG)(2)complexed with intercalators in the presence of cobalt', ACTA Crystallographica Section D - Biological Crystallography, 60, pp. 823 - 828
    Journal articles | 2004
    Zihlif Z; Catchpoole D; He Z; Wakelin LPG; Stewart BW, 2004, '541 Effects of bisintercalating DNA threading agents on global gene expression', European Journal of Cancer Supplements, 2, pp. 165 - 165, http://dx.doi.org/10.1016/s1359-6349(04)80549-4
    Journal articles | 2003
    Baguley BC; Wakelin L; Jacintho J; Kovacic P, 2003, 'Mechanisms of action of DNA intercalating acridine-based drugs: Howimportant are contributions from electron transfer and oxidative stress?', Current Medicinal Chemistry: Cardiovascular and Hematological Agents, 10, pp. 2643 - 2649
    Journal articles | 2003
    Howarth N; Wakelin L; Walker D, 2003, 'Synthesis of the four diastereoisomers of 3-thymine-1-(tbutoxycarbonyl)amino-cyclopentane-1-carboxylic acid.', Tetrahedron Letters, 44, pp. 695 - 698
    Journal articles | 2003
    Howarth N; Wakelin L; Walker D, 2003, 'alpha-cycloPNA: 1-aminocyclopentane-1-carboxylic acid-derived peptide nucleic acids.', Nucleosides, Nucleotides and Nucleic Acids, 22, pp. 1351 - 1353, http://dx.doi.org/10.1081/NCN-120022963
    Journal articles | 2003
    Wakelin L; Bu X; Eleftheriou A; Parmar A; Hayek CB; Stewart BW, 2003, 'Bisintercalating threading diacridines: Relationships between DNAbinding, cytotoxicity, and cell cycle arrest', Journal of Medicinal Chemistry, 46, pp. 5790 - 5802
    Journal articles | 2002
    Adams A; Guss JM; Denny WA; Wakelin L, 2002, 'Crystal structure of 9-amino-N-[2-(4-morpholinyl)ethyl]-4-acridinecrboxamide bound to d (CGTACG)2: implications for structure-activity relationships of acridinecarboxamide topoisomerase poisons', Nucleic Acids Research, 30, pp. 719 - 725
    Journal articles | 2002
    Teixeira SC; Thorpe JH; Todd AK; Powell HK; Adams A; Wakelin L; Denny WA; Cardin CJ, 2002, 'Structural Characterisation of Bisintercalation in Higher-order DNA at a Junction-like Quadruplex', Journal of Molecular Biology, 323, pp. 167 - 171
    Journal articles | 2002
    Wakelin L; Adams A; Denny WA, 2002, 'Kinetic Studies of the Binding of Acridinecarboxamide Topoisomerase Poisons to DNA: Implications for Mode of Binding of Ligands with Unchanged Chromophores', Journal of Medicinal Chemistry, 45, pp. 894 - 901
    Journal articles | 2001
    Kovacic P; Wakelin L, 2001, 'DNA molecular electrostatic potential: novel perspectives for the mechanism of action of anticancer drugs involving electron transfer and oxidative stress', Anti-Cancer Drug Design, 16, pp. 175 - 184
    Journal articles | 2000
    Adams A; Guss M; Collyer C; Denny WA; Prakash AS; Wakelin L, 2000, 'Acridinecarboxamide topoisomerase poisons: structural and kinetic studies of the DNA complexes of 5-substituted 0-amino-(N-(2-dimethylamino)ethyl)acridine-4-carboxamides', Molecular Pharmacology, 58, pp. 649 - 658
    Journal articles | 2000
    Adams A; Guss M; Collyer C; Denny WA; Wakelin L, 2000, 'A novel form of intercalation involving four DNA duplexes in an acridine-4-carboxamide complex of d(CGTACG)2', Nucleic Acids Research, 28, pp. 4244 - 4253
    Journal articles | 2000
    Howarth NM; Wakelin LPG, 2000, 'alpha-PNA: A novel peptide nucleic acid analogue of DNA (vol 62, pg 5442, 1997)', JOURNAL OF ORGANIC CHEMISTRY, 65, pp. 634 - 634, http://dx.doi.org/10.1021/jo974036u
    Journal articles | 1999
    Adams A; Collyer C; Guss M; Denny WA; Wakelin L, 1999, 'Crystal structure of the topoisomerase II poison 9-amino-[N-(2-dimethylamino)ethyl]acridine-4-carboxamide bound to the DNA hexanucleotide d(CGTACG)2', Biochemistry, 38, pp. 9221 - 9233
    Journal articles | 1999
    McClean S; Costelloe C; Denny WA; Searcy M; Wakelin L, 1999, 'Sequence selectivity, cross-linking efficiency and cytotoxicity of DNA-targeted 4-anilinoquinoline aniline mustards', Anti-Cancer Drug Design, 14, pp. 187 - 204
    Journal articles | 1999
    Todd AV; Adams A; Powell HK; Wilcock DJ; Thorpe JH; Lausi A; Zanini F; Wakelin L; Cardin CJ, 1999, 'Determination of MAD-DM of the structure of the DNA duplex d(ACGTACG(5-BrU)2 at 1.4 A and 100 K', ACTA Crystallographica Section D - Biological Crystallography, 55, pp. 729 - 735, http://dx.doi.org/10.1107/S090744499801261X
    Journal articles | 1999
    Todd AV; Adams A; Thorpe J; Denny WA; Wakelin L; Cardin CJ, 1999, 'Major groove binding and a `DNA-induced` fit in the intercalation of a derivative of the mixed topoisomerase I/II inhibitor (N-(2-dimethylamino)ethyl)acridine-4-carboxamide (DACA) into DNA: X-ray structure complexed to d(CG(5-BrU', Journal of Medicinal Chemistry, 42, pp. 536 - 540
    Journal articles | 1998
    Hendersen ; Lacey S; O'Hare C; Hartley J; McClean S; Wakelin L; Kelland L; Robbins D, 1998, 'Synthesis of new bifunctional compounds which selectively alkylate guanines in DNA.', Anti-Cancer Drug Design, 13, pp. 749 - 768
    Journal articles | 1998
    Searcy M; McClean S; Madden B; McGowan A; Wakelin L, 1998, 'Synthesis, DNA-cleaving properties and cytotoxicity of intercalating chelidamic acid derivatives.', Anti-Cancer Drug Design, 13, pp. 837 - 855
    Journal articles | 1998
    Whittaker JK; Mcfadyen DW; Wickham G; Wakelin L; Murray VM, 1998, 'The interaction of DNA-targeted platinum phenanthridinium complexes with DNA', Nucleic Acids Research, 26, pp. 3933 - 3939
    Journal articles | 1997
    Howarth N; Wakelin L, 1997, 'Alpha-PNA: A novel peptide nucleic acid analogue of DNA.', Journal Organic Chemistry, 62, pp. 5441 - 5450
    Journal articles | 1997
    Searcy M; McClean S; Madden B; Wakelin L, 1997, 'Bleomycin mimics. Design and synthesis of an acridine derivative which cleaves DNA in a sequence-neutral manner.', Journal of the Chemical Society, Perkin Transactions 2, pp. 523 - 532
    Journal articles | 1996
    Searcy M; Martin PN; Howarth N; Madden B; Wakelin L, 1996, 'DNA threading agents: Effect of sidechain bulk on DNA binding and cytotoxicity of 9-anilinoacridine-4-carboxamides.', Bioorganic and Medicinal Chemistry Letters, 6, pp. 1831 - 1836
    Journal articles | 1996
    Wilcock DJ; Adams A; Cardin CJ; Wakelin L, 1996, 'Crystal and molecular structure of the DNA octanucleotide d(ACGTACGT)2.', Acta Crystallographica D, 52, pp. 481 - 485
    Journal articles | 1992
    Bailly C; Denny WA; Mellor E; Wakelin L; Waring M, 1992, 'Sequence specificity of the binding of antitumour amsacrine-4-carboxamides to DNA studied by DNase I footprinting.', Biochemistry, 31, pp. 3514 - 3524
    Journal articles | 1992
    Deacon G; Webster L; Buxton D; Hillcoat B; James A; Roos I; Thomson R; Wakelin L; Williams T, 1992, 'Cis-Dipyridineplatinum(II) organoamides with unexpected growth inhibition properties and antitumour activity.', Journal Medicinal Chemistry, 35, pp. 3349 - 3353
    Journal articles | 1992
    Lee H; Palmer B; Baguley BC; Mcfadyen DW; Wickham G; Thorsborn-Palmer D; Wakelin L; Denny WA, 1992, 'DNA-directed alkylating agents. 5. Acridinecarboxamide derivatives of cis-ethane-1,2-diamminodichloro-platinum (II).', Journal Medicinal Chemistry, 35, pp. 2983 - 2987
    Journal articles | 1992
    Palmer B; Wickham G; McFadyen DW; Craik D; Wakelin L; Baguley BC; Denny WA, 1992, 'Synthesis, DNA binding interactions and biological activity of bis platinum (II) complexes of N,N,N',N'-tetrakis(2-aminoethyl)-diamines.', Anti-Cancer Drug Design, 7, pp. 385 - 401
    Journal articles | 1992
    Webster LK; Hillcoat BL; Roos IAG; Wakelin LPG; Deacon GB; Buxton DP; James AM; Thomson RJ; Williams TL, 1992, 'Cis-Bis(pyridine)platinum(II) Organoamides with Unexpected Growth Inhibition Properties and Antitumor Activity', Journal of Medicinal Chemistry, 35, pp. 3349 - 3353, http://dx.doi.org/10.1021/jm00096a007
    Journal articles | 1991
    Gourdie T; Prakash AS; Wakelin L; Woodgate P; Denny WA, 1991, 'Synthesis and evaluation of DNA-targeted spatially-separated bis(aniline mustards) as potential alkylating agents with enhanced DNA cross-linking capability', Journal Medicinal Chemistry, 34, pp. 240 - 248
    Journal articles | 1991
    Plummer S; Parker N; De Kretser T; Wakelin L, 1991, 'Selective inhibition of c-myc and c-myb transcription by antitumour anthracyclines in human tumour cells.', Journal of Cellular Pharmacology, 2, pp. 248 - 256
    Journal articles | 1991
    Prakash AS; Valu K; Wakelin L; Woodgate P; Denny WA, 1991, 'Synthesis and antitumour activity of the spatially-separated mustard bis-N,N'-[3-(N-(2-chloroethyl)-N-ethyl)amino-5-((N,N-dimethylamino)-methyl)aminophenyl]-1,4-benzenedicarboxamide, which alkylates DNA exclusively at adenines in the minor groove.', Anti-Cancer Drug Design, 6, pp. 195 - 206
    Journal articles | 1991
    Searle M; Bicknell W; Wakelin L; Denny WA, 1991, 'Anthracycline antibiotic arugomycin binds in both grooves of the DNA helix simultaneously: an NMR and molecular modelling study.', Nucleic Acids Research, 19, pp. 2897 - 2906
    Journal articles | 1991
    Wickham G; Prakash AS; Wakelin L; McFadyen DW, 1991, 'DNA-binding properties and antitumour activity of monofunctional alkylating groups attached to the DNA-intercalating chromophore phenanthridine: n-bromo-alkylphenanthridinium bromides.', Biochimica Biophysica Acta, 1073, pp. 528 - 537, http://dx.doi.org/10.1016/0304-4165(91)90226-7
    Journal articles | 1990
    Bray A; Kelly D; Mack P; Martin R; Wakelin L, 1990, 'Synthesis of a peptide-linked binuclear platinum (II) terpyridine complex', Australian Journal Chemistry, 43, pp. 629 - 634
    Journal articles | 1990
    Bray AM; Kelly DP; Mack OLP; Martin RF; Wakelin LPG, 1990, 'DNA-Binding Compounds. III. Synthesis of a Peptide-Linked Binuclear Platinum(II)-Terpyridine Complex', Australian Journal of Chemistry, 43, pp. 629 - 634, http://dx.doi.org/10.1071/CH9900629
    Journal articles | 1990
    Denny WA; Wakelin L, 1990, 'Kinetics of the binding of mitoxantrone, ametantrone and analogues to DNA: relationship to binding mode and antitumour activity.', Anti-Cancer Drug Design, 5, pp. 189 - 200
    Journal articles | 1990
    Gourdie T; Valu K; Gravatt G; Boritzki T; Baguley BC; Wakelin L; Wilson W; Woodgate P; Denny WA, 1990, 'DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard', Journal Medicinal Chemistry, 33, pp. 1177 - 1186
    Journal articles | 1990
    McFadyen DW; Sotirellis N; Denny WA; Wakelin L, 1990, 'Interaction of substituted and rigidly-linked diquinolines with DNA.', Biochimica Biophysica Acta, 1048, pp. 50 - 58, http://dx.doi.org/10.1016/0167-4781(90)90021-S
    Journal articles | 1990
    Palmer B; Lee H; Johnson P; Baguley BC; Wickham G; Wakelin L; McFadyen DW; Denny WA, 1990, 'DNA-directed alkylating agents. 2. Synthesis and biological activity of platinum complexes linked to 9-anilinoacridine.', Journal Medicinal Chemistry, 33, pp. 3008 - 3014
    Journal articles | 1990
    Prakash AS; Denny WA; Gourdie T; Valu K; Woodgate P; Wakelin L, 1990, 'DNA-directed alkylating ligands as potential antitumour agents: sequence specificity of alkylation by intercalating aniline mustards', Biochemistry, 29, pp. 9799 - 9807
    Journal articles | 1990
    Prakash AS; Denny WA; Wakelin L, 1990, 'Differences in sequence selectivity of DNA alkylation by isomeric intercalating aniline mustards.', Chemistry-Biology Interactions, 76, pp. 241 - 248, http://dx.doi.org/10.1016/0009-2797(90)90091-Z
    Journal articles | 1990
    Roberts A; Denny WA; Wakelin L; Anderson B; Wilson W, 1990, 'Radio-sensitisation of mammalian cells in vitro by nitroacridines', Radiation Research, 123, pp. 153 - 164, http://dx.doi.org/10.2307/3577539
    Journal articles | 1990
    Searle M; Wakelin L, 1990, 'Conformation and dynamics of the deoxyribose rings in the (nogalamycin)2/d(GCATGC)2 complex studied in solution by 1H NMR spectroscopy.', Biochemical Journal, 269, pp. 341 - 346, http://dx.doi.org/10.1042/bj2690341
    Journal articles | 1990
    Searle M; Wakelin L, 1990, 'Sequence-specific conformation of a DNA decamer containing an adenine tract studied in solution by 1H NMR spectroscopy.', Biochimica Biophysica Acta, 1049, pp. 69 - 77, http://dx.doi.org/10.1016/0167-4781(90)90085-G
    Journal articles | 1990
    Valu K; Gourdie T; Boritzki T; Gravatt G; Baguley BC; Wilson W; Wakelin L; Woodgate P; Denny WA, 1990, 'DNA-directed alkylating agents. 3. Structure activity relationships for acridine-linked aniline mustards: consequences of varying the length of the linker chain.', Journal Medicinal Chemistry, 33, pp. 3014 - 3019
    Journal articles | 1990
    Wakelin L; Chetcuti P; Denny WA, 1990, 'Kinetic and equilibrium studies of amsacrine-4-carboxamides: a class of asymmetrical DNA intercalating agent which must bind by threading through the DNA helix.', Journal Medicinal Chemistry, 33, pp. 2039 - 2044
    Journal articles | 1989
    Searle M; Hall J; Denny WA; Wakelin L, 1989, 'Interaction of the antitumour antibiotic luzopeptin with the hexanucleotide d(5'-GCATGC)2: one and two-dimensional NMR studies.', Biochemical Journal, 259, pp. 433 - 441, http://dx.doi.org/10.1042/bj2590433
    Journal articles | 1989
    Searle M; Hall J; Kyratsis L; Wakelin L, 1989, 'Didemnin B: conformation and dynamics of an antitumour and antiviral depsipeptide studied in solution by 1H and 13C NMR.', International Journal of Peptide and Protein Research, 34, pp. 445 - 454
    Journal articles | 1988
    Mcfadyen DW; Denny WA; Wakelin L, 1988, 'Alkyl-linked diquinolines are monofunctional AT-selective DNA intercalating agents.', FEBS Letters, 228, pp. 235 - 240, http://dx.doi.org/10.1016/0014-5793(88)80006-1
    Journal articles | 1988
    Searle M; Hall J; Denny WA; Wakelin L, 1988, 'NMR studies of the interaction of the antibiotic nogalamycin with the hexadeoxyribonucleotide duplex d(5'-GCATGC)2.', Biochemistry, 27, pp. 4340 - 4349
    Journal articles | 1988
    Searle M; Hall J; Wakelin L, 1988, '1H and 13C NMR studies of the antitumour antibiotic luzopeptin: resonance assignments, conformation and flexibility in solution.', Biochemical Journal, 256, pp. 271 - 278
    Journal articles | 1987
    Brownlee R; McFadyen DW; O'Connor M; Rook T; Roos I; Wakelin L, 1987, 'An NMR study of substituent effects in platinum (II) intercalating agents.', Magnetic Resonance in Chemistry, 25, pp. 492 - 496
    Journal articles | 1987
    Denny WA; Wakelin L, 1987, 'Mode and kinetics of DNA binding of the antitumour agent bisantrene.', Anti-Cancer Drug Design, 2, pp. 71 - 77
    Journal articles | 1987
    Mack P; Kelly D; Martin R; Wakelin L, 1987, 'DNA-binding compounds. II. Synthesis of a peptide-linked triacridine.', Australian Journal of Chemistry, 40, pp. 97 - 105, http://dx.doi.org/10.1071/CH9870097
    Journal articles | 1987
    Mcfadyen DW; Wakelin L; Roos I; Hillcoat B, 1987, 'Binding of dimeric platinum (II) terpyridine complexes to DNA.', Biochemical Journal, 242, pp. 177 - 183
    Journal articles | 1987
    Wakelin L; Atwel G; Rewcastle ; Denny WA, 1987, 'Relationships between DNA binding kinetics and biological activity for the 9-aminoacridine-4-carboxamide class of antitumour agent.', Journal Medicinal Chemistry, 30, pp. 855 - 861
    Journal articles | 1986
    Adams A; Jarrott B; Denny WA; Wakelin L, 1986, 'Differences between central and peripheral alpha-adrenoceptors revealed using binuclear ligands.', European Journal of Pharmacology, 127, pp. 27 - 35
    Journal articles | 1986
    Denny WA; Roos I; Wakelin L, 1986, 'Inter-relationships between antitumour activity, DNA breakage and DNA binding kinetics for 9-aminoacridinecarboxamide antitumour agents.', Anti-Cancer Drug Design, 1, pp. 141 - 146
    Journal articles | 1986
    Denny WA; Wakelin L, 1986, 'Kinetic and equilibrium studies of the interaction of amsacrine and anilino-ring substituted analogues with DNA.', Cancer Research, 46, pp. 1717 - 1721
    Journal articles | 1986
    Mcfadyen DW; Wakelin L; Roos I; Hillcoat B, 1986, 'Binuclear platinum (II) terpyridine complexes: a new class of bifunctional DNA intercalating agent.', Biochemical Journal, 238, pp. 757 - 763
    Journal articles | 1986
    Wakelin L, 1986, 'Polyfunctional DNA intercalating agents.', Medicinal Research Reviews, 6, pp. 275 - 340
    Journal articles | 1985
    Adams A; Jarrott B; Elmes B; Denny WA; Wakelin L, 1985, 'Interaction of DNA-intercalating antitumour agents with adrenoceptors.', Molecular Pharmacology, 27, pp. 480 - 492
    Journal articles | 1985
    Denny WA; Atwel G; Baguley BC; Wakelin L, 1985, 'Potential antitumour agents. Part 44. Synthesis and antitumour activity of new classes of diacridines: the importance of linker chain rigidity for DNA-binding kinetics and antitumour activity.', Journal Medicinal Chemistry, 28, pp. 1568 - 1574
    Journal articles | 1985
    Denny WA; Atwel G; Willmott ; Wakelin L, 1985, 'Interaction of paired homologous series of diacridines and triacridines with deoxyribonucleic acid.', Journal of Biophysical Chemistry, 22, pp. 17 - 26, http://dx.doi.org/10.1016/0301-4622(85)80022-3
    Journal articles | 1985
    KELLY DP; MACK PO; MARTIN RF; WAKELIN LPG, 1985, 'DNA‐binding compounds – synthesis and intercalating properties of a peptide‐diamino diacridine', International Journal of Peptide and Protein Research, 26, pp. 400 - 406, http://dx.doi.org/10.1111/j.1399-3011.1985.tb01006.x
    Journal articles | 1985
    Kelly D; Mack P; Martin R; Wakelin L, 1985, 'A linear peptide as linker chain in polyfunctional DNA-binding agents. Synthesis of a peptide diamino bisacridine.', International Journal of Peptide and Protein Research, 26, pp. 400 - 406
    Journal articles | 1985
    Mcfadyen DW; Wakelin L; Roos I; Leopold V, 1985, 'Activity of platinum (II) intercalating agents against murine leukaemia L1210.', Journal Medicinal Chemistry, 28, pp. 1113 - 1116
    Journal articles | 1985
    Roos I; Wakelin L; Hakkennes J; Coles J, 1985, 'Collection and analysis of kinetic data from a stopped-flow spectrophotometer using a microcomputer.', Analytical Biochemistry, 146, pp. 287 - 298
    Journal articles | 1985
    Roos I; Wakelin L; Henry S, 1985, 'Intracellular DNA damage produced by a series of diacridines.', Biochemical Journal, 226, pp. 175 - 182
    Journal articles | 1984
    Wakelin L; McFadyen DW; Walpole A; Roos I, 1984, 'Interaction of phenylthiolato (2,2',2''-terpyridine) platinum (II) cation with DNA.', Biochemical Journal, 222, pp. 203 - 215
    Journal articles | 1982
    Kobylecki R; Lane A; Smith C; Wakelin L; Cruze W; Egert E; Kennard O, 1982, 'N-methyl nalorphine: definition of N-allyl conformation for antagonism of the opiate receptor.', Journal of Medicinal Chemistry, 25, pp. 1278 - 1280, http://dx.doi.org/10.1021/jm00353a002
    Journal articles | 1981
    Fox K; Wakelin L; Waring M, 1981, 'Kinetics of the interaction between echinomycin and DNA.', Biochemistry, 20, pp. 5768 - 5779
    Journal articles | 1981
    Fox KR; Wakelin LPG; Waring MJ, 1981, 'Kinetics of the Interaction between Echinomycin and Deoxyribonucleic Acid', Biochemistry, 20, pp. 5768 - 5779, http://dx.doi.org/10.1021/bi00523a020
    Journal articles | 1981
    Viswamitra M; Kennard O; Cruze W; Egert E; Sheldrick G; Jones P; Waring M; Wakelin L; Olsen F, 1981, 'The structure of the quinoxaline antibiotic analogue TANDEM and its relevance to the mechanism of bifunctional intercalation.', Nature, 289, pp. 817 - 819
    Journal articles | 1981
    Viswamitra MA; Kennard O; Cruse WBT; Egert E; Sheldrick GM; Jones PG; Waring MJ; Wakelin LPG; Olsen RK, 1981, 'Structure of TANDEM and its implication for bifunctional intercalation into DNA', Nature, 289, pp. 817 - 819, http://dx.doi.org/10.1038/289817a0
    Journal articles | 1981
    Wakelin L; Hunter C; Adams A; Waring M, 1981, 'Interaction of crystal violet with nucleic acids.', Biochemistry, 20, pp. 5779 - 5787
    Journal articles | 1981
    Wilson W; Baguley BC; Wakelin L; Waring M, 1981, 'Interaction of the antitumour drug m-AMSA and related acridines with nucleic acids.', Molecular Pharmacology, 20, pp. 404 - 414
    Journal articles | 1981
    Wilson WR; Baguley BC; Wakelin LPG; Waring MJ, 1981, 'Interaction of the antitumor drug 4'-(9-acridinylamino)methanesulfon-m-anisidide and related acridines with nucleic acids', Molecular Pharmacology, 20, pp. 404 - 414
    Journal articles | 1980
    Dean P; Wakelin L, 1980, 'Electrostatic components of drug-receptor recognition: I. Structural and sequence analogues of DNA polynucleotides.', Proceedings of the Royal Society, B, 209, pp. 453 - 471
    Journal articles | 1980
    Dean P; Wakelin L, 1980, 'Electrostatic components of drug-receptor recognition: II. The DNA-binding antibiotic actinomycin.', Proceedings of the Royal Society, B, 209, pp. 473 - 489, http://dx.doi.org/10.1098/rspb.1980.0108
    Journal articles | 1980
    Wakelin L; Waring M, 1980, 'Kinetics of drug-DNA interaction: dependence of the binding mechanism on structure of the ligand.', Journal of Molecular Biology, 144, pp. 183 - 214
    Journal articles | 1980
    Wright RGMR; Wakelin LPG; Fieldes A; Acheson RM; Waring MJ, 1980, 'Effects of Ring Substituents and Linker Chains on the Bifunctional Intercalation of Diacridines into Deoxyribonucleic Acid', Biochemistry, 19, pp. 5825 - 5836, http://dx.doi.org/10.1021/bi00566a026
    Journal articles | 1979
    Dean P; Wakelin L, 1979, 'The docking manoeuvre at a drug receptor: a quantum mechanical study of intercalative attack of ethidium and its carboxylated derivative on a DNA fragment.', Philosphical Transactions of the Royal Society, B, 287, pp. 571 - 607
    Journal articles | 1979
    Wakelin L; Creasy T; Waring M, 1979, 'The binding of an homologous series of diacridines to DNA.', FEBS Letters, 104, pp. 261
    Journal articles | 1978
    Balcarova Z; Kleinwà chter V; Koudelka J; Lober G; Reinert K; Wakelin L; Waring M, 1978, 'Interaction of phenosafranine with nucleic acids and model polyphosphates. II. Characterisation of phenosafranine binding to double helical DNAs.', Biophysical Chemistry, 8, pp. 27 - 40
    Journal articles | 1978
    Balcarová Z; Kleinwächter V; Koudelka J; Klarner R; Löber G, 1978, 'Interaction of phencsafranine with nucleic acids and model polyphosphates. I. Self-aggregation and complex formation with inorganic polyphosphates', Biophysical Chemistry, 8, pp. 17 - 25, http://dx.doi.org/10.1016/0301-4622(78)85019-4
    Journal articles | 1978
    Kleinwachter V; Balcarova Z; Koudelka J; Lober G; Reinert K; Wakelin L; Waring M, 1978, 'Characterisation of different modes of phenosafranine binding to double helical DNAs.', Studia Biophysica, 67, pp. S53 - S54, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1978ED19800028&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Journal articles | 1978
    Wakelin L; Romanos M; Chen T; Glaubiger D; Canellakis E; Waring M, 1978, 'Structural limitations on the bifunctional intercalation of diacridines into DNA.', Biochemistry, 17, pp. 5057 - 5063
    Journal articles | 1976
    Balcarova Z; Kleinwächter V; Waring M; Wakelin L; Lober G, 1976, 'Properties of phenosafranine complexes with deoxyribonucleic acids.', Studia Biophysica, 60, pp. 119 - 124
    Journal articles | 1976
    Wakelin L; Romanos M; Canellakis E; Waring M, 1976, 'Diacridines as bifunctional DNA-intercalating agents.', Studia Biophysica, 60, pp. 111 - 118
    Journal articles | 1976
    Wakelin L; Waring M, 1976, 'The binding of echinomycin to DNA.', Biochemical Journal, 157, pp. 721 - 740
    Journal articles | 1975
    Waring M; Wakelin L; Lee J, 1975, 'A solvent partition method for measuring the binding of drugs to DNA: application to the quinoxaline antibiotics echinomycin and triostin A.', BIOCHIMICA ET BIOPHYSICA ACTA, 407, pp. 200 - 212
    Journal articles | 1974
    Wakelin L; Waring M, 1974, 'The unwinding of circular deoxyribonucleic acid by phenanthridinium drugs: structure-activity relations for the intercalation reaction.', Molecular Pharmacology, 10, pp. 544 - 561
    Journal articles | 1974
    Wakelin L, 1974, 'Interaction of platinum II compounds with circular DNA.', Biochemical Society Transactions, 2, pp. 866 - 868, http://dx.doi.org/10.1042/bst0020866
    Journal articles | 1974
    Waring M; Wakelin L, 1974, 'Echinomycin: a bifunctional intercalating antibiotic.', Nature, 252, pp. 653 - 657, http://dx.doi.org/10.1038/252653a0
    Journal articles | 1971
    Wall K; Wakelin L, 1971, 'Measurement of the rate of anion exchange and the effect of organic fouling.', Journal of Applied Chemistry and Biotechnology, 21, pp. 1 - 4
  • Conference Papers | 2017
    Pracey CP; Serobian A; Thomas DS; Ball GE; Wakelin LP, 2017, 'Solution structure of the Mitoxantrone-DNA complex: A NMR and molecular modelling study', in EUROPEAN BIOPHYSICS JOURNAL WITH BIOPHYSICS LETTERS, SPRINGER, SCOTLAND, British Biophys Soc, Edinburgh, pp. S228 - S228, presented at 19th IUPAB Congress / 11th EBSA Congress, SCOTLAND, British Biophys Soc, Edinburgh, 16 July 2017 - 20 July 2017, https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000416406201323&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a29b250adbe88d1
    Conference Papers | 2010
    Zihlif M; Wakelin L; Catchpool D; Stewart BBW, 2010, 'Insights into the cellular responses against different DNA-binding agents', in EJC SUPPLEMENTS, PERGAMON-ELSEVIER SCIENCE LTD, GERMANY, Berlin, pp. 105 - 105, presented at 22nd EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics, GERMANY, Berlin, 16 November 2010 - 19 November 2010, http://dx.doi.org/10.1016/S1359-6349(10)72036-X
    Conference Papers | 2008
    Freewan M; Denny WA; Wakelin L, 2008, 'Poisoning of human topoisomerase II alpha by acridinecarboxamides and related cytotoxins', in EJC Supplements, Pergamon-Elsevier Science Ltd, Kidlington, Oxford, England, pp. 28 - 28, presented at 20th Meeting of the European Association for Cancer Research, Lyon, FRANCE, 05 July 2008 - 08 July 2008, http://dx.doi.org/10.1016/S1359-6349(08)71283-7
    Conference Papers | 2008
    Khazaly AN; He Z; Stewart BW; Edwards GL; Wakelin L, 2008, 'Bisintercalating threading agents as cytotoxic inhibitors of transcription', in EJC Supplements, Pergamon-Elsevier Science Ltd, Kidlington, Oxford, England, pp. 83 - 84, presented at 20th Meeting of the European Association for Cancer Research, Lyon, FRANCE, 05 July 2008 - 08 July 2008
    Conference Papers | 2006
    Edwards GL; Black DS; Deacon G; Wakelin L, 2006, 'Cycometallated platinum and palladium complexes as anticancer agents: Everything old is new again', in Australia and New Zealand Symposium on Organometallic Chemistry OZOM3, Monash university, Gippsland, Australia, pp. 47 - 47, presented at 3rd Australian and New Zealand Symposium on Oranometallic Chemistry, Monash university, Gippsland, Australia, 08 January 2006 - 11 January 2006
    Conference Papers | 2005
    Peters FB; Serobian A; Ball GE; Denny WA; Wakelin L, 2005, 'DNA Intercalation by bix(phenazinecarboxamides): Structural Insights Into Anticancer Activity', in Apte S; Kable S; Baker AT (eds.), Connect 2005 - Chemical Challenges for the 21st Century, Sydney, Convention Centre, Darling Harbour, Sydney, pp. M017 PO Bi - -, presented at Connect 2005 - Chemical Challenges for the 21st Century, Sydney, Convention Centre, Darling Harbour, Sydney, 03 July 2005 - 07 July 2005
    Conference Papers | 2005
    Tam R; Suzuki M; Denny WA; Dawes I; Wakelin L, 2005, 'Mutations within the alpha4 helix of human DNA topoisomerase IIalpha confer differential sensitivities to topoisomerase poisons.', in Proceedings of the American Association for Cancer Research vol 46, American Association for Cancer Research, Philadelphia, USA, pp. 2401 - 2401, presented at 96th AACR Annual Meeting, Anaheim, USA, -
    Conference Papers | 2003
    Catchpoole DR; Guo D; Stewart BW; Eleftheriou A; Wakelin L, 2003, 'Effects of bisintercalating DNA threading agents on transcription in human leukemic CCRF-CEM cells studied by microarray analysis', in CLINICAL CANCER RESEARCH, AMER ASSOC CANCER RESEARCH, MASSACHUSETTS, BOSTON, pp. 6082S - 6082S, presented at AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, MASSACHUSETTS, BOSTON, 17 November 2003 - 21 November 2003, https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000187467300053&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a29b250adbe88d1
    Conference Papers | 2002
    Adams A; Guss JM; Denny WA; Wakelin LP, 2002, 'CRYSTAL STRUCTURES OF ACRIDINE-4-CARBOXAMIDES COMPLEXED WITH THE DNA HEXANUCLEOTIDE d(CGTACG)2', in ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES, INT UNION CRYSTALLOGRAPHY, pp. C55 - C55, http://dx.doi.org/10.1107/S0108767302087317
    Conference Papers | 2001
    Adams A; Guss M; Denny WA; Wakelin L, 2001, 'Crystal structure of 9-amino[N-(2-morpholino)ethyl]acridine-4-carboxamide bound to d(CGTACG)2: A DNA complex of a biologically inactive derivative of the acridinecarboxamide topoisomerase poisons.', in Clinical Cancer Research vol 7, AMER ASSOC CANCER RESEARCH, PO BOX 11806, BIRMINGHAM, AL 35202 USA, Birmingham, USA., pp. 3798S - 3798S, presented at AACR-NCI-EORTC Conference on Molecular Targets and Cancer Therapeutics., Florida, USA., http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000172121800710&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Conference Papers | 2001
    Majid AA; Fonseka T; Smythe GA; Shiel M; Denny WA; Wakelin L, 2001, 'Characterisation of the DNA complex of an antitumour-active bifunctional polybenzamide alkylating agent using electrospray and MALDI-TOF mass spectrometry.', in Clinical Cancer Research vol 7, AMER ASSOC CANCER RESEARCH, PO BOX 11806, BIRMINGHAM, AL 35202 USA, Birmingham, USA., pp. 3796S - 3796S, presented at AACR-NCI-EORTC Conference on Molecular Targets and Cancer Therapeutics., Florida, USA, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000172121800700&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Conference Papers | 2000
    Adams A; Guss M; Collyer C; Prakash AS; Denny WA; Wakelin L, 2000, 'Acridinecarboxamide topoisomerase poisons: structural and kinetic studies of the DNA complexes of 5-substituted 9-amino-(N-(2-dimethylamino)ethyl)-acridine-4-carboxamides.', in Clinical Cancer Research vol 6, AMER ASSOC CANCER RESEARCH, PO BOX 11806, BIRMINGHAM, AL 35202 USA, Birmingham, USA, pp. 4531S - 4531S, presented at 11th NCI-EORTC-AACR Symposium on New Drugs in Cancer Therapy., Amsterdam, Holland.
    Conference Papers | 1999
    Adams A; Collyer C; Guss M; Denny WA; Wakelin L, 1999, 'Crystal structure of the topoisomerase II poison 9-amino-[N-(2-dimethylamino)ethyl]acridine-4-carboxamide bound to the DNA hexanucleotide d(CGTACG)2.', in Clinical Cancer Research vol 5, AMER ASSOC CANCER RESEARCH, PO BOX 11806, BIRMINGHAM, AL 35202 USA, Birmingham, USA., pp. 3854S - 3854S, presented at 10th NCI-EORTC-AACR Symposium on New Drugs in Cancer Therapy, Washington, USA., http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000083945700614&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Conference Papers | 1990
    Major B; Wickham G; Prakash AS; Wakelin L; Cotton R; Denny WA; Leaver D, 1990, 'CONFORMATIONAL DISTORTIONS INDUCED IN DNA UPON BINDING OF CISPLATIN AND INTERCALATING ANALOGS', in European Journal of Pharmacology Vol 183, Elsevier, Amsterdam, Netherlands, pp. 191 - 192, http://dx.doi.org/10.1016/0014-2999(90)93025-L
    Conference Papers | 1984
    Adams A; Jarrott B; Elmes B; Denny WA; Wakelin L, 1984, 'Interaction of diacridines and diquinolines with adrenoceptors.', in Proceedings of the Australian Biochemical Society vol 16, PROC AUST BIOCHEMICAL SOC, MONASH UNIV DEPT BIOCHEMISTRY, CLAYTON VICTORIA 3168, AUSTRALIA, Clayton, Victoria, Australia, pp. S87 - S87, presented at Australian Biochemical Society Meeting, Sydney, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1984ANC4600278&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Conference Papers | 1984
    Mcfadyen DW; Wakelin L; Leopold V; Roos I; Hillcoat B, 1984, 'Cytotoxicity of DNA intercalating platinum (II) complexes.', in Medical and Pediatric Oncology vol 13, WILEY-LISS, DIV JOHN WILEY & SONS INC 605 THIRD AVE, NEW YORK, NY 10158-0012, New York, USA, pp. 137 - 138, presented at Clinical Oncology Society of Australia Meeting, Melbourne, Australia, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1985AHS3500022&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Conference Papers | 1984
    Mcfadyen DW; Wakelin L; Leopold V; Roos I; Hillcoat B, 1984, 'Cytotoxicity of DNA intercalating platinum (II) complexes.', in Proceedings of the Australian Biochemical Society 1984, PROC AUST BIOCHEMICAL SOC, MONASH UNIV DEPT BIOCHEMISTRY, CLAYTON VICTORIA 3168, AUSTRALIA, Clayton, Victoria, Australia, pp. S44 - S44, presented at Australian Biochemical Society Meeting, Sydney, Australia, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1984ANC4600191&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Conference Papers | 1984
    Roos I; Wakelin L; Henry S, 1984, 'Interaction of diacridines with intracellular DNA.', in Proceedings of the Australian Biochemical Society Vol 16, PROC AUST BIOCHEMICAL SOC, MONASH UNIV DEPT BIOCHEMISTRY, CLAYTON VICTORIA 3168, AUSTR, Clayton, Victoria, Australia, pp. S19 - S19, presented at Australian Biochemical Society, Sydney, Australia, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1984ANC4600035&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Conference Papers | 1984
    Wakelin L; Denny WA; Atwel G, 1984, 'Kinetics of the interaction between 9-aminoacridinecarboxamides and DNA.', in Medical and Pediatric Oncology vol 13, WILEY-LISS, DIV JOHN WILEY & SONS INC 605 THIRD AVE, NEW YORK, NY 10158-0012, New York, USA, pp. 134 - 135, presented at Clinical Oncology Society of Australia Meeting, Melbourne, Australia, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1985AHS3500011&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a
    Conference Papers | 1983
    Roos I; Wakelin L; Hillcoat B; Henry S, 1983, 'The interaction of diacridines with cellular DNA.', in Medical and Pediatric Oncology vol 12, WILEY-LISS, DIV JOHN WILEY & SONS INC, 605 THIRD AVE, NEW YORK, NY 10158-0012, New York, USA, pp. 278 - 278, presented at Clinical Oncology Society of Australia Meeting, Brisbane, Australia, http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:A1984TC60000026&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=891bb5ab6ba270e68a

Total funds of $A3.5 million (at contemporary values) for studies of DNA-directed anti-cancer drugs. Sources include the UK Science Research Council, the UK Medical Research Council, the Australian Research Council, the Australian National Health and Medical Research Council, the Irish Research Council, the Irish Health Research Board, the Anti-Cancer Council of Victoria, the Association for International Cancer Research Scotland, and Cure Cancer Australia.

Cancer is a disease that kills one in three of us. Practically all cytotoxic cancer drugs inhibit the biochemical functions of DNA, many doing so by binding to DNA directly. Our current research focusses on the discovery of novel DNA-targeted alkylating agents for the treatment of the brain tumours glioblastoma (GB) and cranial metastatic triple negative breast cancer (TNBC). These are particularly lethal cancers, in large part, because the tumour is shielded from drugs in the circulation by the blood brain barrier (BBB).

The BBB puts stringent restrictions on the physical properties of drugs that can access the brain by diffusion. For example, molecular weight must be less than 500 Daltons, lipophilicity should have a log P of about 2.5, the polar surface area should be less than 90 Å sq, and the drug should be weakly basic. We are developing agents which accord with these requirements, that are intended to kill GB and cranial TNBC cancer cells by inhibiting DNA replication as a result of crosslinking their DNA strands in novel ways that cells will find difficult to repair.

This is a collaborative effort involving the School of Chemistry, the Auckland Cancer Society Research Centre, and colleagues at University College London, and the University of Southampton. Here, in the School of Chemistry, the work involves ligand design by molecular modelling facilitated by docking and molecular dynamics; organic synthesis; and mass spectrometry, NMR, and spectrophotometric studies of ligand binding to DNA. Cytotoxicity and antitumour activity are evaluated by colleagues in Auckland, sequence selectivity, mechanisms of crosslinking and repair, and crystal structures of DNA-drug complexes are investigated by colleagues in the UK.

Current Major Collaborators

Associate Professor Graham Ball, School of Chemistry, UNSW.
Associate Professor Luke Hunter, School of Chemistry, UNSW.
Professor Martina Stenzel, School of Chemistry, UNSW.
Dr. Donald Thomas, School of Chemistry, UNSW.
Professor William A. Denny, Auckland Cancer Society Research Centre, New Zealand.
Professor Bruce Baguley, Auckland Cancer Society Research Centre, New Zealand.
Dr. Euphemia Leung, Auckland Cancer Society Research Centre, New Zealand.
Professor John Hartley, University College London.
Associate Professor Gary Parkinson, University College London.
Professor Keith Fox, University of Southampton.

Society Memberships

Fellow of the Royal Society of Chemistry, UK, FRSC

Fellow of the Royal Australian Chemical Institute, FRACI

Fellow of the Royal Society of New South Wales, FRSN

Member of the Australasian Society of Clinical and Experimental Pharmacology and Toxicology, ASCEPT

Member of the Intellectual Property Society of Australia and New Zealand, IPSANZ

Member of AusBiotech

My Research Supervision

Mr. Christopher Pracey (Joint supervisor with Associate Professor Graham Ball).
Mr. Daniel Weissberger (Joint supervisor with Associate Professors Luke Hunter and Graham Ball, and Professor Martina Stenzel).