By Associate Professor Laurence P. G. Wakelin

Book Chapters

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, InTech, November, 2011, pp. 3 - 30

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

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

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, Pergamon Press, Oxford, UK, pp. 703 - 724

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, Kluwer Academic Publishers, Dordrecht, pp. 191 - 206

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, Adenine Press, USA, pp. 329 - 337

Journal articles

Zihlif M; Catchpoole DR; Stewart BW; Wakelin LPG, 2022, 'Withdrawn: Variations in Altered Global Gene Expression caused by Topoisomerase II Poisons Assessed with Reference to Differences in DNA Binding.', Curr Mol Pharmacol,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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Howarth N; Wakelin L, 1997, 'Alpha-PNA: A novel peptide nucleic acid analogue of DNA.', Journal Organic Chemistry, 62, pp. 5441 - 5450

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