Search Results - "Wakelin, Laurence P. G."

Exploring DNA topoisomerase I ligand space in search of novel anticancer agents by Drwal, Malgorzata N, Agama, Keli, Wakelin, Laurence P G, Pommier, Yves, Griffith, Renate

“…DNA topoisomerase I (Top1) is over-expressed in tumour cells and is an important target in cancer chemotherapy. It relaxes DNA torsional strain generated…”
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In vitro assessment of novel transcription inhibitors and topoisomerase poisons in rhabdomyosarcoma cell lines by Wolf, Steven J, Wakelin, Laurence P. G, He, Zhicong, Stewart, Bernard W, Catchpoole, Daniel R

“…Purpose Rhabdomyosarcoma (RMS) is the most common soft tissue sarcoma in children. Current chemotherapy regimes include the topoisomerase II poison etoposide…”
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Novel DNA topoisomerase IIα inhibitors from combined ligand- and structure-based virtual screening by Drwal, Malgorzata N, Marinello, Jessica, Manzo, Stefano G, Wakelin, Laurence P G, Capranico, Giovanni, Griffith, Renate

“…DNA topoisomerases are enzymes responsible for the relaxation of DNA torsional strain, as well as for the untangling of DNA duplexes after replication, and are…”
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[Co(III)(cyclen)Cl 2]Cl is selectively cytotoxic to human leukaemia cells by He, Zhicong, Lai, Donna, Wakelin, Laurence P.G.

“…Co(III)-cyclen complexes are known to cause DNA strand breaks by hydrolytically cleaving the phosphodiester backbone via a mechanism that does not require…”
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The solution structure of bis(phenazine-1-carboxamide)-DNA complexes: MLN 944 binding corrected and extended by Serobian, Andre, Thomas, Donald S., Ball, Graham E., Denny, William A., Wakelin, Laurence P. G.

“…ABSTRACT MLN 944 is a bisintercalating DNA‐binding antitumor agent known to be a template inhibitor of transcription. Previous 1H NMR studies of its d(ATGCAT)2…”
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Bisintercalating Threading Diacridines:  Relationships between DNA Binding, Cytotoxicity, and Cell Cycle Arrest by Wakelin, Laurence P. G, Bu, Xianyong, Eleftheriou, Alexandra, Parmar, Alpesh, Hayek, Charbel, Stewart, Bernard W

“…We have synthesized a series of bis(9-aminoacridine-4-carboxamides) linked via the 9-position with neutral flexible alkyl chains, charged flexible polyamine…”
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DNA threading bis(9-aminoacridine-4-carboxamides): Effects of piperidine sidechains on DNA binding, cytotoxicity and cell cycle arrest by He, Zhicong, Bu, Xianyong, Eleftheriou, Alexandra, Zihlif, Malik, Qing, Zhang, Stewart, Bernard W., Wakelin, Laurence P.G.

“…A series of bis(9-aminoacridine-4-carboxamides) with ethylpiperidino and N-methylpiperidin-4-yl sidechains were synthesized and evaluated for the effects on…”
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Molecular dynamic simulations of diacridine binding to DNA: Indications that C6 diacridine can bisintercalate spanning two base pairs by Rowell, Keiran N., Thomas, Donald S., Ball, Graham E., Wakelin, Laurence P. G.

“…Dimers of 9‐aminoacridine linked via the 9‐amino group with polymethylene chains, termed diacridines, are known to bisintercalate into DNA when the linker…”
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Mass Spectrometry Studies of the Binding of the Minor Groove-Directed Alkylating Agent Alkamin to AT-Tract Oligonucleotides by Abdul Majid, Amin M. S, Smythe, George, Denny, William A, Wakelin, Laurence P. G

“…Minor groove binding alkylating agents, which have potential as cancer drugs, generate cytotoxic DNA adducts that are relatively resistant to repair as a…”
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Structures and dynamics of DNA complexes of the desmethyl analog of the cytotoxin MLN944: Insights into activity when a methyl isn't futile by Serobian, Andre, Pracey, Christopher P., Thomas, Donald S., Denny, William A., Ball, Graham E., Wakelin, Laurence P. G.

“…Structure activity relationships for tricyclic‐carboxamide topoisomerase II poisons indicate that cytotoxicity is enhanced by the presence of methyl, and…”
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Structure of the d(CGCGAATTCGCG)2 complex of the minor groove binding alkylating agent alkamin studied by mass spectrometry by Majid, Amin M S Abdul, Smythe, George, Denny, William A, Wakelin, Laurence P G

“…Nitrogen mustard alkylating agents are important cancer drugs. Much interest has been focused on redirecting their covalent adducts from the N7 atoms of…”
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Kinetic Studies of the Binding of Acridinecarboxamide Topoisomerase Poisons to DNA:  Implications for Mode of Binding of Ligands with Uncharged Chromophores by Wakelin, Laurence P. G, Adams, Adrienne, Denny, William A

“…We have used stopped-flow spectrophotometry and the sodium dodecyl sulfate sequestration technique to study the kinetics of dissociation of DNA complexes of…”
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Intracellular trafficking as a determinant of AS-DACA cytotoxicity in rhabdomyosarcoma cells by Wolf, Steven J, Huynh, Tony, Bryce, Nicole S, Hambley, Trevor W, Wakelin, Laurence P G, Stewart, Bernard W, Catchpoole, Daniel R

“…Rhabdomyosarcoma (RMS) is a malignant soft tissue sarcoma derived from skeletal muscle precursor cells, which accounts for 5-8% of all childhood malignancies…”
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Crystal structure of 9-amino-N-[2-(4-morpholinyl)ethyl]-4-acridinecarboxamide bound to d(CGTACG)2: implications for structure-activity relationships of acridinecarboxamide topoisomerase poisons by Adams, Adrienne, Guss, J Mitchell, Denny, William A, Wakelin, Laurence P G

“…The structure of the complex formed between d(CGTACG)2 and 9-amino-N-[2-(4-morpholinyl)ethyl]-4-acridinecarboxamide, an inactive derivative of the antitumour…”
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Crystal Structure of the Topoisomerase II Poison 9-Amino-[N-(2-dimethylamino)ethyl]acridine-4-carboxamide Bound to the DNA Hexanucleotide d(CGTACG)2 by Adams, Adrienne, Guss, J. Mitchell, Collyer, Charles A, Denny, William A, Wakelin, Laurence P. G

“…The structure of the complex formed between d(CGTACG)2 and the antitumor agent 9-amino-[N-(2-dimethylamino)ethyl]acridine-4-carboxamide has been solved to a…”
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DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard by Gourdie, Trudi A, Valu, Kisione K, Gravatt, G. Lance, Boritzki, Theodore J, Baguley, Bruce C, Wakelin, Laurence P. G, Wilson, William R, Woodgate, Paul D, Denny, William A

“…A series of DNA-targeted aniline mustards have been prepared, and their chemical reactivity and in vitro and in vivo cytotoxicity have been evaluated and…”
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Major Groove Binding and ‘DNA-Induced' Fit in the Intercalation of a Derivative of the Mixed Topoisomerase I/II Poison N-(2-(Dimethylamino)ethyl)acridine-4- carboxamide (DACA) into DNA:  X-ray Structure Complexed to d(CG(5-BrU)ACG)2 at 1.3-Å Resolution by Todd, Alan K, Adams, Adrienne, Thorpe, James H, Denny, William A, Wakelin, Laurence P. G, Cardin, Christine J

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DNA-directed alkylating agents. 2. Synthesis and biological activity of platinum complexes linked to 9-anilinoacridine by Palmer, Brian D, Lee, Ho H, Johnson, Paul, Baguley, Bruce C, Wickham, Geoffrey, Wakelin, Laurence P. G, McFadyen, W. David, Denny, William A

“…Two different classes of cis-diaminedichloroplatinum(II) complexes linked to the DNA-intercalating chromophore 9-anilinoacridine have been synthesized and…”
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α-PNA:  A Novel Peptide Nucleic Acid Analogue of DNA by Howarth, Nicola M, Wakelin, Laurence P. G

“…Peptide nucleic acid (PNA) analogues of DNA have attracted interest as potential pharmacological regulators of gene expression since they have the capacity to…”
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A novel form of intercalation involving four DNA duplexes in an acridine-4-carboxamide complex of d(CGTACG)2 by Adams, A.

“…The structures of the complexes formed between 9-amino-[N-(2-dimethyl-amino)butyl]acridine-4-car-boxa-mide and d(CG5BrUACG)2 and d(CGTACG)2 have been solved by…”
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