Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Keith A. Menear"'
Autor:
Kristoffer Valerie, Timothy van Meter, Lawrence F. Povirk, Mark J. O'Connor, Keith A. Menear, Laurent Rigoreau, Marc Hummersone, Wei Yee Chong, Xiaoling F. Cockcroft, Mark Frigerio, Isa Hussaini, Nicholas Valerie, Elizabeth Rosenberg, Sarah E. Golding
Supplementary Data from Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9427b6f42606cf9cfd80b7c24538468c
https://doi.org/10.1158/1535-7163.22485738.v1
https://doi.org/10.1158/1535-7163.22485738.v1
Autor:
Kristoffer Valerie, Timothy van Meter, Lawrence F. Povirk, Mark J. O'Connor, Keith A. Menear, Laurent Rigoreau, Marc Hummersone, Wei Yee Chong, Xiaoling F. Cockcroft, Mark Frigerio, Isa Hussaini, Nicholas Valerie, Elizabeth Rosenberg, Sarah E. Golding
Ataxia telangiectasia (A-T) mutated (ATM) is critical for cell cycle checkpoints and DNA repair. Thus, specific small molecule inhibitors targeting ATM could perhaps be developed into efficient radiosensitizers. Recently, a specific inhibitor of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63df1a3370c90e12a492a8e058827180
https://doi.org/10.1158/1535-7163.c.6532065
https://doi.org/10.1158/1535-7163.c.6532065
Autor:
Niall M. B. Martin, Heather Mary Ellen Duggan, Kurt Gordon Pike, Sarah L. Pass, Marc Geoffrey Hummersone, Sylvie Gomez, Karine Malagu, Linette Ruston, Keith Allan Menear, Martin Pass
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1212-1216
The optimization of a potent and highly selective series of dual mTORC1 and mTORC2 inhibitors is described. An initial focus on improving cellular potency whilst maintaining or improving other key parameters, such as aqueous solubility and margins ov
Autor:
Celine Cano, Pia Thommes, Niall M. B. Martin, Yan Zhao, Liam Cornell, Michael A. Batey, Helen Jenkins, Jody Barbeau, Keith Allan Menear, Julia Bardos, Nicola J. Curtin, Michele Tavecchio, David R. Newell, Roger J. Griffin, Caroline Richardson, Graeme C. M. Smith, Andrew Slade, Joanne M. Munck
Publikováno v:
Molecular Cancer Therapeutics. 11:1789-1798
DNA double-strand breaks (DSB) are the most cytotoxic lesions induced by topoisomerase II poisons. Nonhomologous end joining (NHEJ) is a major pathway for DSB repair and requires DNA-dependent protein kinase (DNA-PK) activity. DNA-PK catalytic subuni
Autor:
Keith Allan Menear, Ian R. Hardcastle, Edward Jolyon Griffen, M. Raymond V. Finlay, Roger J. Griffin, Kate M. Clapham, Bernard T. Golding, Celine Cano, Attilla Ting, Turner Paul, Julia Bardos, Gail L. Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:966-970
Introduction of an O-alkoxyphenyl substituent at the 8-position of the 2-morpholino-4H-chromen-4-one pharmacophore enabled regions of the ATP-binding site of DNA-dependent protein kinase (DNA-PK) to be probed further. Structure-activity relationships
Autor:
Alastair H. Kyle, Jennifer H.E. Baker, Judit Banaáth, Samuel Edward Mann, Andrew I. Minchinton, Keith Allan Menear, Karen H. Fryer, Taixiang Wang, Soraya S. Porres, George Hynd
Publikováno v:
Molecular Cancer Therapeutics. 17:A110-A110
Targeting tumor hypoxia continues to be a goal of translational radiation oncology owing to overwhelming preclinical and clinical validation of the importance of tumor oxygenation to radiation sensitivity. We describe a rational, structure-based drug
Autor:
Sylvie Gomez, Karine Malagu, Thomas Presnot, Sally Ewen, Mihiro Sunose, Xiao-Ling Fan Cockcroft, Niall M. B. Martin, Alexandra Fundo, Armelle Le Gall, Keith Allan Menear, Hermann Gesine Johanna, Luisa Sebastian, Kristel Blackburn, Ian Hickson, Christine Bailey, Graeme C. M. Smith, Eleanor Torode, Kurt Gordon Pike
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5898-5901
A pharmacophore mapping approach, derived from previous experience of PIKK family enzymes, was used to identify a hit series of selective inhibitors of the mammalian target of rapamycin (mTOR). Subsequent refinement of the SAR around this hit series
Autor:
Kristoffer Valerie, Laurent Rigoreau, Nicholas C.K. Valerie, Marc Geoffrey Hummersone, Isa M. Hussaini, Keith Allan Menear, Lawrence F. Povirk, Wei Yee Chong, Mark Frigerio, Elizabeth Rosenberg, Xiao-Ling Fan Cockcroft, Mark J. O'Connor, Timothy E. Van Meter, Sarah E. Golding
Publikováno v:
Molecular Cancer Therapeutics. 8:2894-2902
Ataxia telangiectasia (A-T) mutated (ATM) is critical for cell cycle checkpoints and DNA repair. Thus, specific small molecule inhibitors targeting ATM could perhaps be developed into efficient radiosensitizers. Recently, a specific inhibitor of the
Autor:
Roger J. Griffin, Celine Cano, Bernard T. Golding, Attilla Ting, Mark Frigerio, Keith Allan Menear, Julia Bardos, Christopher M. Bailey, Marc Geoffrey Hummersone, Kappusamy Saravanan, Kerry Shea, Ian R. Hardcastle, Caroline Richardson, Nicola J. Curtin, Pia Thommes, Graeme C. M. Smith, David R. Newell
Publikováno v:
Journal of medicinal chemistry. 56(16)
Analogues of (dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-one (NU7441), a potent inhibitor of DNA-dependent protein kinase (DNA-PK; IC50 = 42 ± 2 nM), have been synthesized in which water-solubilizing groups [NHCO(CH₂)nNR¹R², where n =
Autor:
Xiao-Ling Fan Cockcroft, Graeme C. M. Smith, Marc Geoffrey Hummersone, David R. Newell, Mark Frigerio, Heather Mary Ellen Duggan, Olivier Barbeau, Christine Bailey, Nicola J. Curtin, Bernard T. Golding, Ian R. Hardcastle, Caroline Richardson, Charlotte Knights, Roger J. Griffin, Ben Spittle, Celine Cano, Keith Allan Menear
Publikováno v:
Journal of medicinal chemistry. 53(24)
Following the discovery of dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-one (NU7441) ( Leahy , J. J. J. ; Golding , B. T. ; Griffin , R. J. ; Hardcastle , I. R. ; Richardson , C. ; Rigoreau , L. ; Smith , G. C. M. Bioorg. Med. Chem. Lett. 200