Zobrazeno 1 - 10
of 43
pro vyhledávání: '"Niall M. B. Martin"'
Autor:
Diana Zatreanu, Helen M. R. Robinson, Omar Alkhatib, Marie Boursier, Harry Finch, Lerin Geo, Diego Grande, Vera Grinkevich, Robert A. Heald, Sophie Langdon, Jayesh Majithiya, Claire McWhirter, Niall M. B. Martin, Shaun Moore, Joana Neves, Eeson Rajendra, Marco Ranzani, Theresia Schaedler, Martin Stockley, Kimberley Wiggins, Rachel Brough, Sandhya Sridhar, Aditi Gulati, Nan Shao, Luned M. Badder, Daniela Novo, Eleanor G. Knight, Rebecca Marlow, Syed Haider, Elsa Callen, Graeme Hewitt, Joost Schimmel, Remko Prevo, Christina Alli, Amanda Ferdinand, Cameron Bell, Peter Blencowe, Chris Bot, Mathew Calder, Mark Charles, Jayne Curry, Tennyson Ekwuru, Katherine Ewings, Wojciech Krajewski, Ellen MacDonald, Hollie McCarron, Leon Pang, Chris Pedder, Laurent Rigoreau, Martin Swarbrick, Ed Wheatley, Simon Willis, Ai Ching Wong, Andre Nussenzweig, Marcel Tijsterman, Andrew Tutt, Simon J. Boulton, Geoff S. Higgins, Stephen J. Pettitt, Graeme C. M. Smith, Christopher J. Lord
Publikováno v:
Nature Communications, Vol 12, Iss 1, Pp 1-15 (2021)
Polθ has been recently identified as a therapeutic target in cancer but specific inhibitors are currently unavailable. Here, the authors identify small molecule inhibitors of Polθ’s polymerase activity which elicit BRCA1/2 synthetic lethality, en
Externí odkaz:
https://doaj.org/article/a5462d8522964b13a5f79a9e1b35250a
Autor:
Christina Alli, Christopher J. Lord, Marcel Tijsterman, Katherine Ewings, Marco Ranzani, Ai Ching Wong, Claire McWhirter, Martin Swarbrick, Harry Finch, Robert A. Heald, Rachel Brough, Nan Shao, Rebecca Marlow, Shaun Moore, Vera Grinkevich, Ellen Macdonald, Jayne Curry, Helen M. R. Robinson, Graeme Hewitt, Eleanor Knight, Christopher Bot, Syed Haider, Mathew Calder, Theresia A. Schaedler, Hollie McCarron, Luned M. Badder, Aditi Gulati, Martin Stockley, Eeson Rajendra, Sophie Langdon, Stephen J. Pettitt, Simon J. Boulton, Chris Pedder, Elsa Callen, Ed Wheatley, Wojciech Krajewski, André Nussenzweig, Daniela Novo, Peter Blencowe, Jayesh B. Majithiya, Laurent Rigoreau, Lerin Geo, Cameron Bell, Kimberley A. Wiggins, Diana Zatreanu, Geoff S. Higgins, Remko Prevo, Tennyson Ekwuru, Leon Pang, Simon N. Willis, Sandhya Sridhar, Marie Boursier, Diego Grande, Joana F. Neves, Mark Charles, Joost Schimmel, Andrew Tutt, Niall M. B. Martin, Omar Alkhatib, Amanda Ferdinand, Graeme C. M. Smith
Publikováno v:
Nature Communications, 12(1). NATURE RESEARCH
Nature Communications, Vol 12, Iss 1, Pp 1-15 (2021)
Nature Communications
Nature Communications, Vol 12, Iss 1, Pp 1-15 (2021)
Nature Communications
To identify approaches to target DNA repair vulnerabilities in cancer, we discovered nanomolar potent, selective, low molecular weight (MW), allosteric inhibitors of the polymerase function of DNA polymerase Polθ, including ART558. ART558 inhibits t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e50fa596497393cd588028cd95531690
https://hdl.handle.net/1887/3213877
https://hdl.handle.net/1887/3213877
Autor:
Diana A. Zatreanu, Helen M. R. Robinson, Omar Alkhatib, Marie Boursier, Harry Finch, Lerin Geo, Diego Grande, Vera Grinkevich, Robert Heald, Sophie Langdon, Jayesh Majithiya, Claire McWhirter, Niall M. B. Martin, Shaun Moore, Joana Neves, Eeson Rajendra, Marco Ranzani, Theresia Schaedler, Martin Stockley, Kimberley Wiggins, Rachel Brough, Sandhya Sridhar, Aditi Gulati, Nan Shao, Luned M Badder, Daniela Novo, Eleanor G. Knight, Rebecca Marlow, Syed Haider, Elsa Callen, Graeme Hewitt, Joost Schimmel, Remko Prevo, Christina Alli, Amanda Ferdinand, Cameron Bell, Peter Blencowe, Mathew Calder, Mark Charles, Jayne Curry, Tennyson Ekwuru, Katherine Ewings, Andre Nussenzweig, Marcel Tijsterman, Andrew Tutt, Simon J. Boulton, Geoff S. Higgins, Steve Pettitt, Graeme C. M. Smith, Christopher J. Lord
Publikováno v:
Molecular Cancer Therapeutics. 20:P056-P056
To target DNA repair vulnerabilities in cancer, we discovered nanomolar potent, selective, low molecular weight, allosteric inhibitors of the polymerase function of DNA polymerase Theta (Polθ), including ART558. ART558 inhibits the major Polθ-media
Autor:
Niall M. B. Martin, Bastiaan Evers, Charlotte Knights, Janneke E. Jaspers, Jos Jonkers, Attilla Ting, Henry Brown, Keith W. Caldecott, Sven Rottenberg, Rajesh Odedra, Lenka Oplustil O'Connor, Robert Hugh Bradbury, Aaron Cranston, David Alan Rudge, Mark J. O'Connor, Marina Pajic, Louise J. Jones, Alan Lau, Stuart L. Rulten
Publikováno v:
Cancer Research. 76:6084-6094
The PARP inhibitor AZD2461 was developed as a next-generation agent following olaparib, the first PARP inhibitor approved for cancer therapy. In BRCA1-deficient mouse models, olaparib resistance predominantly involves overexpression of P-glycoprotein
Publikováno v:
Nature Reviews. Drug Discovery
Key Points The deubiquitylating enzyme (DUB) family contains ~100 proteins that remove the post-translational modification ubiquitin from a variety of substrates.DUBs have key roles in various areas of cell biology of high relevance to pathologies su
Autor:
Yan Zhao, Nicola J. Curtin, Suzanne Kyle, Alan Lau, Niall M. B. Martin, Andrew Slade, Michael A. Batey, Caroline Richardson, David R. Newell
Publikováno v:
Molecular Cancer Therapeutics. 12:959-967
Ataxia telangiectasia mutated (ATM) kinase signals DNA double-strand breaks (DSB) to cell-cycle arrest via p53 and DNA repair. ATM-defective cells are sensitive to DSB-inducing agents, making ATM an attractive target for anticancer chemo- and radiose
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:
Ellen Wientjens, Niall M. B. Martin, Jos Jonkers, Ariena Kersbergen, Alan Lau, Liesbeth van Deemter, Sven Rottenberg, Serge A.L. Zander, Mark J. O'Connor, James H. Doroshow, Jiuping Ji, Ute Boon, Rinske Drost, Piet Borst, Amal Aly, Aaron Cranston, Janneke E. Jaspers, Shridar Ganesan, Wendy Sol
Publikováno v:
Cancer Discovery; Vol 3
Cancer discovery, 3(1), 68-81. American Association for Cancer Research Inc.
Cancer discovery, 3(1), 68-81. American Association for Cancer Research Inc.
Inhibition of PARP is a promising therapeutic strategy for homologous recombination–deficient tumors, such as BRCA1-associated cancers. We previously reported that BRCA1-deficient mouse mammary tumors may acquire resistance to the clinical PARP inh
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:
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