Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Clare Gregson"'
Autor:
David Longmire, Haley Woods, Phillip B Rawlins, Jessie Hao-Ru Hsu, Daniel H O' Donovan, Alexandra Borodovsky, Peng Wang, Sharan K Bagal, Shaun M Fillery, Peter Barton, Clare Gregson, Beth Williamson, Samuel C Nash, Andrew Pike, Jon A Read, Kurt Gordon Pike, Andrew Bloecher, Erin Code, Minhui Shen, Sameer Kawatkar, Youfeng Nai, Jia Tang, Chengzhi Li, James C. Robinson
Publikováno v:
Journal of Medicinal Chemistry. 64:17146-17183
Aberrant activity of the histone methyltransferase polycomb repressive complex 2 (PRC2) has been linked to several cancers, with small-molecule inhibitors of the catalytic subunit of the PRC2 enhancer of zeste homologue 2 (EZH2) being recently approv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cfbef686d9310c0393124b8f8df7ca38
https://doi.org/10.1021/acs.jmedchem.1c01161
https://doi.org/10.1021/acs.jmedchem.1c01161
Publikováno v:
Expert Opinion on Therapeutic Patents. 31:119-135
PRC2 is a histone methyltransferase complex associated with several cancer types. Tazemetostat was recently approved as the first inhibitor targeting the catalytic subunit EZH2 and several other EZH2 inhibitors are now under clinical evaluation. Beyo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1496a9d48dda47419e6ed10dacb321c2
https://doi.org/10.1080/13543776.2021.1841167
https://doi.org/10.1080/13543776.2021.1841167
Autor:
Darren Cross, Matthew J. Martin, Carine M. Guérot, Nicolas Floc'h, Clare Gregson, Jonathan P. Orme, Michal Bista, Lin Xue, Xu Li, Amar Rahi, Xiliang Zhao, Richard A. Ward, L. Evans, Gail L. Wrigley, Arash Mosallanejad, Tieguang Yao, Claire McWhirter, David J. Hargreaves, Nicola Colclough, Sue Bickerton, Darren Mckerrecher, Peter Barton, Yang Ye, Yi Liu, Marta Wylot, M. Raymond V. Finlay, Xiaoming Kang, Eva M. Lenz, Daniel O'Neill, Verity Talbot, Olivier Lorthioir, Paul D. Smith
Publikováno v:
Journal of medicinal chemistry. 64(18)
The epidermal growth factor receptor (EGFR) harboring activating mutations is a clinically validated target in non-small-cell lung cancer, and a number of inhibitors of the EGFR tyrosine kinase domain, including osimertinib, have been approved for cl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58199c545ee296c2c44cec7db12bfba5
https://pubmed.ncbi.nlm.nih.gov/34491761
https://pubmed.ncbi.nlm.nih.gov/34491761
Publikováno v:
Organic letters. 21(22)
The facile synthesis of both saturated and unsaturated tricyclic pyrrolo-pyridones starting from a single readily available, common monocyclic reagent has been developed. An intermolecular annulation via a tandem Buchwald-Hartwig/Heck reaction led to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f53bb247d52b170a042c167d4085f1ec
https://pubmed.ncbi.nlm.nih.gov/31696715
https://pubmed.ncbi.nlm.nih.gov/31696715
Autor:
Sameer Kawatkar, Jon Read, Ron Tomlinson, S. Bagal, Huawei Chen, James Robinson, Jonathan Tart, Erin Code, Daniel Hillebrand O'donovan, Xiahui Zhu, Philip B. Rawlins, Ning Gao, Clare Gregson, Karen Jones, Tony Cheung, Andy Bloecher
Publikováno v:
ACS Chemical Biology.
Enhancer of zeste homologue 2 (EZH2), the catalytic subunit of polycomb repressive complex 2 (PRC2), regulates chromatin state and gene expression by methylating histone H3 lysine 27. EZH2 is overexpressed or mutated in various hematological malignan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::096f021bbf396a838ab6fe03afd94bb8
https://doi.org/10.1021/acschembio.9b00468
https://doi.org/10.1021/acschembio.9b00468
Autor:
Sameer Kawatkar, Philip B. Rawlins, Kurt Gordon Pike, Jessie Hao-Ru Hsu, Shaun M. Fillery, Clare Gregson, Minhui Shen, Daniel H. O' Donovan, Martin J. Packer, Jon Read, S. Bagal, Andrew Bloecher, Beth Williamson, James Robinson, Peter Barton, Ryan Greenwood, Erin Code, Haley Woods
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 39:127904
Free Energy Perturbation (FEP) calculations can provide high-confidence predictions of the interaction strength between a ligand and its protein target. We sought to explore a series of triazolopyrimidines which bind to the EED subunit of the PRC2 co
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b19eb341b997e66a555f392e58836843
https://doi.org/10.1016/j.bmcl.2021.127904
https://doi.org/10.1016/j.bmcl.2021.127904
Publikováno v:
Tetrahedron Letters. 55:6734-6737
A synthetic strategy for the synthesis of a library of 4- N -benzylamino-2- N -phenyl-pyridines is herein described. The approach involves a Pd-assisted cross-coupling of a 4-chloro- N -phenylpyridin-2-amine intermediate with a range of benzylamines.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e4bb4bac1efc6f361ea3284285e4f28e
https://doi.org/10.1016/j.tetlet.2014.09.115
https://doi.org/10.1016/j.tetlet.2014.09.115
Publikováno v:
ChemInform. 46
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::07e35a2d46f3b0df4bf907ad15eed534
https://doi.org/10.1002/chin.201516058
https://doi.org/10.1002/chin.201516058
Autor:
Clare Gregson, Shaun M. Fillery, Emma J. Williams, Ryan Greenwood, Kurt Gordon Pike, Lorraine A. Hassall, Thomas M. McGuire, Kevin Blades, Julie Demeritt, Kevin Michael Foote
Publikováno v:
ChemInform. 45
Two novel synthetic strategies that allow rapid diversification of the sulfone moiety in sulfonylmethyl pyrimidines, a class of compounds with a wide range of biological activity, which are of interest in a wide variety of drug discovery programmes,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::02e75da52bb056da471a8b0a5f888685
https://doi.org/10.1002/chin.201452160
https://doi.org/10.1002/chin.201452160