Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Philip G Humphreys"'
Autor:
Philip G. Humphreys, Niall A. Anderson, Paul Bamborough, Andrew Baxter, Chun-wa Chung, Rosa Cookson, Peter D. Craggs, Toryn Dalton, Julie C. L. Fournier, Laurie J. Gordon, Heather F. Gray, Matthew W. Gray, Richard Gregory, David J. Hirst, Craig Jamieson, Katherine L. Jones, Hripsimee Kessedjian, David Lugo, Grant McGonagle, Vipulkumar K. Patel, Christopher Patten, Darren L. Poole, Rab K. Prinjha, Cesar Ramirez-Molina, Inmaculada Rioja, Gail Seal, Kayleigh A. J. Stafford, Rishi R. Shah, Daniel Tape, Natalie H. Theodoulou, Laura Tomlinson, Sabri Ukuser, Ian D. Wall, Natalie Wellaway, Gemma White
Publikováno v:
Journal of Medicinal Chemistry. 65:15174-15207
The bromodomain and extra terminal (BET) family of proteins are an integral part of human epigenome regulation, the dysregulation of which is implicated in multiple oncology and inflammatory diseases. Disrupting the BET family bromodomain acetyl-lysi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::247c403b556d0cdc2a89bb75345904c1
https://doi.org/10.1021/acs.jmedchem.2c01102
https://doi.org/10.1021/acs.jmedchem.2c01102
Autor:
Patricia F Medeiros, Mythily Vimal, Vipulkumar Kantibhai Patel, John Evans, Neil R Carlson, Antonia J. Lewis, Paul Bamborough, Katherine L Jones, Jane E Smith, Michael O'Sullivan, Scott McCleary, Darren J. Mitchell, Heather Barnett, Chun-wa Chung, Gang Yao, Anthony W. J. Cooper, Rab K. Prinjha, Laurie Gordon, Mahnoor Mahmood, Peter D. Craggs, Isobel L Harada, Rino A Bit, Natalie Wellaway, Armelle Le Gall, Robert J. Watson, Tony W Dean, Dominique Amans, Ian D. Wall, Kayleigh A J Stafford, Dave Lugo, Matthew J Lindon, Rishi R Shah, David Jonathan Hirst, Chris Patten, Darren L Poole, Jack A Brown, Philip G Humphreys, Robert P Davis, Christopher Roland Wellaway, Pamela J Thomas
Publikováno v:
Journal of Medicinal Chemistry. 63:714-746
The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) post-translational modifications on histone tails. These interactions
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdb502737af78aed357d47636c87313d
https://doi.org/10.1021/acs.jmedchem.9b01670
https://doi.org/10.1021/acs.jmedchem.9b01670
Autor:
Nicholas C. O. Tomkinson, Jonathan M. Curle, Alan R. Kennedy, Marina C. Perieteanu, Philip G. Humphreys
Publikováno v:
Organic Letters
Malonoyl peroxide [6] is an effective reagent for the syn- or anti-oxyamination of alkenes. Reaction of [6] and an alkene in the presence of O-tert-butyl-N-tosylcarbamate (R3 = CO2tBu) leads to the anti-oxyaminated product in up to 99% yield. Use of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9fa6b51621cc45940054e6ceefcb44eb
http://europepmc.org/articles/PMC7146911
http://europepmc.org/articles/PMC7146911
Publikováno v:
ChemMedChem. 14:362-385
The bromodomain and extra terminal (BET) family of bromodomain‐containing proteins (BCPs) have been the subject of extensive research over the past decade, resulting in a plethora of high‐quality chemical probes for their tandem bromodomains. In
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b3ddf6e17dc514b37808da13bc2cb9e
https://doi.org/10.1002/cmdc.201800738
https://doi.org/10.1002/cmdc.201800738
Autor:
Emmanuel Hubert Demont, Philip G. Humphreys, Alex Phillipou, Michael A. Clegg, Paul Bamborough, Peter D. Craggs, Chun-wa Chung, Rab K. Prinjha, Gemma Michele Liwicki, Nicholas C. O. Tomkinson, Natalie Hope Theodoulou, Laurie J. Gordon
Publikováno v:
ACS Med Chem Lett
[Image: see text] Bromodomain containing proteins and the acetyl-lysine binding bromodomains contained therein are increasingly attractive targets for the development of novel epigenetic therapeutics. To help validate this target class and unravel th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a371aaebd689aa1b81c6ef189c8b2232
https://pubmed.ncbi.nlm.nih.gov/34413961
https://pubmed.ncbi.nlm.nih.gov/34413961
Autor:
Corentine M C, Laurin, Joseph P, Bluck, Anthony K N, Chan, Michelle, Keller, Andrew, Boczek, Amy R, Scorah, K F Larissa, See, Laura E, Jennings, David S, Hewings, Fern, Woodhouse, Jessica K, Reynolds, Matthias, Schiedel, Philip G, Humphreys, Philip C, Biggin, Stuart J, Conway
Publikováno v:
ACS infectious diseases. 7(8)
The
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::e030c77cf6bcf268bf3807d21e74595e
https://pubmed.ncbi.nlm.nih.gov/33203208
https://pubmed.ncbi.nlm.nih.gov/33203208
Autor:
Ishna N. Mistry, Philip G. Humphreys, Panagis Filippakopoulos, Amy Hicks, Pavel Guzanov, Laura E. Jennings, Larissa See, Jessica K. Reynolds, Amy R. Scorah, Matthias Schiedel, Anna K. Mapp, James Clayton, David S. Hewings, Paul A. Bruno, Mustafa Moroglu, Charles N. G. Evans, Corentine M.C. Laurin, Stuart J. Conway, Joseph P. Bluck, Ester M. Hammond, Giulia Stazi, Sarah Picaud, Philip C. Biggin
Publikováno v:
Bioorganic & Medicinal Chemistry
Ligands for the bromodomain and extra-terminal domain (BET) family of bromodomains have shown promise as useful therapeutic agents for treating a range of cancers and inflammation. Here we report that our previously developed 3,5-dimethylisoxazole-ba
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5288898f111ff477f3c2c64891244a9
https://doi.org/10.1016/j.bmc.2018.05.003
https://doi.org/10.1016/j.bmc.2018.05.003
Publikováno v:
Current Opinion in Chemical Biology. 33:58-66
Bromodomains have emerged as an exciting target class for drug discovery over the past decade. Research has primarily focused on the bromodomain and extra terminal (BET) family of bromodomains, which has led to the development of multiple small molec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5db86cae2274bdedd2efb380e57036f
https://doi.org/10.1016/j.cbpa.2016.05.028
https://doi.org/10.1016/j.cbpa.2016.05.028
Autor:
Rab K. Prinjha, Anne Rueger, Neil Stuart Garton, Dirk Eberhard, David Matthew Wilson, Marcus Bantscheff, Robert J. Sheppard, Kevin Lee, Jack A. Brown, Nigel Ramsden, Susan Marie Westaway, Gerard Drewes, Philip G. Humphreys, Toby Mathieson, Gerard Joberty, Marcel Muelbaier, Valerie Reader, Markus Boesche
Publikováno v:
ACS Chemical Biology. 11:2002-2010
The 2-oxoglutarate-dependent dioxygenase target class comprises around 60 enzymes including several subfamilies with relevance to human disease, such as the prolyl hydroxylases and the Jumonji-type lysine demethylases. Current drug discovery approach
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1e514fee0ea43db13a3bff9292a026a
https://doi.org/10.1021/acschembio.6b00080
https://doi.org/10.1021/acschembio.6b00080
Autor:
Rab K. Prinjha, Alex Preston, Inma Rioja, Roy Katso, Melanie Leveridge, Chun-wa Chung, Michael David Barker, Laurens Kruidenier, Gerard Joberty, Kevin Lee, Onkar M. P. Singh, Joanna Taylor, Matthew Campbell, Michelle Pemberton, Fiona Brown, Robert Eagle, Carl Haslam, David Matthew Wilson, Neil Stuart Garton, Tracy Jane Shipley, Colin J. Suckling, Philip G. Humphreys, Gerard Drewes, Laurie J. Gordon, Pamela Thomas, Jack A. Brown, Gail A. Seal, Thomas George Christopher Hayhow, Susan Marie Westaway
Publikováno v:
Journal of Medicinal Chemistry. 59:1370-1387
Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1dd41f32203668dbba76c4b0b0fbc2e4
https://doi.org/10.1021/acs.jmedchem.5b01538
https://doi.org/10.1021/acs.jmedchem.5b01538