Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Alex Phillipou"'
Autor:
Marcus Bantscheff, Christian Eberl, Chun-wa Chung, Nicholas C. O. Tomkinson, Stephanie Lehmann, Ken G. M. Fantom, Jacob T. Bush, Alex Phillipou, Christopher J. Schofield, Francesca Zappacosta, David J. Fallon, Vipulkumar Kantibhai Patel
Publikováno v:
Chemistry – A European Journal. 27:17880-17888
We present a one-step Ugi reaction protocol for the expedient synthesis of photoaffinity probes for live-cell MS-based proteomics. The reaction couples an amine affinity function with commonly used photoreactive groups, and a variety of handle functi
Autor:
Stephen John Atkinson, Patricia F Medeiros, Paola Grandi, Simon Taylor, Chun-wa Chung, James Gray, Robert J. Watson, Ian D. Wall, Alexander L. Satz, Rab K. Prinjha, Francesco Rianjongdee, Alex Preston, Emmanuel Hubert Demont, Gang Yao, Alex Phillipou, Inmaculada Rioja, Cassie Messenger, Laura J. Kaushansky
Publikováno v:
Journal of Medicinal Chemistry. 64:10806-10833
Second-generation bromodomain and extra terminal (BET) inhibitors, which selectively target one of the two bromodomains in the BET proteins, have begun to emerge in the literature. These inhibitors aim to help determine the roles and functions of eac
Autor:
Peter Ernest Soden, Massimo Petretich, Robert J. Watson, Laurie J. Gordon, Chun-wa Chung, Paola Grandi, Alex Phillipou, Paul Bamborough, Emmanuel Hubert Demont, Rab K. Prinjha, Inmaculada Rioja, Thilo Werner, Robert E. Davis, Heather A. Barnett
Publikováno v:
Journal of Medicinal Chemistry. 63:9045-9069
Pan-bromodomain and extra terminal (BET) inhibitors interact equipotently with all eight bromodomains of the BET family of proteins. They have shown profound efficacy in vitro and in vivo in oncology and immunomodulatory models, and a number of them
Autor:
Alex Phillipou, Ryan G. Kruger, Simon Taylor, Chun-wa Chung, Rab K. Prinjha, Laurie J. Gordon, Robert J. Watson, James Gray, Alex Preston, James J. Foley, Cassie Messenger, Anna K. Bassil, Inmaculada Rioja, James Michael Woolven, Xi-Ping Zhang, Francesco Rianjongdee, Paola Grandi, Jeanne J. Matteo, Anastasia Wyce, Ian D. Wall, Paul Bamborough, Darren Jason Mitchell, Lee Andrew Harrison, Michael T. McCabe, Stephen John Atkinson, Jonathan Thomas Seal, Emmanuel Hubert Demont
Publikováno v:
Journal of medicinal chemistry. 64(15)
The profound efficacy of pan-BET inhibitors is well documented, but these epigenetic agents have shown pharmacology-driven toxicity in oncology clinical trials. The opportunity to identify inhibitors with an improved safety profile by selective targe
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
Autor:
Jonathan D Lea, Robert J. Young, Duncan S. Holmes, Christopher P. Tinworth, Jonathan P. Hutchinson, Semra Kitchen, Justyna Wojno-Picon, Leng Nickels, Michelle Pemberton, Hester Sheehan, Justyna Korczynska, Margarete Neu, Jessica L. Schneck, Efstratios Stratikos, Despoina Koumantou, Iain Uings, Ted Cecconie, Alex Phillipou, Emma J. Jones, John Liddle, Paul Rowland
Publikováno v:
Journal of medicinal chemistry. 63(6)
ER aminopeptidase 1 (ERAP1) is an intracellular enzyme that generates antigenic peptides and is an emerging target for cancer immunotherapy and the control of autoimmunity. ERAP1 inhibitors described previously target the active site and are limited