Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Paul Scott-Stevens"'
Autor:
Han Dai, Robert P. Law, John P. Evans, Gillian F. Watt, Chun-wa Chung, Markus A. Queisser, John D. Harling, Antonia J. Lewis, Marcus Bantscheff, João Osvaldo Rodrigues Nunes, Adam Flinders, Paul Scott-Stevens, Andrew B. Benowitz, Peter Stacey, Christopher J. Tame, Karol Buda, Diana Klimaszewska, Marcel Muelbaier, Nico Zinn
Publikováno v:
Angewandte Chemie. 133:23515-23522
Focal adhesion kinase (FAK) is a key mediator of tumour progression and metastasis. To date, clinical trials of FAK inhibitors have reported disappointing efficacy for oncology indications. We report the design and characterisation of GSK215, a poten
Autor:
Don T. Fisher, Gillian F. Watt, Ian Churcher, Laurie J. Gordon, Andrea D Gonçalves, Alina Mares, Phoebe Dace, Rakesh Nagilla, Bartholomew J. Votta, Ian Edward David Smith, John D. Harling, Pamela A. Haile, Afjal Hussain Miah, Paul Giffen, Paul Scott-Stevens, Aditya R. Thawani, Mark David Rackham, Jane Denyer
Publikováno v:
Journal of Medicinal Chemistry. 64:12978-13003
Receptor-interacting serine/threonine protein kinase 2 (RIPK2) is an important kinase of the innate immune system. Herein, we describe the optimization of a series of RIPK2 PROTACs which recruit members of the inhibitor of apoptosis (IAP) family of E
Publikováno v:
Future Medicinal Chemistry. 14:119-121
Autor:
Mark R. Harpel, Ghotas Evindar, Shenaz Bunally, David G. Washburn, Steve Wilson, Joanne Prendergast, Scott G. Summerfield, Katrina Rivera, Chun-wa Chung, Julien C. Vantourout, Steven R. Skinner, Neil Young, Xiaopeng Bai, Christopher C. Arico-Muendel, Albert Isidro-Llobet, Rakesh Lad, William Traylen, Graham L. Simpson, Josephine Yuen, Letian Kuai, Paul Scott-Stevens, Kim Lambert, Sandeep Pal, Saul Needle, Andrew M. Mason, Michael J Hobbs, Emma V. Edgar, Richard Snell, Lara S. Kallander, Eric X Shi, Lisa M. Shewchuk, Dennis A. Holt, Allan J. B. Watson
Publikováno v:
Bioconjugate Chemistry. 32:279-289
Reducing the required frequence of drug dosing can improve the adherence of patients to chronic treatments. Hence, drugs with longer in vivo half-lives are highly desirable. One of the most promising approaches to extend the in vivo half-life of drug
Autor:
Laurie P Volak, Heide Marika Duevel, Sara Humphreys, David Nettleton, Colin Phipps, Andy Pike, Caroline Rynn, Paul Scott-Stevens, Donglu Zhang, Michael Zientek
Publikováno v:
Drug Metabolism and Disposition. :DMD-AR
Autor:
Jenni Cryan, Don T. Fisher, Michael Reilly, Ian Edward David Smith, Anna Vossenkämper, Gillian F. Watt, Ian Churcher, John D. Harling, Allison M. Beal, Thomas T. MacDonald, Alina Mares, Phoebe Dace, Bartholomew J. Votta, Marcus Bantscheff, Jane Denyer, Paul Scott-Stevens, Afjal Hussain Miah, Andrew B. Benowitz, Aditya R. Thawani, Carol A. Capriotti, Mark David Rackham, Nico Zinn, Pamela A. Haile
Publikováno v:
Communications Biology, Vol 3, Iss 1, Pp 1-13 (2020)
Communications Biology
Communications Biology
Proteolysis-Targeting Chimeras (PROTACs) are heterobifunctional small-molecules that can promote the rapid and selective proteasome-mediated degradation of intracellular proteins through the recruitment of E3 ligase complexes to non-native protein su
Autor:
Paul Scott-Stevens, Qin Donghui, Allen Oliff, Andrew N. Hobbs, Yoshiaki Washio, Josh Cottom, Jennifer A. Borthwick, Julia Coggins, Robert J. Young, Biju Mangatt, Jordi Munoz-Muriedas, Paris Ward, Siegfried B. Christensen, Helen L. Evans, Jingsong Yang, Nino Campobasso, Graham L. Simpson, Julien Chabanet, Xuan Hong, Sophie M. Bertrand, Susan Chen, Helen C. Dawson
Publikováno v:
Journal of Medicinal Chemistry. 62:2154-2171
Abelson kinase (c-Abl) is a ubiquitously expressed, nonreceptor tyrosine kinase which plays a key role in cell differentiation and survival. It was hypothesized that transient activation of c-Abl kinase via displacement of the N-terminal autoinhibito
Publikováno v:
Protein Degradation with New Chemical Modalities ISBN: 9781788016865
Many examples of PROTACs possessing in vivo efficacy in pre-clinical studies have now been disclosed. While building pharmacokinetic (PK)/pharmacodynamic (PD) relationships is recognized as a key activity in small-molecule drug discovery to support t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::20bd3803ad89dfc67765bf21eb34f214
https://doi.org/10.1039/9781839160691-00075
https://doi.org/10.1039/9781839160691-00075
Autor:
Angela Bridges, Sandrine Jayne, Jennifer Schofield, Ana Sousa Manso, Duncan S. Holmes, Xi-Ping Zhang, Larissa Lezina, Michael T. McCabe, Mark James Bamford, Anastasia Wyce, David Jonathan Hirst, Máire A. Convery, Tom Slocombe, Andrew C. Pearce, Don O. Somers, Simon D. Wagner, Paul Scott-Stevens, Ann Louise Walker, Jonathan P. Hutchinson, Constantinos Demetriou, Cassie Messenger, Melissa C. Musso, Sian Evans, Ruth C. Barber, Joanne Morley, Thomas Gobbetti
Publikováno v:
The Journal of Biological Chemistry
B-cell lymphoma 6 (BCL6) is a zinc finger transcriptional repressor possessing a BTB–POZ (BR-C, ttk, and bab for BTB; pox virus and zinc finger for POZ) domain, which is required for homodimerization and association with corepressors. BCL6 has mult
Publikováno v:
Drug discovery today. Technologies. 31
Proteolysis Targeting Chimeras (PROTACs) are a rapidly expanding new therapeutic modality inducing selective protein degradation and offering the potential of a differentiated pharmacological profile across multiple therapeutic areas. As the repertoi