Zobrazeno 1 - 10
of 74
pro vyhledávání: '"Mark E Bunnage"'
Autor:
Susanne Müller, Suzanne Ackloo, Cheryl H Arrowsmith, Marcus Bauser, Jeremy L Baryza, Julian Blagg, Jark Böttcher, Chas Bountra, Peter J Brown, Mark E Bunnage, Adrian J Carter, David Damerell, Volker Dötsch, David H Drewry, Aled M Edwards, James Edwards, Jon M Elkins, Christian Fischer, Stephen V Frye, Andreas Gollner, Charles E Grimshaw, Adriaan IJzerman, Thomas Hanke, Ingo V Hartung, Steve Hitchcock, Trevor Howe, Terry V Hughes, Stefan Laufer, Volkhart MJ Li, Spiros Liras, Brian D Marsden, Hisanori Matsui, John Mathias, Ronan C O'Hagan, Dafydd R Owen, Vineet Pande, Daniel Rauh, Saul H Rosenberg, Bryan L Roth, Natalie S Schneider, Cora Scholten, Kumar Singh Saikatendu, Anton Simeonov, Masayuki Takizawa, Chris Tse, Paul R Thompson, Daniel K Treiber, Amélia YI Viana, Carrow I Wells, Timothy M Willson, William J Zuercher, Stefan Knapp, Anke Mueller-Fahrnow
Publikováno v:
eLife, Vol 7 (2018)
Potent, selective and broadly characterized small molecule modulators of protein function (chemical probes) are powerful research reagents. The pharmaceutical industry has generated many high-quality chemical probes and several of these have been mad
Externí odkaz:
https://doaj.org/article/959198e7fd31440495c0d4c7cf3c5c06
Autor:
Ogo Egbuna, Brandon Zimmerman, George Manos, Anne Fortier, Madalina C. Chirieac, Leslie A. Dakin, David J. Friedman, Kate Bramham, Kirk Campbell, Bertrand Knebelmann, Laura Barisoni, Ronald J. Falk, Debbie S. Gipson, Michael S. Lipkowitz, Akinlolu Ojo, Mark E. Bunnage, Martin R. Pollak, David Altshuler, Glenn M. Chertow
Publikováno v:
New England Journal of Medicine. 388:969-979
Autor:
Brian Juba, Betsy Pierce, Steve Kortum, Armon Sharei, Jing Li, Erik C. Hett, Jean-Baptiste Telliez, Bu Wang, Mark E. Bunnage, Lee R. Roberts, Strohbach Joseph Walter, Michael Pacheco, Atli Thorarensen, Lyn H. Jones, Michael L. Vazquez, Jonathan B. Gilbert
Publikováno v:
ACS Chemical Biology. 12:2970-2974
Biochemical screening is a major source of lead generation for novel targets. However, during the process of small molecule lead optimization, compounds with excellent biochemical activity may show poor cellular potency, making structure-activity rel
Autor:
Mark E. Bunnage, Lyn H. Jones
Publikováno v:
Nature Reviews Drug Discovery. 16:285-296
The allure of phenotypic screening, combined with the industry preference for target-based approaches, has prompted the development of innovative chemical biology technologies that facilitate the identification of new therapeutic targets for accelera
Autor:
Abdellah Allali-Hassani, Marius Sudol, Amber L. Couzens, Menno J. Oudhoff, Hong Zeng, Peter Brown, Masoud Vedadi, Mitchell J.S. Braam, Aiping Dong, Anne-Claude Gingras, Brian S. Gerstenberger, Fengling Li, Richard Marcellus, Spencer A. Freeman, Fabio M.V. Rossi, Dafydd R. Owen, Rima Al-awar, Lee R. Roberts, Tatlock John H, Hong Wu, Paul V. Fish, Steven Kennedy, Ahmed Aman, Colby Zaph, Guillermo A. Senisterra, Matthieu Schapira, Jean-Philippe Lambert, Ekaterina Kuznetsova, Cheryl H. Arrowsmith, Mark E. Bunnage, Rachel L. Grimley, Dalia Barsyte-Lovejoy, Caroline L. Benn
Publikováno v:
Proceedings of the National Academy of Sciences. 111:12853-12858
SET domain containing (lysine methyltransferase) 7 (SETD7) is implicated in multiple signaling and disease related pathways with a broad diversity of reported substrates. Here, we report the discovery of (R)-PFI-2-a first-in-class, potent (Ki (app) =
Autor:
Li Xing, Jane M. Withka, Guoyun Bai, Mark E. Bunnage, Bruce Allen Lefker, Leslie Anthony Dakin, Sheng Tan, Shenping Liu, Mary Ellen Banker, Parag Sahasrabudhe, Ariamala Gopalsamy, Atli Thorarensen, Hua Xu, Jennifer A. Young, Joerg Bussenius, Boris A. Chrunyk, Jinshan M. Chen, Kieran F. Geoghegan, Stephen W. Wright, Suman Shanker, Jeremy T. Starr, Paul Balbo, Xiayang Qiu, Zuojun Guo, Wei Li, Lyn H. Jones, Fabien Vincent, Lise R. Hoth
Publikováno v:
Scientific Reports
Interleukin-17A (IL-17A) is a principal driver of multiple inflammatory and immune disorders. Antibodies that neutralize IL-17A or its receptor (IL-17RA) deliver efficacy in autoimmune diseases, but no small-molecule IL-17A antagonists have yet progr
Autor:
Stephen G. Davies, Jonathan M. Withey, Andrew D. Smith, Paul M. Roberts, Richard M. Parkin, Mark E. Bunnage
High levels of stereocontrol are observed in the conjugate addition of lithium dibenzylamide to tert-butyl (RS)-3-alkylcyclopentene-1-carboxylates (alkyl = Et, Bn), with addition occurring exclusively anti- to the 3-alkyl substituent. Treatment of a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68e205f5c416d476253c4ece8fa03e2e
https://ora.ox.ac.uk/objects/uuid:c605d986-15e9-4a3d-a054-6cec12d30bb4
https://ora.ox.ac.uk/objects/uuid:c605d986-15e9-4a3d-a054-6cec12d30bb4
Autor:
Paul Brennan, Martin Philpott, Dafydd R. Owen, Juerg Schwaller, Panagis Filippakopoulos, Phillippe Taniere, David Da Costa, Tatjana Stankovic, Stefan Knapp, Brendan O'Sullivan, Sarah Picaud, Paul V. Fish, Angeliki Thanasopoulou, Susanne Müller, Mark E. Bunnage, James E. Bradner, Oleg Fedorov
Publikováno v:
CANCER RESEARCH
Bromo and extra terminal (BET) proteins (BRD2, BRD3, BRD4, and BRDT) are transcriptional regulators required for efficient expression of several growth promoting and antiapoptotic genes as well as for cell-cycle progression. BET proteins are recruite
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb616d902f55b63b0ffc1a995d0511d1
https://doi.org/10.1158/0008-5472.can-12-3292
https://doi.org/10.1158/0008-5472.can-12-3292
Allophenylnorstatine [APNS; (2 S ,3 S )-3-amino-2-hydroxy-4-phenylbutanoic acid], a novel amino acid found in the kynostatin class of HIV-1 protease inhibitors, has been prepared in 39% overall yield via a tandem conjugate addition-electrophilic hydr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e638b3f846821487e0ddbde78e3b9b14
https://ora.ox.ac.uk/objects/uuid:5a2411b3-31bb-4704-8fbf-408d16ddc9e6
https://ora.ox.ac.uk/objects/uuid:5a2411b3-31bb-4704-8fbf-408d16ddc9e6
Autor:
Charlotte Alice Louise Lane, David Ellis, Rachel Russel, Mathias John Paul, Lesa Watson, James R. Gosset, David James Rawson, Maw Graham Nigel, Street Stephen Derek Albert, Martin Corless, Mark E. Bunnage, Stephen Martin Denton, Kevin Beaumont, Laura Foster, Susan Cole, Stephen Ballard, Marion Floc’h, Jenny Price, William A. Million, Barber Christopher Gordon, Cedric Poinsard, David Leahy, Laura Barker, Frances Holmwood
Publikováno v:
Bioorganic & Medicinal Chemistry. 20:498-509
This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and go