Zobrazeno 1 - 10
of 26
pro vyhledávání: '"A K, Bassil"'
Autor:
Rebecca C. Furze, Judit Molnar, Nigel J. Parr, Faiz Ahmad, Yvette Henry, David Howe, Rajendra Singh, Martin Toal, Anna K. Bassil, Sharon G. Bernard, Robert P. Davis, Adele Gibson, N. Claire Maller, Catriona Sharp, David F. Tough, Rab K. Prinjha, Huw D. Lewis
Publikováno v:
British Journal of Clinical Pharmacology. 88:5238-5256
To improve the tolerability and therapeutic application of histone deacetylase inhibitors (HDACi), by application of an esterase-sensitive motif (ESM), to target pharmacological activity directly to mononuclear myeloid cells expressing the processing
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b986a405b103538adcd6ab638dd0581c
https://doi.org/10.1111/bcp.15428
https://doi.org/10.1111/bcp.15428
Autor:
Antonia J. Lewis, Anna K. Bassil, Lee Andrew Harrison, Darren Jason Mitchell, Dave Lugo, Robert J. Watson, James Gray, Rab K. Prinjha, Alex Preston, Anne-Marie Michon, Ian D. Wall, Simon Taylor, Chun-wa Chung, Jonathan Thomas Seal, Stephen John Atkinson, Etienne Levernier, Paola Grandi, Emmanuel Hubert Demont, Inmaculada Rioja, James Michael Woolven, Cassie Messenger
Publikováno v:
Journal of Medicinal Chemistry. 64:10742-10771
Domain-specific BET bromodomain ligands represent an attractive target for drug discovery with the potential to unlock the therapeutic benefits of antagonizing these proteins without eliciting the toxicological aspects seen with pan-BET inhibitors. W
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d61563a5d35b9e5dc33735f58cc99285
https://doi.org/10.1021/acs.jmedchem.0c02155
https://doi.org/10.1021/acs.jmedchem.0c02155
Autor:
Emmanuel Hubert Demont, Jonathan Thomas Seal, Stephen John Atkinson, Anna K. Bassil, Paola Grandi, Robert J. Watson, Thomas George Christopher Hayhow, James Gray, Chun-wa Chung, Aylott Helen Elizabeth, Alexander N Phillipou, Darren Jason Mitchell, James Michael Woolven, Inmaculada Rioja, Laurie J. Gordon, Francesco Rianjongdee, Paul Bamborough, Ian D. Wall, Rab K. Prinjha, Alex Preston, Lee Andrew Harrison, Cassie Messenger
Publikováno v:
Journal of Medicinal Chemistry. 64:3249-3281
A number of reports have recently been published describing the discovery and optimization of bromo and extraterminal inhibitors which are selective for the second bromodomain (BD2); these include our own work toward GSK046 (3) and GSK620 (5). This p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::654a0dddd40ac85f0e3f79a9cc1d806c
https://doi.org/10.1021/acs.jmedchem.0c02156
https://doi.org/10.1021/acs.jmedchem.0c02156
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4e26e07fd3767cf6b96980599351c38
https://pubmed.ncbi.nlm.nih.gov/34255512
https://pubmed.ncbi.nlm.nih.gov/34255512
Autor:
Peter Ernest Soden, Emma J. Roberts, Danette L. Daniels, Chun-wa Chung, Stephen John Atkinson, Paul Bamborough, Anne Marie Michon, Johanna Vappiani, Andrea C. Haynes, Massimo Petretich, Marcus Bantscheff, Miriam M. Yeung, Matthew J Bell, Sarah-Jane Dawson, Paola Grandi, Dane Vassiliadis, Simon Taylor, James Gray, Omer Gilan, Kathy Knezevic, Marjeta Urh, Matthew J Lindon, Marian L. Burr, Rab K. Prinjha, Alex Preston, Inmaculada Rioja, Mark A. Dawson, Gerard Drewes, Thilo Werner, Christopher Roland Wellaway, Emmanuel Hubert Demont, Anna K. Bassil, Nicola Harker, Thomas Gobbetti, Enid Y.N. Lam, David F. Tough, Vinod Kumar
Publikováno v:
Science
Bromodomain inhibitors revisited Bromodomain and extraterminal domain (BET) proteins contribute to the pathogenesis of cancer and immune diseases through their effects on transcriptional regulation. BET proteins contain two nearly identical bromodoma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58f230e3011891f1a84ffe803aee2fab
https://europepmc.org/articles/PMC7610820/
https://europepmc.org/articles/PMC7610820/
Autor:
Marc-Werner Dobenecker, Rab K. Prinjha, Anna K. Bassil, Alexander Tarakhovsky, Michael T. McCabe, Richard Gregory, Inmaculada Rioja, Joon Seok Park, Steven D. Knight, Jonas Marcello
Publikováno v:
The Journal of Experimental Medicine
PRC2 is a known chromatin regulator. Here the authors show novel cytosolic components of PRC2 and that PRC2 inactivation results in attenuation of MAPK/Erk signaling and impaired T cell activation. Systemic PRC2 inhibition in vivo cures the autoimmun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::097d923dc52893e51f5de6bd67c83492
https://doi.org/10.1084/jem.20170084
https://doi.org/10.1084/jem.20170084
Autor:
G Bruton, C M Taylor, Anna K. Bassil, Scott G. Summerfield, Kevin Lee, Victoria J. Bolton, Gareth J. Sanger, Wendy J. Winchester, Jason D. Brown, Leanne Cutler, Karen M. Gray
Publikováno v:
British Journal of Pharmacology. 158:252-258
Background: 5-HT2B receptors are localized within the myenteric nervous system, but their functions on motor/sensory neurons are unclear. To explore the role of these receptors, we further characterized the 5-HT2B receptor antagonist RS-127445 and st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8182932bc634723850fcae0abc3b25ea
https://doi.org/10.1111/j.1476-5381.2009.00155.x
https://doi.org/10.1111/j.1476-5381.2009.00155.x
Publikováno v:
Pharmacological Research. 57:339-343
The antidepressant tianeptine is associated with a small but significant incidence of gastrointestinal (GI) side effects, including nausea and constipation. Since the site of action of tianeptine is not clear, we looked for an ability of this drug to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ba1b401dc2669506ed88d2a853cd695
https://doi.org/10.1016/j.phrs.2008.03.006
https://doi.org/10.1016/j.phrs.2008.03.006
Autor:
Anna K. Bassil, R J McArthur-Wilson, E. Z. H. Sung, Kevin Lee, Emma M. Jarvie, Ramkumar Thangiah, Richard A. Borman, Gareth J. Sanger
Publikováno v:
British Journal of Pharmacology. 154:126-135
Background and purpose: Lubiprostone (Amitiza), a possible ClC-2 channel opener derived from prostaglandin E1 and indicated for the treatment of constipation, increases chloride ion transport and fluid secretion into the intestinal lumen. As lubipros
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::39305b9ab152d79a4b879de1184b7bf1
https://doi.org/10.1038/bjp.2008.84
https://doi.org/10.1038/bjp.2008.84
Autor:
Olutunde Lalude, Karen M. Gray, Ramkumar Thangiah, Anna K. Bassil, Selim Cellek, Alan Wheeldon, Gareth J. Sanger, Shanmugam Vivekanandan, Jennifer L. Stretton, Michael Schemann, Colin A. Campbell, Kevin Lee, Wendy J. Winchester
Publikováno v:
Gastroenterology. 133:175-183
Although the beta(3)-adrenoceptor (AR) has been suggested to be involved in regulation of gut motility and visceral algesia, the precise mechanisms have been unknown. beta(3)-AR has been postulated to have a nonneuronal expression, being initially ch
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4da732d75939a6b3d1664e01134cac42
https://doi.org/10.1053/j.gastro.2007.05.009
https://doi.org/10.1053/j.gastro.2007.05.009