Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Robert J. Sheppard"'
Autor:
Michael J. Waring, Iwan J. P. de Esch, Zhiyong Wang, Sebastiaan Kuhne, Maikel Wijtmans, Reggie Bosma, Albert J. Kooistra, Nick Bushby, Rob Leurs, Robert J. Sheppard, Henry F. Vischer, Jelle van den Bor, Chris de Graaf
Publikováno v:
Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 62(14), 6630-6644. American Chemical Society
Bosma, R, Wang, Z, Kooistra, A J, Bushby, N, Kuhne, S, Van Den Bor, J, Waring, M J, De Graaf, C, De Esch, I J, Vischer, H F, Sheppard, R J, Wijtmans, M & Leurs, R 2019, ' Route to prolonged residence time at the histamine H 1 receptor : Growing from desloratadine to rupatadine ', Journal of Medicinal Chemistry, vol. 62, no. 14, pp. 6630-6644 . https://doi.org/10.1021/acs.jmedchem.9b00447
Journal of Medicinal Chemistry, 62(14), 6630-6644. American Chemical Society
Bosma, R, Wang, Z, Kooistra, A J, Bushby, N, Kuhne, S, Van Den Bor, J, Waring, M J, De Graaf, C, De Esch, I J, Vischer, H F, Sheppard, R J, Wijtmans, M & Leurs, R 2019, ' Route to prolonged residence time at the histamine H 1 receptor : Growing from desloratadine to rupatadine ', Journal of Medicinal Chemistry, vol. 62, no. 14, pp. 6630-6644 . https://doi.org/10.1021/acs.jmedchem.9b00447
Drug-target binding kinetics are an important predictor of in vivo drug efficacy, yet the relationship between ligand structures and their binding kinetics is often poorly understood. We show that both rupatadine (1) and desloratadine (2) have a long
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c829e91f8290d6334a1a657c0200b0f
https://doi.org/10.1021/acs.jmedchem.9b00447
https://doi.org/10.1021/acs.jmedchem.9b00447
Autor:
Catherine Bardelle, James M. Smith, Nidhal Selmi, Alice Lanne, Robert J. Sheppard, Daniel Hillebrand O'donovan, Jon Read, Geoffrey A. Holdgate
Publikováno v:
Drug discovery today. 27(4)
Dysregulation of the epigenome is associated with the onset and progression of several diseases, including cancer, autoimmune, cardiovascular, and neurological disorders. Members from the three families of epigenetic proteins (readers, writers, and e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1767602e5f23f8762840780554ff6b00
https://pubmed.ncbi.nlm.nih.gov/34728375
https://pubmed.ncbi.nlm.nih.gov/34728375
Autor:
Chun-wa Chung, Rab K. Prinjha, Simon C. C. Lucas, Nicholas C. O. Tomkinson, Alexander N Phillipou, Stephen John Atkinson, Darren Jason Mitchell, Paul Bamborough, Robert J. Sheppard, Emmanuel Hubert Demont, Robert J. Watson, Laurie J. Gordon, Heather A. Barnett
Most bromodomain inhibitors mimic the interactions of the natural acetylated lysine (KAc) histone substrate through key interactions with conserved asparagine and tyrosine residues within the binding pocket. Herein we report the optimization of a ser
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5846b0ef827565f0ccfd4008efb5659
https://strathprints.strath.ac.uk/73265/1/Lucas_etal_JMC_2020_The_optimisation_of_potent_ATAD2_and_CECR2_Bromodomain_inhibitors_with_an_atypical_binding_mode.pdf
https://strathprints.strath.ac.uk/73265/1/Lucas_etal_JMC_2020_The_optimisation_of_potent_ATAD2_and_CECR2_Bromodomain_inhibitors_with_an_atypical_binding_mode.pdf
Autor:
Stephen J. Hill, Leigh A. Stoddart, Stephen J. Briddon, Robert J. Sheppard, Monica Bouzo-Lorenzo, Amaury Ernesto Fernandez-Montalvan, Henry F. Vischer, Loretta Inkoom, Nick Bushby, Michael J. Waring, Victoria Georgi, Reggie Bosma, Rob Leurs
Publikováno v:
Scientific Reports, 9(1):7906. Nature Publishing Group
Bosma, R, Stoddart, L A, Georgi, V, Bouzo-Lorenzo, M, Bushby, N, Inkoom, L, Waring, M J, Briddon, S J, Vischer, H F, Sheppard, R J, Fernández-Montalván, A, Hill, S J & Leurs, R 2019, ' Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor ', Scientific Reports, vol. 9, no. 1, 7906 . https://doi.org/10.1038/s41598-019-44025-5
Scientific Reports, Vol 9, Iss 1, Pp 1-13 (2019)
Scientific Reports
Bosma, R, Stoddart, L A, Georgi, V, Bouzo-Lorenzo, M, Bushby, N, Inkoom, L, Waring, M J, Briddon, S J, Vischer, H F, Sheppard, R J, Fernández-Montalván, A, Hill, S J & Leurs, R 2019, ' Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor ', Scientific Reports, vol. 9, no. 1, 7906 . https://doi.org/10.1038/s41598-019-44025-5
Scientific Reports, Vol 9, Iss 1, Pp 1-13 (2019)
Scientific Reports
Drug-target binding kinetics are suggested to be important parameters for the prediction of in vivo drug-efficacy. For G protein-coupled receptors (GPCRs), the binding kinetics of ligands are typically determined using association binding experiments
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18bb0560032e7652def15ba7a60b5227
https://doi.org/10.1038/s41598-019-44025-5
https://doi.org/10.1038/s41598-019-44025-5
Autor:
Andrew D. Roberts, Peter Francis, Paola Grandi, Emma J. Jones, David P. Dixon, Robert J. Watson, Christina Rau, Peter Pogány, Angela Bridges, Chun-wa Chung, Darren Jason Mitchell, Rab K. Prinjha, Peter D. Craggs, Kelly Locke, Emmanuel Hubert Demont, Anne-Marie Michon, Bhumika Karamshi, Rebecca C. Furze, Paul Bamborough, Robert J. Sheppard, Simon C. C. Lucas, Ana Maria Roa
Publikováno v:
Journal of medicinal chemistry. 62(16)
The bromodomain of ATAD2 has proved to be one of the least-tractable proteins within this target class. Here, we describe the discovery of a new class of inhibitors by high-throughput screening and show how the difficulties encountered in establishin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f80874ffd274bf81cab3a201c3f2f1c
https://pubmed.ncbi.nlm.nih.gov/31398032
https://pubmed.ncbi.nlm.nih.gov/31398032
Autor:
Clement Douault, Tony Kouzarides, Robert J. Sheppard, Hawa Diallo, Paola Grandi, Samuel Robson, Chun-wa Chung, Ka Hing Che, Rab K. Prinjha, Richard J. Upton, Darren Jason Mitchell, Rebecca C. Furze, Emmanuel Hubert Demont, Andrew J. Bannister, Anne-Marie Michon, Robert J. Watson, Christina Rau, Paul Bamborough
Publikováno v:
Angew Chem Int Ed Engl
ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF(2) as a sulfone
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4422b24c26e10a43ba070267a1d8114d
https://doi.org/10.1002/anie.201603928
https://doi.org/10.1002/anie.201603928
Autor:
Laurie J. Gordon, David J. Fallon, Heather A. Barnett, Chun-wa Chung, Darren Jason Mitchell, Emma J. Jones, Robert J. Watson, Rab K. Prinjha, Armelle Le Gall, Isabelle Becher, Paola Grandi, Emmanuel Hubert Demont, Edward Hooper-Greenhill, Peter D. Craggs, Mark J. Bird, Allan J. B. Watson, Hawa Diallo, Robert P. Law, Robert J. Sheppard, Anne-Marie Michon, Dave Lugo, Paul Bamborough, Clare I. Hobbs
Publikováno v:
ACS Medicinal Chemistry Letters. 7:552-557
The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d0e6b381fa59b5ceac0bfd9cdc17c45
https://doi.org/10.1021/acsmedchemlett.6b00092
https://doi.org/10.1021/acsmedchemlett.6b00092
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, Emmanuel Hubert Demont, Rebecca C. Furze, Chun-wa Chung, Robert J. Sheppard, Robert J. Watson, Heather A. Barnett, Christina Rau, Paul Bamborough, Anne-Marie Michon, Thilo Werner, Paola Grandi, Darren Jason Mitchell
Publikováno v:
Journal of medicinal chemistry. 61(18)
ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of its class. In our recent disclosure of the first chemical probe against this bromodomain, GSK8814 (6), we described the use of a conformationall
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1c3643b91595cb6858e3190a4228dab
https://pubmed.ncbi.nlm.nih.gov/30226378
https://pubmed.ncbi.nlm.nih.gov/30226378
Autor:
Emma J. Jones, David P. Dixon, Robert J. Watson, Chun-wa Chung, Anne-Marie Michon, Clement Douault, Emmanuel Hubert Demont, Paul Bamborough, Hawa Diallo, Thilo Werner, Christina Rau, Paola Grandi, Robert J. Sheppard, Rab K. Prinjha, Rebecca C. Furze, Bhumika Karamshi, Darren Jason Mitchell, Heather A. Barnett
Publikováno v:
Journal of Medicinal Chemistry. 58:6151-6178
ATAD2 is a bromodomain-containing protein whose overexpression is linked to poor outcomes in a number of different cancer types. To date, no potent and selective inhibitors of the bromodomain have been reported. This article describes the structure-b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e851c14806280d0cfece0632536d172
https://doi.org/10.1021/acs.jmedchem.5b00773
https://doi.org/10.1021/acs.jmedchem.5b00773