Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Susan Marie Westaway"'
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, Alex Preston, Inma Rioja, Roy Katso, Melanie Leveridge, Chun-wa Chung, Michael David Barker, Laurens Kruidenier, Gerard Joberty, Kevin Lee, Onkar M. P. Singh, Joanna Taylor, Matthew Campbell, Michelle Pemberton, Fiona Brown, Robert Eagle, Carl Haslam, David Matthew Wilson, Neil Stuart Garton, Tracy Jane Shipley, Colin J. Suckling, Philip G. Humphreys, Gerard Drewes, Laurie J. Gordon, Pamela Thomas, Jack A. Brown, Gail A. Seal, Thomas George Christopher Hayhow, Susan Marie Westaway
Publikováno v:
Journal of Medicinal Chemistry. 59:1370-1387
Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1dd41f32203668dbba76c4b0b0fbc2e4
https://doi.org/10.1021/acs.jmedchem.5b01538
https://doi.org/10.1021/acs.jmedchem.5b01538
Autor:
Akane Kawamura, Vassilios Bavetsias, Elisabeth D. Martinez, Olivia W. Rossanese, Susan Marie Westaway, Butrus Atrash, Vicki Gamble, Anthony Tumber, Susanne Müller, C. Bountra, Paul Brennan, Oleg Fedorov, Rab K. Prinjha, Udo Oppermann, Christopher J. Schofield, Gian Filippo Ruda, Stephanie B Hatch, Jack A. Brown, Clarence Yapp, Kathy Tomlin, Rachel M. Lanigan, LeAnne Carmichael, Florence I. Raynaud, Pavel Savitsky, Raquel Carvalho Montenegro, Rosemary Burke, Julian Blagg
Publikováno v:
Epigenetics & Chromatin
Repositório Institucional da Universidade Federal do Ceará (UFC)
Universidade Federal do Ceará (UFC)
instacron:UFC
Repositório Institucional da Universidade Federal do Ceará (UFC)
Universidade Federal do Ceará (UFC)
instacron:UFC
Background Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders. The first KDM inhibitors for KDM1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e858f3994a18641fd21ab8ad7cdfac8f
https://ora.ox.ac.uk/objects/uuid:5c854f9a-6888-478c-85f9-b4a155f8b999
https://ora.ox.ac.uk/objects/uuid:5c854f9a-6888-478c-85f9-b4a155f8b999
Autor:
Laurens Kruidenier, Rebecca Randle, Hawa Diallo, Inma Rioja, Clement Douault, Anne Rueger, Chun-wa Chung, Thomas George Christopher Hayhow, Rab K. Prinjha, Alex Preston, Roy Katso, Matthew Campbell, Michael David Barker, J. Mosley, Kevin Lee, Joanna Taylor, Marcel Muelbaier, Douglas W. Thomson, Gail A. Seal, Jack A. Brown, Susan Marie Westaway, Onkar M. P. Singh, Gerard Joberty, Philip G. Humphreys, Melanie Leveridge, Laurie J. Gordon, Pamela Thomas, Carl Haslam, Fiona Brown, John Liddle, Gerard Drewes, Robert Eagle, Robert J. Sheppard, David Matthew Wilson
Publikováno v:
Journal of medicinal chemistry. 59(4)
Optimization of KDM6B (JMJD3) HTS hit 12 led to the identification of 3-((furan-2-ylmethyl)amino)pyridine-4-carboxylic acid 34 and 3-(((3-methylthiophen-2-yl)methyl)amino)pyridine-4-carboxylic acid 39 that are inhibitors of the KDM4 (JMJD2) family of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::169f1f983c8269e73c78cea4fff0100e
https://pubmed.ncbi.nlm.nih.gov/26771107
https://pubmed.ncbi.nlm.nih.gov/26771107
Autor:
Alison I. Muir, Izzy Boyfield, Kalindi Vaidya, Barry Sidney Orlek, Etienne Fleury, David G. Evans, Jackie S. Scott, Hindy Mok, Victoria J. Bolton, Ward John Gerard, Geoffrey Stemp, Tom D. Heightman, Kim L. Matthews, Kirk Lawless, Gareth J. Sanger, Fiona McKay, Alexander J. Stevens, Emma M. Jarvie, James Matthew Bailey, Susan Marie Westaway, Mervyn Thompson, Jonathan B. Basilla
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6452-6458
Optimisation of a series of benzazepine sulfonamide hit compounds identified from high throughput screening led to the discovery of a new series of tractable, potent motilin receptor agonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2f11cdd038a55294786dd33de3ee625
https://doi.org/10.1016/j.bmcl.2009.09.027
https://doi.org/10.1016/j.bmcl.2009.09.027
Autor:
Jason D. Speake, Cunyu Zhang, Michael J. Bishop, Luz H. Carballo, Susan Marie Westaway, Mike Hu, Aaron S. Goetz, Andrea H. Epperly
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(2)
Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.5
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4cb7920d6348306539054d68f00521d4
https://pubmed.ncbi.nlm.nih.gov/21193310
https://pubmed.ncbi.nlm.nih.gov/21193310
Autor:
Jonathan M. Barford, Victoria J. Bolton, Geoffrey Stemp, Shiyam Mohamed, Stephen Christopher Martin Fell, Christopher N. Johnson, Gareth J. Sanger, David MacPherson, Samantha Louisa Brown, Chermaine Cluff, Darren Jason Mitchell, Sadhia R. Mahmood, Fiona McKay, Beverley Smith, Jon T. Seal, James Myatt, Alison I. Muir, Mervyn Thompson, Kim L. Matthews, Kirk Lawless, Steven J. Stanway, Emma M. Jarvie, Alexander J. Stevens, Susan Marie Westaway
Publikováno v:
Journal of medicinal chemistry. 52(4)
N-(3-Fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine 12 (GSK962040) is a novel small molecule motilin receptor agonist. It possesses excellent activity at the recombinant human motilin receptor and also at the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8857cec1d323c56eea1c718edc45757b
https://pubmed.ncbi.nlm.nih.gov/19191554
https://pubmed.ncbi.nlm.nih.gov/19191554
Autor:
Gareth J. Sanger, Susan Marie Westaway
Publisher Summary The gastrointestinal (GI) tract is central to the process of eating. This organ plays a vital role in promoting the sensation of hunger, while helping other parts of the body to cope with the intake of nutrients ingested during a me
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ad6c8d69fc8bf8931f73ee6e29b79b37
https://doi.org/10.1016/s0079-6468(09)04802-4
https://doi.org/10.1016/s0079-6468(09)04802-4
Autor:
Andrea Colombo, Izzy Boyfield, Christopher N. Johnson, Alessandra Consonni, Emma M. Jarvie, Victoria J. Bolton, Darren Jason Mitchell, Paolo Celestini, Michael A. Briggs, Sharon C Stratton, James Myatt, Geoffrey Stemp, David MacPherson, Alexander J. Stevens, Jon T. Seal, Stefania Gagliardi, Steven J. Stanway, Macdonald Gregor James, Mauro Riccaboni, Kate Lapsley, Susan Marie Westaway, Silvano Ronzoni, Gareth J. Sanger, Tom D. Heightman, Kim L. Matthews, Samantha Louisa Brown, Mervyn Thompson, Elizabeth Conway
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(24)
Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing favourable physicochemical and A
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2cf8a53bdb66c538b47ff91cc8129e4
https://pubmed.ncbi.nlm.nih.gov/19006669
https://pubmed.ncbi.nlm.nih.gov/19006669
Autor:
Silvano Ronzoni, Gareth J. Sanger, Sharon Butler, Emma M. Jarvie, Mauro Riccaboni, Paolo Celestini, Susan Marie Westaway, Alison I. Muir, Fiona McKay, Kalindi Vaidya, Macdonald Gregor James, Ben Powney, Alan Wise, Tom D. Heightman, Elizabeth Conway, Geoffrey Stemp, Kim Winborn, Stefania Gagliardi, David F. Corbett
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(24)
High-throughput screening resulted in the identification of a series of novel motilin receptor agonists with relatively low molecular weights. The series originated from an array of biphenyl derivatives designed to target 7-transmembrane (7-TM) recep
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54ae2959608cf4c54d287d9645a0d7c6
https://pubmed.ncbi.nlm.nih.gov/18980843
https://pubmed.ncbi.nlm.nih.gov/18980843