Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Gordon, Saxty"'
Autor:
Stacey M. Southall, Joydeep Banerjee, Jason Brown, Kristina Butkovic, Andrew D. Cansfield, Julie E. Cansfield, Miles S. Congreve, Gabriella Cseke, Francesca Deflorian, Martina Petrovic Hunjadi, Antun Hutinec, Trinadh Kumar Inturi, Renata Rupcic, Gordon Saxty, Stephen P. Watson
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1776-1782
The diastereomeric macrocyclic calcitonin generelated peptide (CGRP) antagonists HTL0029881 (3) and HTL0029882 (4), in which the stereochemistry of a spiro center is reversed, surprisingly demonstrate comparable potency. X-ray crystallographic charac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6056f84865bf327ec61e26bf41ed7b3
https://doi.org/10.1021/acsmedchemlett.2c00400
https://doi.org/10.1021/acsmedchemlett.2c00400
Autor:
Matthew V. Lorenzi, Sylvie Laquerre, Patrick Angibaud, Christopher Moy, Jayaprakash D. Karkera, Suso J. Platero, Jennifer Yang, Liang Xie, Na Cheng, David R. Newell, Neil T. Thompson, George Ward, Ron Gilissen, Christopher W. Murray, Martin Page, Gordon Saxty, Matthew Squires, David C. Rees, Eddy Freyne, Peter King, Kelly Van De Ven, Caroline Paulussen, Tinne Verhulst, Desiree De Lange, Jorge Vialard, Laurence Mevellec, Eleonora Jovcheva, Timothy P.S. Perera
A) Structure of JNJ-42541707, a structurally related compound to JNJ-42756493. B) 72h growth inhibition (IC50) of JNJ-42541707 against 236 cancer cell lines from multiple origins color coded based on FGFR1,2,4 mRNA overexpression and FGFR WT.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::014876daf0ea3141cec8e46d4cd3afe8
https://doi.org/10.1158/1535-7163.22503741
https://doi.org/10.1158/1535-7163.22503741
Autor:
Matthew V. Lorenzi, Sylvie Laquerre, Patrick Angibaud, Christopher Moy, Jayaprakash D. Karkera, Suso J. Platero, Jennifer Yang, Liang Xie, Na Cheng, David R. Newell, Neil T. Thompson, George Ward, Ron Gilissen, Christopher W. Murray, Martin Page, Gordon Saxty, Matthew Squires, David C. Rees, Eddy Freyne, Peter King, Kelly Van De Ven, Caroline Paulussen, Tinne Verhulst, Desiree De Lange, Jorge Vialard, Laurence Mevellec, Eleonora Jovcheva, Timothy P.S. Perera
In vitro kinase inhibition by DiscoverX KinomeScan assay. For details see (19)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::707b5abacc5ec387fe47990836d03d73
https://doi.org/10.1158/1535-7163.22503738
https://doi.org/10.1158/1535-7163.22503738
Autor:
Matthew V. Lorenzi, Sylvie Laquerre, Patrick Angibaud, Christopher Moy, Jayaprakash D. Karkera, Suso J. Platero, Jennifer Yang, Liang Xie, Na Cheng, David R. Newell, Neil T. Thompson, George Ward, Ron Gilissen, Christopher W. Murray, Martin Page, Gordon Saxty, Matthew Squires, David C. Rees, Eddy Freyne, Peter King, Kelly Van De Ven, Caroline Paulussen, Tinne Verhulst, Desiree De Lange, Jorge Vialard, Laurence Mevellec, Eleonora Jovcheva, Timothy P.S. Perera
Inhibitory activity of Brivanib and JNJ-42756943 in kinase (top) and BaF3 kinase dependent proliferation (bottom) assays and ratio of FGFRs/VEGFR2 activities.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60399ae060b7382e0f81605f3d51fc78
https://doi.org/10.1158/1535-7163.22503735
https://doi.org/10.1158/1535-7163.22503735
Autor:
Matthew V. Lorenzi, Sylvie Laquerre, Patrick Angibaud, Christopher Moy, Jayaprakash D. Karkera, Suso J. Platero, Jennifer Yang, Liang Xie, Na Cheng, David R. Newell, Neil T. Thompson, George Ward, Ron Gilissen, Christopher W. Murray, Martin Page, Gordon Saxty, Matthew Squires, David C. Rees, Eddy Freyne, Peter King, Kelly Van De Ven, Caroline Paulussen, Tinne Verhulst, Desiree De Lange, Jorge Vialard, Laurence Mevellec, Eleonora Jovcheva, Timothy P.S. Perera
JNJ-42756493 anti-proliferative activity against cancer cells lines from multiple origins.. Detailed data supporting Figure 2.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59bca756040d98715cf3d679230a312d
https://doi.org/10.1158/1535-7163.22503732.v1
https://doi.org/10.1158/1535-7163.22503732.v1
Autor:
Andrew D. Cansfield, Mark A. Ator, Joydeep Banerjee, Michael Bestwick, Andrea Bortolato, Giles A. Brown, Jason Brown, Kristina Butkovic, Julie E. Cansfield, John A. Christopher, Miles Congreve, Gabriella Cseke, Francesca Deflorian, Benjamin Dugan, Martina Petrovic Hunjadi, Antun Hutinec, Trinadh Kumar Inturi, Goran Landek, Jonathan Mason, Alistair O’Brien, Gregory R. Ott, Renata Rupcic, Gordon Saxty, Stacey M. Southall, Rahela Zadravec, Stephen P. Watson
Publikováno v:
ACS Chemical Neuroscience. 13:751-765
A series of macrocyclic calcitonin gene-related peptide (CGRP) receptor antagonists identified using structure-based design principles, exemplified by HTL0028016 (1) and HTL0028125 (2), is described. Structural characterization by X-ray crystallograp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c446db762c3a729f140cd365a9977f1b
https://doi.org/10.1021/acschemneuro.1c00696
https://doi.org/10.1021/acschemneuro.1c00696
Autor:
Ivaylo Jivkov Elenkov, Simon Feldbaek Nielsen, Kristina Butković, Sanja Koštrun, Dijana Pesic, Dack Kevin Neil, Tine Skak-Nielsen, Dinko Žiher, Martin Stahlhut, Adriana Petrinić Grba, Vlatka Bencetić Mihaljević, Ana Čikoš, Samra Kapić, Andrea Fajdetić, Renata Rupčić, Gordon Saxty, Maja Lambert, Jasna Padovan, Ivana Ozimec Landek, Karmen Brajša, Dubravko Jelić, Haakan Bladh, Ana Grgičević
Publikováno v:
Journal of Medicinal Chemistry. 64:8354-8383
Interleukin 17 (IL-17) cytokines promote inflammatory pathophysiology in many autoimmune diseases, including psoriasis, multiple sclerosis, rheumatoid arthritis, and inflammatory bowel disease. Such broad involvement of IL-17 in various autoimmune di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a05f28315da0be7107038b135d157e95
https://doi.org/10.1021/acs.jmedchem.1c00327
https://doi.org/10.1021/acs.jmedchem.1c00327
Autor:
Helen F. Sneddon, Rodolfo Cadilla, Young Do, Jeffrey Guss, Gordon Saxty, Paresh I. Masuria, Caterina Musetti, J. Darren Stuart, Beth Pietrak, Daniela Ennulat, Andrew G. King, Barry G. Shearer, Nicholas J. Kramer, Peckham Gregory, Chuck Poole, Alan R. Rendina, Daniel J. Price, H. Fritz Kramer, Tiahshun Xu, Girish Sati, Stephen A. Thomson, Patricia A. Elkins, Jason A. Holt, Alan V. McDougal, Joseph W. Wilson, Susan B. Laffan, Michael R. Jeune, Jan Klapwijk, Dean N. Thomas, Mark Youngman, Paris Ward, Paul N. Mortenson, Lisa M. Shewchuk, Eugene L. Stewart, David N. Deaton
Publikováno v:
Bioorganicmedicinal chemistry. 28(23)
GlaxoSmithKline and Astex Pharmaceuticals recently disclosed the discovery of the potent H-PGDS inhibitor GSK2894631A 1a (IC50 = 9.9 nM) as part of a fragment-based drug discovery collaboration with Astex Pharmaceuticals. This molecule exhibited good
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0464fe491c8ae02c9501daac98d3f990
https://pubmed.ncbi.nlm.nih.gov/33059303
https://pubmed.ncbi.nlm.nih.gov/33059303
Autor:
Gianni Chessari, Ildiko Maria Buck, Edward J. Lewis, Elisabetta Chiarparin, Jong Sook Ahn, Gordon Saxty, Anna Hopkins, Nicola E. Wilsher, Michael Reader, George Ward, Torren M. Peakman, Steven Howard, Pamela A. Williams, Tomoko Smyth, Christopher N. Johnson, Neil T. Thompson, Vanessa Martins, Joanne M. Munck, Alessia Millemaggi, James Edward Harvey Day, Lee William Page, Sharna J. Rich
Publikováno v:
Journal of Medicinal Chemistry. 61:7314-7329
Inhibitor of apoptosis proteins (IAPs) are promising anticancer targets, given their roles in the evasion of apoptosis. Several peptidomimetic IAP antagonists, with inherent selectivity for cellular IAP (cIAP) over X-linked IAP (XIAP), have been test
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8886a2b897d2049d145784a903935471
https://doi.org/10.1021/acs.jmedchem.8b00900
https://doi.org/10.1021/acs.jmedchem.8b00900
Autor:
Young Do, Lisa A. Orband-Miller, Anthony Shillings, Joelle Le, Caterina Musetti, Gordon Saxty, Beth Pietrak, Simon Teanby Hodgson, Petrov Kimberly, Daniel J. Price, Stephen A. Thomson, Eugene L. Stewart, Christie Schulte, Ashley Paul Hancock, Terrence L. Smalley, Michael R. Jeune, H. Fritz Kramer, Chuck Poole, Heather Hobbs, Kirsten M. Kahler, J. Darren Stuart, Paul N. Mortenson, Robert T. Nolte, Jason A. Holt, David N. Deaton, Don O. Somers, Elsie Diaz, Jeffrey Guss, Robert T. Gampe, Peckham Gregory
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 47:128113
Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally active imida
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7e5ec2ff7577c529db47e5be2c91881
https://doi.org/10.1016/j.bmcl.2021.128113
https://doi.org/10.1016/j.bmcl.2021.128113