G
Gordon Saxty
Researcher at Astex
Publications - 69
Citations - 1873
Gordon Saxty is an academic researcher from Astex. The author has contributed to research in topics: Bicyclic molecule & Derivative (chemistry). The author has an hindex of 21, co-authored 67 publications receiving 1653 citations. Previous affiliations of Gordon Saxty include Institute of Cancer Research.
Papers
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Journal ArticleDOI
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.
Paul Graham Wyatt,Andrew James Woodhead,Valerio Berdini,John A. Boulstridge,Maria Grazia Carr,David M. Cross,Deborah J. Davis,Lindsay A. Devine,Theresa Rachel Early,Ruth Feltell,E. Jonathan Lewis,Rachel McMenamin,Eva Figueroa Navarro,Michael Alistair O'brien,Marc O'Reilly,Matthias Reule,Gordon Saxty,Lisa C A Seavers,Donna-Michelle Smith,M. Squires,Gary Trewartha,Margaret T. Walker,Alison Jo-Anne Woolford +22 more
TL;DR: The structure-guided optimization of indazole is detailed, using information gained from multiple ligand-CDK2 cocrystal structures, which led to the identification of 33 (AT7519), which is currently being evaluated in clinical trials for the treatment of human cancers.
Journal ArticleDOI
Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery
T.G. Davies,William E. Wixted,Joseph E. Coyle,Charlotte Mary Griffiths-Jones,Keisha Hearn,Rachel McMenamin,David Norton,Sharna J. Rich,Caroline Richardson,Gordon Saxty,Henriëtte M. G. Willems,Alison Jo-Anne Woolford,Joshua E. Cottom,Jen-Pyng Kou,John Yonchuk,Heidi G. Feldser,Yolanda Sanchez,Joseph P. Foley,Brian Bolognese,Gregory A. Logan,Patricia L. Podolin,Hongxing Yan,James F. Callahan,Tom D. Heightman,Jeffrey K. Kerns +24 more
TL;DR: This work resulted in a promising lead compound which exhibits tight and selective binding to KEAP1, and activates the NRF2 antioxidant response in cellular and in vivo models, thereby providing a high quality chemical probe to explore the therapeutic potential of disrupting theKEAP1-NRF2 interaction.
Journal ArticleDOI
Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.
Timothy Perera,Eleonora Jovcheva,Laurence Anne Mevellec,Jorge Vialard,Desiree De Lange,Tinne Verhulst,Caroline Paulussen,Kelly Van De Ven,Peter King,Eddy Jean Edgard Freyne,David C. Rees,Matthew S Squires,Gordon Saxty,Martin Page,Christopher William Murray,Ron Gilissen,George Ward,Neil T. Thompson,David R. Newell,Na Cheng,Liang Xie,Jennifer Yang,Suso Platero,Jayaprakash Karkera,Christopher Moy,Patrick Angibaud,Sylvie Laquerre,Matthew V. Lorenzi +27 more
TL;DR: The results of the current study provide a strong rationale for the clinical investigation of JNJ-42756493 in patients with tumors harboring FGFR pathway alterations and show rapid uptake into the lysosomal compartment of cells in culture, which is associated with prolonged inhibition of FGFR signaling.
Journal ArticleDOI
Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery
Gordon Saxty,Steven John Woodhead,Valerio Berdini,T.G. Davies,Marcel L. Verdonk,Paul Graham Wyatt,Robert George Boyle,David Barford,Robert Downham,Michelle D. Garrett,Robin Arthur Ellis Carr +10 more
TL;DR: This work describes the rapid elaboration of highly potent and ligand efficient analogues using a fragment growing approach to identify a novel, low molecular weight inhibitor of protein kinase B (PKB).
Patent
Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors
Valerio Berdini,Robert George Boyle,Gordon Saxty,David Winter Walker,Steven John Woodhead,Paul Graham Wyatt,A. Donald,John J. Caldwell,Ian Collins,Tatiana Faria Da Fonseca +9 more
TL;DR: In this paper, a compound for use as a protein kinase B inhibitor is described, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof.