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Gordon Saxty

Explore the profile of Gordon Saxty including associated specialties, affiliations and a list of published articles. Areas
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Articles 14
Citations 444
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Recent Articles
1.
Southall S, Banerjee J, Brown J, Butkovic K, Cansfield A, Cansfield J, et al.
ACS Med Chem Lett . 2022 Nov; 13(11):1776-1782. PMID: 36385934
The diastereomeric macrocyclic calcitonin gene-related peptide (CGRP) antagonists HTL0029881 () and HTL0029882 (), in which the stereochemistry of a spiro center is reversed, surprisingly demonstrate comparable potency. X-ray crystallographic characterization...
2.
Cansfield A, Ator M, Banerjee J, Bestwick M, Bortolato A, Brown G, et al.
ACS Chem Neurosci . 2022 Mar; 13(6):751-765. PMID: 35245037
A series of macrocyclic calcitonin gene-related peptide (CGRP) receptor antagonists identified using structure-based design principles, exemplified by HTL0028016 () and HTL0028125 (), is described. Structural characterization by X-ray crystallography of...
3.
Kostrun S, Fajdetic A, Pesic D, Brajsa K, Bencetic Mihaljevic V, Jelic D, et al.
J Med Chem . 2021 Jun; 64(12):8354-8383. PMID: 34100601
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 diseases...
4.
Schulte C, Deaton D, Diaz E, Do Y, Gampe R, Guss J, et al.
Bioorg Med Chem Lett . 2021 May; 47:128113. PMID: 33991628
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...
5.
Cadilla R, Deaton D, Do Y, Elkins P, Ennulat D, Guss J, et al.
Bioorg Med Chem . 2020 Oct; 28(23):115791. PMID: 33059303
GlaxoSmithKline and Astex Pharmaceuticals recently disclosed the discovery of the potent H-PGDS inhibitor GSK2894631A 1a (IC = 9.9 nM) as part of a fragment-based drug discovery collaboration with Astex Pharmaceuticals....
6.
Heightman T, Callahan J, Chiarparin E, Coyle J, Griffiths-Jones C, Lakdawala A, et al.
J Med Chem . 2019 Apr; 62(9):4683-4702. PMID: 30973731
The KEAP1-NRF2-mediated cytoprotective response plays a key role in cellular homoeostasis. Insufficient NRF2 signaling during chronic oxidative stress may be associated with the pathophysiology of several diseases with an inflammatory...
7.
Deaton D, Do Y, Holt J, Jeune M, Kramer H, Larkin A, et al.
Bioorg Med Chem . 2019 Mar; 27(8):1456-1478. PMID: 30858025
With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a fragment-based screen of hematopoietic prostaglandin D synthase was performed. The 76 crystallographic hits...
8.
Johnson C, Ahn J, Buck I, Chiarparin E, Day J, Hopkins A, et al.
J Med Chem . 2018 Aug; 61(16):7314-7329. PMID: 30091600
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...
9.
Alihodzic S, Bukvic M, Elenkov I, Hutinec A, Kostrun S, Pesic D, et al.
Prog Med Chem . 2018 Apr; 57(1):113-233. PMID: 29680148
This chapter will discuss the recent literature of macrocycles and drug-like property space moving beyond the rule of five (bRo5). Trends in chemical classes that fall within this definition are...
10.
Perera T, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, et al.
Mol Cancer Ther . 2017 Mar; 16(6):1010-1020. PMID: 28341788
Fibroblast growth factor (FGF) signaling plays critical roles in key biological processes ranging from embryogenesis to wound healing and has strong links to several hallmarks of cancer. Genetic alterations in...