Publications by authors named "Gordon Saxty"

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Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
Stacey M Southall, Joydeep Banerjee, Jason Brown, Kristina Butkovic, Andrew D Cansfield, Gordon Saxty

ACS Med Chem Lett· November 2022

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Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.
Andrew D Cansfield, Mark A Ator, Joydeep Banerjee, Michael Bestwick, Andrea Bortolato, Gordon Saxty

ACS Chem Neurosci· March 2022

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A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Christie A Schulte, David N Deaton, Elsie Diaz, Young Do, Robert T Gampe, Gordon Saxty

Bioorg Med Chem Lett· September 2021

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Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction.
Sanja Koštrun, Andrea Fajdetić, Dijana Pešić, Karmen Brajša, Vlatka Bencetić Mihaljević, Gordon Saxty

J Med Chem· June 2021

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The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Rodolfo Cadilla, David N Deaton, Young Do, Patricia A Elkins, Daniela Ennulat, Gordon Saxty

Bioorg Med Chem· December 2020

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Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Tom D Heightman, James F Callahan, Elisabetta Chiarparin, Joseph E Coyle, Charlotte Griffiths-Jones, Gordon Saxty

J Med Chem· May 2019

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The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.
David N Deaton, Young Do, Jason Holt, Michael R Jeune, H Fritz Kramer, Gordon Saxty

Bioorg Med Chem· April 2019

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Current Trends in Macrocyclic Drug Discovery and beyond-Ro5.
Sulejman Alihodžić, Mirjana Bukvić, Ivaylo J Elenkov, Antun Hutinec, Sanja Koštrun, Gordon Saxty

Prog Med Chem· December 2018

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A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).
Christopher N Johnson, Jong Sook Ahn, Ildiko M Buck, Elisabetta Chiarparin, James E H Day, Gordon Saxty

J Med Chem· August 2018

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Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.
Timothy P S Perera, Eleonora Jovcheva, Laurence Mevellec, Jorge Vialard, Desiree De Lange, Gordon Saxty

Mol Cancer Ther· June 2017

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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.
Thomas G Davies, William E Wixted, Joseph E Coyle, Charlotte Griffiths-Jones, Keisha Hearn, Gordon Saxty

J Med Chem· April 2016

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Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.
Christopher W Murray, Valerio Berdini, Ildiko M Buck, Maria E Carr, Anne Cleasby, Gordon Saxty

ACS Med Chem Lett· July 2015

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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 G Wyatt, Andrew J Woodhead, Valerio Berdini, John A Boulstridge, Maria G Carr, Gordon Saxty

J Med Chem· August 2008

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Identification of inhibitors of protein kinase B using fragment-based lead discovery.
Gordon Saxty, Steven J Woodhead, Valerio Berdini, Thomas G Davies, Marcel L Verdonk

J Med Chem· May 2007

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