John A Christopher
Overview
Explore the profile of John A Christopher including associated specialties, affiliations and a list of published articles.
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Articles
33
Citations
510
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Recent Articles
1.
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...
2.
Bucknell S, Ator M, Brown A, Brown J, Cansfield A, Cansfield J, et al.
J Med Chem
. 2020 Jun;
63(14):7906-7920.
PMID: 32558564
Structure-based drug design enabled the discovery of , HTL22562, a calcitonin gene-related peptide (CGRP) receptor antagonist. The structure of complexed with the CGRP receptor was determined at a 1.6 Å...
3.
Bennett K, Christopher J, Tehan B
Adv Pharmacol
. 2020 May;
88:35-58.
PMID: 32416871
The metabotropic glutamate (mGlu) receptors are a family of eight class C G protein-coupled receptors (GPCRs) which modulate cell signaling and synaptic transmission to the major excitatory neurotransmitter l-glutamate (l-glutamic...
4.
Rappas M, Ali A, Bennett K, Brown J, Bucknell S, Congreve M, et al.
J Med Chem
. 2019 Dec;
63(4):1528-1543.
PMID: 31860301
The orexin system, which consists of the two G protein-coupled receptors OX and OX, activated by the neuropeptides OX-A and OX-B, is firmly established as a key regulator of behavioral...
5.
Suzuki R, Brown G, Christopher J, Scully C, Congreve M
J Med Chem
. 2019 Oct;
63(3):905-927.
PMID: 31577440
Glucagon-like peptide 1 (GLP-1) and glucagon-like peptide 2 (GLP-2) are proglucagon derived peptides that are released from gut endocrine cells in response to nutrient intake. These molecules are rapidly inactivated...
6.
OBrien A, Andrews S, Baig A, Bortolato A, Brown A, Brown G, et al.
Bioorg Med Chem Lett
. 2019 Aug;
29(20):126611.
PMID: 31447084
A series of novel allosteric antagonists of the GLP-1 receptor (GLP-1R), exemplified by HTL26119, are described. SBDD approaches were employed to identify HTL26119, exploiting structural understanding of the allosteric binding...
7.
Kerns J, Busch-Petersen J, Fu W, Boehm J, Nie H, Muratore M, et al.
ACS Med Chem Lett
. 2019 Jan;
9(12):1164-1169.
PMID: 30613320
IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization...
8.
Christopher J, Orgovan Z, Congreve M, Dore A, Errey J, Marshall F, et al.
J Med Chem
. 2018 Feb;
62(1):207-222.
PMID: 29455526
Two interesting new X-ray structures of negative allosteric modulator (NAM) ligands for the mGlu receptor, M-MPEP (3) and fenobam (4), are reported. The new structures show how the binding of...
9.
Oswald C, Rappas M, Kean J, Dore A, Errey J, Bennett K, et al.
Nature
. 2016 Dec;
540(7633):462-465.
PMID: 27926729
Chemokines and their G-protein-coupled receptors play a diverse role in immune defence by controlling the migration, activation and survival of immune cells. They are also involved in viral entry, tumour...
10.
Christopher J, Dore A, Tehan B
Curr Top Med Chem
. 2016 Jul;
17(1):71-78.
PMID: 27448651
Class C G protein-coupled receptors encompass a range of promising therapeutic targets for a variety of diseases, yet to date only two members of this sub-family of GPCRs have been...