John A Christopher
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Explore the profile of John A Christopher including associated specialties, affiliations and a list of published articles.
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33
Citations
510
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Recent Articles
11.
Tehan B, Christopher J
Curr Opin Pharmacol
. 2016 Jul;
30:8-13.
PMID: 27400445
Recent developments in receptor stabilisation have facilitated major advances in G protein-coupled receptor (GPCR) research, notably structural biology, over the past eight years. Here we review the application of fragment,...
12.
Andrews S, Aves S, Christopher J, Nonoo R
Curr Top Med Chem
. 2015 Sep;
16(29):3438-3469.
PMID: 26416477
The orexin receptors OX1 and OX2 play important roles in the regulation of sleep-wake cycles, feeding, reward and energy homeostasis. Since these G protein-coupled receptors were deorphanised in 1998, more...
13.
Christopher J, Aves S, Bennett K, Dore A, Errey J, Jazayeri A, et al.
J Med Chem
. 2015 Jul;
58(16):6653-64.
PMID: 26225459
Fragment screening of a thermostabilized mGlu5 receptor using a high-concentration radioligand binding assay enabled the identification of moderate affinity, high ligand efficiency (LE) pyrimidine hit 5. Subsequent optimization using structure-based...
14.
Christopher J
Pharm Pat Anal
. 2014 Dec;
3(6):625-38.
PMID: 25489915
The orexin-1 and orexin-2 receptors are two G protein-coupled receptors that bind the neuropeptides orexin-A and orexin-B. Dual antagonism of the receptors by small molecules is clinically efficacious in the...
15.
Bennett K, Dore A, Christopher J, Weiss D, Marshall F
Curr Opin Pharmacol
. 2014 Dec;
20:1-7.
PMID: 25462286
The metabotropic glutamate receptor family includes many potential therapeutic targets for a wide range of neurological disorders however to date no approved drugs have progressed to market. For some receptor...
16.
Andrews S, Brown G, Christopher J
ChemMedChem
. 2013 Dec;
9(2):256-75.
PMID: 24353016
G protein-coupled receptors (GPCRs) are an important family of membrane proteins; historically, drug discovery in this target class has been fruitful, with many of the world's top-selling drugs being GPCR...
17.
Christopher J
Pharm Pat Anal
. 2013 Nov;
1(3):329-46.
PMID: 24236845
The orexin neuropeptides bind to two G protein-coupled receptors, orexin-1 and -2. Small-molecule antagonism of the receptors has potential therapeutic utility in a number of areas, most notably insomnia, for...
18.
Christopher J, Brown J, Dore A, Errey J, Koglin M, Marshall F, et al.
J Med Chem
. 2013 Mar;
56(9):3446-55.
PMID: 23517028
Biophysical fragment screening of a thermostabilized β1-adrenergic receptor (β1AR) using surface plasmon resonance (SPR) enabled the identification of moderate affinity, high ligand efficiency (LE) arylpiperazine hits 7 and 8. Subsequent...
19.
Christopher J, Congreve M
Expert Opin Ther Pat
. 2013 Jan;
23(2):273-7.
PMID: 23282091
Application WO2012081692 from Taisho Pharmaceutical Co. Ltd. claims pyrazole-based antagonists of the orexin-1 and orexin-2 receptors. Utility in a number of therapeutic areas is claimed, including the treatment of sleep...
20.
Bamborough P, Brown M, Christopher J, Chung C, Mellor G
J Med Chem
. 2011 Jun;
54(14):5131-43.
PMID: 21699136
A kinase-focused screening set of fragments has been assembled and has proved successful for the discovery of ligand-efficient hits against many targets. Here we present some of our general conclusions...