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Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain

Autor: Andrews Mark David, Robert M. Owen, Mathilde Grenie, Kevin Beaumont, David C. Pryde, Sebastien Galan, Dannielle Frances Roberts, Tram T. Tran, Paul Alan Glossop, Amy S. Kenyon, Graham Lunn, Alan S. Jessiman, Maw Graham Nigel, Kerry af Forselles

Publikováno v: ACS Medicinal Chemistry Letters. 6:419-424

The transient receptor potential (TRP) family of ion channels comprises nonselective cation channels that respond to a wide range of chemical and thermal stimuli. TRPM8, a member of the melastatin subfamily, is activated by cold temperatures (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::941a1288871b774cfd5c8457ad7fad19
https://doi.org/10.1021/ml500479v

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Use of libraries to access new chemical space: Applications to CRTH2

Autor: Graham Lunn, David Winpenny, M. J. Gardner, M. Abid Masood, Dack Kevin Neil

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:3682-3687

The generation of novel CRTH2 ligands in heavily congested chemical space, by de novo design of libraries is disclosed. Novel (1719) compounds across seven libraries were synthesised. More than 100 of these compounds showed binding potency

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9813bfd0d008060fc9336d8b8386d5c4
https://doi.org/10.1016/j.bmcl.2012.04.041

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SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as μ opioid ligands

Autor: Graham Lunn, Lee R. Roberts, Stephane Content, Douglas J. Critcher, Sara Douglas, Ashley E. Fenwick, David M. Gethin, Graham Goodwin, David Greenway, Sean Greenwood, Kim Hall, Martin Thomas, Stephen Thompson, David Williams, Gavin Wood, Andrew Wylie

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:2200-2203

3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral μ opioid receptor ligands for the treatment of pruritus in dogs. In this paper, we describe the SAR of this class of opioid ligand, highlighting changes to the lead structure which l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c017f322826a745bdf3dc4c3c39e124b
https://doi.org/10.1016/j.bmcl.2012.01.099

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The discovery and profile of PF-0868087, a CNS-sparing histamine H3 receptor antagonist for the treatment of allergic rhinitis

Autor: Michael Yeadon, Tanya Hay, Wai L. S. Liu, Charles E. Mowbray, Valerie M. Joynson, Graham Lunn

Publikováno v: Med. Chem. Commun.. 3:339-343

We wished to identify a CNS-sparing histamine H3 receptor antagonist for the treatment of allergic rhinitis. We aimed for compounds with low permeability, high solubility, that were substrates for the BBB efflux transporters MDR-1 and BCRP. The key l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::686aec730e5fd6b030bae89265f437a6
https://doi.org/10.1039/c2md00276k

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Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a ‘magic methyl’ giving a 35-fold improvement in binding

Autor: Yogesh A. Sabnis, Alan John Pettman, Bernard Joseph Banks, Neil Feeder, Robert Crook, Graham Lunn

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:4608-4611

In looking for a novel achiral μ opioid receptor antagonist for the treatment of pruritus, we designed and synthesised azabicyclo[3.1.0]hexane compounds as a new class of opioid ligand. During optimisation, an addition of a single methyl resulted in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0e297263a99c7bdbaee7eefac415c3a
https://doi.org/10.1016/j.bmcl.2011.05.132

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In vitro and In vivo Assessment of Pi3Kγ Inhibitors for Anti-Inflammatory Indications: Challenges of Selectivity over Pi3Kα

Autor: Graham Lunn, Iain Kilty, David J. Lamb, Mark O Reilly, Cheryl Butler

Publikováno v: Journal of Pulmonary & Respiratory Medicine.

Class 1 PI3Ks are a growing area of interest as pharmacological targets across a number of disease mechanisms. We have assessed the feasibility of developing selective PI3Kgamma inhibitors based upon the ATP-binding hinge site. Following full file sc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::60d51fa78a6fc686da4d79ce9e30a5f5
https://doi.org/10.4172/2161-105x.1000157

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Investigation of the effect of molecular properties on the binding kinetics of a ligand to its biological target

Autor: Paul Driscoll, Miller Duncan Charles, Nichola L. Davies, Peter Jones, Graham Lunn, Yogesh A. Sabnis

Publikováno v: MedChemComm. 3:449

A database of binding kinetic data across multiple targets has been created. Analysis of this database provides insights into trends for the effects of physicochemical properties (molecular weight, clogP, rotatable bond count) on the dissociation kin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::77b0f03c9a0f9217ba086206d1295f70
https://doi.org/10.1039/c2md00270a

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