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A new small molecule inhibitor of soluble guanylate cyclase

Mota, F; Gane, P; Hampden-Smith, K; Allerston, CK; Garthwaite, J; Selwood, DL; (2015) A new small molecule inhibitor of soluble guanylate cyclase. Bioorganic & Medicinal Chemistry , 23 (17) pp. 5303-5310. 10.1016/j.bmc.2015.07.074. Green open access

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Abstract

Soluble guanylate cyclase (sGC) is a haem containing enzyme that regulates cardiovascular homeostasis and multiple mechanisms in the central and peripheral nervous system. Commonly used inhibitors of sGC activity act through oxidation of the haem moiety, however they also bind haemoglobin and this limits their bioavailability for in vivo studies. We have discovered a new class of small molecule inhibitors of sGC and have characterised a compound designated D12 (compound 10) which binds to the catalytic domain of the enzyme with a KD of 11 μM in a SPR assay.

Type: Article
Title: A new small molecule inhibitor of soluble guanylate cyclase
Location: England
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.bmc.2015.07.074
Publisher version: http://dx.doi.org/10.1016/j.bmc.2015.07.074
Language: English
Additional information: © 2015 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
Keywords: Nitric oxide, ODQ, Surface plasmon resonance, sGC (soluble guanylate cyclase)
UCL classification: UCL
UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Wolfson Inst for Biomedical Research
URI: https://discovery.ucl.ac.uk/id/eprint/1472966
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