A new small molecule inhibitor of soluble guanylate cyclase

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 l...

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Detalles Bibliográficos
Autores principales: Mota, Filipa, Gane, Paul, Hampden-Smith, Kathryn, Allerston, Charles K., Garthwaite, John, Selwood, David L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Science 2015
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4558462/
https://www.ncbi.nlm.nih.gov/pubmed/26264842
http://dx.doi.org/10.1016/j.bmc.2015.07.074
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author Mota, Filipa
Gane, Paul
Hampden-Smith, Kathryn
Allerston, Charles K.
Garthwaite, John
Selwood, David L.
author_facet Mota, Filipa
Gane, Paul
Hampden-Smith, Kathryn
Allerston, Charles K.
Garthwaite, John
Selwood, David L.
author_sort Mota, Filipa
collection PubMed
description 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 K(D) of 11 μM in a SPR assay.
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spelling pubmed-45584622015-10-14 A new small molecule inhibitor of soluble guanylate cyclase Mota, Filipa Gane, Paul Hampden-Smith, Kathryn Allerston, Charles K. Garthwaite, John Selwood, David L. Bioorg Med Chem Article 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 K(D) of 11 μM in a SPR assay. Elsevier Science 2015-09-01 /pmc/articles/PMC4558462/ /pubmed/26264842 http://dx.doi.org/10.1016/j.bmc.2015.07.074 Text en © 2015 The Authors http://creativecommons.org/licenses/by/4.0/ This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Mota, Filipa
Gane, Paul
Hampden-Smith, Kathryn
Allerston, Charles K.
Garthwaite, John
Selwood, David L.
A new small molecule inhibitor of soluble guanylate cyclase
title A new small molecule inhibitor of soluble guanylate cyclase
title_full A new small molecule inhibitor of soluble guanylate cyclase
title_fullStr A new small molecule inhibitor of soluble guanylate cyclase
title_full_unstemmed A new small molecule inhibitor of soluble guanylate cyclase
title_short A new small molecule inhibitor of soluble guanylate cyclase
title_sort new small molecule inhibitor of soluble guanylate cyclase
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4558462/
https://www.ncbi.nlm.nih.gov/pubmed/26264842
http://dx.doi.org/10.1016/j.bmc.2015.07.074
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