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
Descripción
Sumario: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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