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Bioorg Med Chem. 2015 Sep 1;23(17):5303-10. doi: 10.1016/j.bmc.2015.07.074. Epub 2015 Aug 4.

A new small molecule inhibitor of soluble guanylate cyclase.

Author information

1
The Wolfson Institute for Biomedical Research, University College London, Gower Street, London WC1E 6BT, United Kingdom.
2
Structural Genomics Consortium, University of Oxford, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom.
3
The Wolfson Institute for Biomedical Research, University College London, Gower Street, London WC1E 6BT, United Kingdom. Electronic address: d.selwood@ucl.ac.uk.

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.

KEYWORDS:

Nitric oxide; ODQ; Surface plasmon resonance; sGC (soluble guanylate cyclase)

PMID:
26264842
PMCID:
PMC4558462
DOI:
10.1016/j.bmc.2015.07.074
[Indexed for MEDLINE]
Free PMC Article

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