Mota, F;
Allerston, CK;
Hampden-Smith, K;
Garthwaite, J;
Selwood, DL;
(2014)
Surface plasmon resonance using the catalytic domain of soluble guanylate cyclase allows the detection of enzyme activators.
Bioorg Med Chem Lett
, 24
(4)
pp. 1075-1079.
10.1016/j.bmcl.2014.01.015.
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Abstract
Soluble Guanylate Cyclase (sGC) is the receptor for the signalling agent nitric oxide (NO) and catalyses the production of the second messenger cyclic guanosine monophosphate (cGMP) from guanosine triphosphate (GTP). The enzyme is an attractive drug target for small molecules that act in the cardiovascular and pulmonary systems, and has also shown to be a potential target in neurological disorders. We have discovered that 5-(indazol-3-yl)-1,2,4-oxadiazoles activate the enzyme in the absence of added NO and shown they bind to the catalytic domain of the enzyme after development of a surface plasmon resonance assay that allows the biophysical detection of intrinsic binding of ligands to the full length sGC and to a construct of the catalytic domain.
| Type: | Article |
|---|---|
| Title: | Surface plasmon resonance using the catalytic domain of soluble guanylate cyclase allows the detection of enzyme activators. |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1016/j.bmcl.2014.01.015 |
| Publisher version: | http://dx.doi.org/10.1016/j.bmcl.2014.01.015 |
| Additional information: | �© 2014 The Authors. Published by Elsevier Ltd. All rights reserved. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
| Keywords: | Biophysical techniques, Enzyme activators, Nitric oxide, Soluble guanylate cyclase, Surface plasmon resonance |
| UCL classification: | UCL 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/1421998 |
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