A Series of Substituted Bis-Aminotriazines Are Activators of the Natriuretic Peptide Receptor C.


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
14 04 2022
Historique:
pubmed: 26 3 2022
medline: 16 4 2022
entrez: 25 3 2022
Statut: ppublish

Résumé

C-type natriuretic peptide (CNP) is involved in the regulation of vascular homeostasis, which is at least partly mediated through agonism of natriuretic peptide receptor C (NPR-C), and loss of this signaling has been associated with vascular dysfunction. As such, NPR-C is a novel therapeutic target to treat cardiovascular diseases. A series of novel small molecules have been designed and synthesized, and their structure-activity relationships were evaluated by a surface plasmon resonance binding assay. The biological activity of hit compounds was confirmed through organ bath assays measuring vascular relaxation and inhibition of cAMP production, which was shown to be linked to its NPR-C activity. Lead compound

Identifiants

pubmed: 35333039
doi: 10.1021/acs.jmedchem.1c01974
pmc: PMC9014859
doi:

Substances chimiques

Natriuretic Peptide, C-Type 127869-51-6

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

5495-5513

Subventions

Organisme : British Heart Foundation
ID : TG/15/3/31692
Pays : United Kingdom

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Auteurs

Robert J Smith (RJ)

Wolfson Institute for Biomedical Research, University College London, Cruciform Building, Gower St, London WC1E 6DH, U.K.

Cristina Perez-Ternero (C)

William Harvey Research Institute, Barts & The London School of Medicine, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, U.K.

Daniel Conole (D)

Wolfson Institute for Biomedical Research, University College London, Cruciform Building, Gower St, London WC1E 6DH, U.K.

Capucine Martin (C)

William Harvey Research Institute, Barts & The London School of Medicine, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, U.K.

Samuel H Myers (SH)

Wolfson Institute for Biomedical Research, University College London, Cruciform Building, Gower St, London WC1E 6DH, U.K.

Adrian J Hobbs (AJ)

William Harvey Research Institute, Barts & The London School of Medicine, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, U.K.

David L Selwood (DL)

Wolfson Institute for Biomedical Research, University College London, Cruciform Building, Gower St, London WC1E 6DH, U.K.

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Classifications MeSH