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Journal Articles Peptides Year : 2005

Development of a selective peptide antagonist for the human natriuretic peptide receptor-B.

Abstract

Activation by C-type natriuretic peptide (CNP) of its receptor NPRB results in venodilation and inhibition of cellular proliferation. NPRB-selective antagonists should be useful to understand their physiological implications. We previously observed that [Thr9,Ser11,Arg16](N,C-ANP)pBNP (P12) is an antagonist for bNPRB and a potent agonist for bNPRA. The antagonist [Ser11](N-CNP,C-ANP)pBNP(2-26) (P18) displays six-fold selectivity towards hNPRB versus hNPRA. Deletion of the C-terminus in [Ser11](N-CNP,C-ANP)pBNP(2-25) (P19) decreases its affinity for hNPRA but improves its selectivity 35-fold. Peptide libraries based on P19 using phage display methodology yielded two positive clones P20 and P21. P19 behaves as the most potent antagonist, but P20 is the most selective.

Domains

Toxicology

Dates and versions

pasteur-00820035 , version 1 (03-05-2013)

Identifiers

Cite

Julie Deschênes, Cécile Duperé, Normand Mcnicoll, Nicholas L'Heureux, François Auger, et al.. Development of a selective peptide antagonist for the human natriuretic peptide receptor-B.. Peptides, 2005, 26 (3), pp.517-24. ⟨10.1016/j.peptides.2004.10.017⟩. ⟨pasteur-00820035⟩

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