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Small atrial natriuretic peptide analogues: design, synthesis, and structural requirements for guanylate cyclase activation.

Abstract：

:Structure/activity studies on atrial natriuretic peptide ANP (1-28) have highlighted three portions of the native molecule as necessary for its biological responses. We have linked these three regions and excised the remaining segments to produce a family of small analogues (less than half the size of the parent) which demonstrate the full range of ANP's actions. Importantly, these compounds act at both major types of ANP receptor. Two critical modifications lead to more potent analogues; both involve expanding the cyclic portion of the molecule. Further optimization of one of these modified structures leads to A68828, a full ANP agonist which shows promise as a preventative agent against acute renal failure.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

von Geldern TW,Rockway TW,Davidsen SK,Budzik GP,Bush EN,Chu-Moyer MY,Devine EM Jr,Holleman WH,Johnson MC,Lucas SD

doi

10.1021/jm00083a003

keywords:

subject

Has Abstract,Author List Incomplete

pub_date

1992-03-06 00:00:00

pages

808-16

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

35

pub_type

杂志文章

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