2. Academic Validation
  3. The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1

The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1

  • Bioorg Med Chem Lett. 2000 Sep 4;10(17):1949-52. doi: 10.1016/s0960-894x(00)00387-5.
C A Veale 1,  V C Alford,  D Aharony,  D L Banville,  R A Bialecki,  F J Brown,  J R Damewood Jr,  C L Dantzman,  P D Edwards,  R T Jacobs,  R C Mauger,  M M Murphy,  W Palmer,  K K Pine,  W L Rumsey,  L E Garcia-Davenport,  A Shaw,  G B Steelman,  J M Surian,  E P Vacek
Affiliations

Affiliation

  • 1 Department of Chemistry, AstraZeneca Pharmaceuticals, Wilmington, DE 19850-5437, USA. [email protected]
PMID: 10987424 DOI: 10.1016/s0960-894x(00)00387-5
Abstract

The cyclic peptide ANP 4-23 and the linear peptide analogue AP-811 have been shown to be selective ANP-CR antagonists. Via alanine scanning and truncation studies we sought to determine which residues in these molecules were important in their binding to the clearance receptor and the relationship between these two molecules. These studies show that several modifications to these compounds are possible which improve physical properties of these molecules while retaining high affinity for the ANP-CR.

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