Affordable Access

Publisher Website

Stable expression of natriuretic peptide receptors: Effects of HS-142-1, a non-peptide ANP antagonist

Authors
Journal
Biochemical and Biophysical Research Communications
0006-291X
Publisher
Elsevier
Publication Date
Volume
189
Issue
1
Identifiers
DOI: 10.1016/0006-291x(92)91563-6

Abstract

Abstract We established clonal cell lines stably expressing each of two subtypes of membrane bound guanylate cyclases (GC-A and GC-B), which are known as natriuretic peptide receptors. Using these cell lines, we showed that GC-A is an ANP/BNP receptor, whereas GC-B is a specific receptor for CNP. Effects of HS-142-1, a novel non-peptide ANP antagonist, on GC-A and GC-B were examined by using these cells. In cells expressing either GC-A or GC-B, HS-142-1 inhibited cGMP production elicited by ANP or CNP with IC 50 values of 1.8 μg/ml and 1.5 μg/ml, respectively, and also competitively blocked specific binding of the natriuretic peptides with IC 50 values of 2.2 μg/ml and 3.3 μg/ml, respectively. These results indicate that HS-142-1 is a potent antagonist of CNP as well as ANP. We also showed that CNP suppressed the growth of cells expressing GC-B by 22% and that HS-142-1 blocked the antiproliferative action of CNP.

There are no comments yet on this publication. Be the first to share your thoughts.