Iodocalcitonin binds to human calcitonin receptors with higher affinity than calcitonin

David P. Cohen, Daniel R. Nussenzveig, Marvin C. Gershengorn

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

The reported binding affinities of cloned human calcitonin receptors (hCTRs) for salmon calcitonin (sCT) vary over a wide range. Because the greatest differences were between values estimated in association binding versus competition binding experiments, we considered the possibility that this variation was due to differences in the affinities of hCTRs for moniodinated sCT (I-sCT) and sCT. We found that I-sCT competed with 125- sCT for binding with 9.3±0.58 times the apparent affinity of sCT in COS-1 and Madin Darby canine kidney (MDCK) cells expressing cloned hCTRs. I-sCT was 25 times more potent than sCT in stimulating cAMP formation in MDCK cells expressing hCTRs. These data demonstrate that monoiodinated sCT interacts more avidly with hCTRs than sCT with a consequent enhanced potency in stimulating second messenger formation. Therefore, as I-sCT (or 125I-sCT) binds with different affinity to hCTRs than sCT, affinity measurements must be performed with I-sCT (or 125I-sCT) alone.

Original languageEnglish (US)
Pages (from-to)4507-4510
Number of pages4
JournalEndocrinology
Volume137
Issue number10
DOIs
StatePublished - 1996

ASJC Scopus subject areas

  • Endocrinology

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