Antagonism of human adiponectin receptors and their membrane progesterone receptor paralogs by TNFα and a ceramidase inhibitor

Brian R. Kupchak, Ibon Garitaonandia, Nancy Y. Villa, Jessica L. Smith, Thomas J. Lyons

Research output: Contribution to journalArticle

37 Scopus citations

Abstract

The progestin and AdipoQ receptor (PAQR) family of proteins comprises three distinct structural classes, each with seemingly different agonist specificities. For example, Class I receptors, like the human adiponectin receptors (AdipoR1 and AdipoR2), sense proteins with a particular three-dimensional fold, while Class II receptors are nonclassical membrane receptors for the steroid hormone progesterone. Using a previously developed heterologous expression system to study PAQR receptor activity, we demonstrate that human PAQRs from all three classes are antagonized by both 1(S),2(R)-D-erythro-2-(N-myristoylamino)-1-phenyl-1-propanol, a ceramidase inhibitor, and TNFα, a homologue of adiponectin that functions antagonistically to both adiponectin and progesterone in human cells.

Original languageEnglish (US)
Pages (from-to)5504-5506
Number of pages3
JournalBiochemistry
Volume48
Issue number24
DOIs
StatePublished - Jun 23 2009

ASJC Scopus subject areas

  • Biochemistry

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