Chemical genetic identification of the histamine H1 receptor as a stimulator of insulin-induced adipogenesis

Yoshinori Kawazoe, Satoshi Tanaka, Motonari Uesugi

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

A large collection of bioactive compounds with diverse biological effects can be used as probes to elucidate new biological mechanisms that influence a particular cellular process. Here we analyze the effects of 880 well-known small-molecule bioactives or drugs on the insulin-induced adipogenesis of 3T3-L1 fibroblasts, a cell-culture model of fat cell differentiation. Our screen identified 86 compounds as modulators of the adipogenic differentiation of 3T3-L1 cells. Examination of their chemical and pharmacological information revealed that antihistamine drugs with distinct chemical scaffolds inhibit differentiation. Histamine H1 receptor is expressed in 3T3-L1 cells, and its knockdown by small interfering RNA impaired the insulin-induced adipogenic differentiation. Histamine receptors and histamine-like biogenic amines may play a role in inducing adipogenesis in response to insulin.

Original languageEnglish
Pages (from-to)907-913
Number of pages7
JournalChemistry and Biology
Volume11
Issue number7
DOIs
Publication statusPublished - Jul 1 2004

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry

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