TY - JOUR
T1 - Chemical genetic identification of the histamine H1 receptor as a stimulator of insulin-induced adipogenesis
AU - Kawazoe, Yoshinori
AU - Tanaka, Satoshi
AU - Uesugi, Motonari
N1 - Funding Information:
This work is supported in part by U.S. Department of Defense Prostate Cancer Research Program (DAMD17-03-1-0228). Y.K. is a Postdoctoral Fellow of The American Parkinson Disease Association. We thank J.H. Wilson for editing the manuscript and the members of the Uesugi group for discussion and encouragement.
Copyright:
Copyright 2011 Elsevier B.V., All rights reserved.
PY - 2004/7
Y1 - 2004/7
N2 - 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.
AB - 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.
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U2 - 10.1016/j.chembiol.2004.04.017
DO - 10.1016/j.chembiol.2004.04.017
M3 - Article
C2 - 15271349
AN - SCOPUS:3342885452
VL - 11
SP - 907
EP - 913
JO - Cell Chemical Biology
JF - Cell Chemical Biology
SN - 2451-9448
IS - 7
ER -