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Discovery of Ligands for the Nuclear Peroxisome Proliferator‐activated Receptors
Author(s) -
WILLSON TIMOTHY M.,
LEHMANN JÜRGEN M.,
KLIEWER STEVEN A.
Publication year - 1996
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1111/j.1749-6632.1996.tb18622.x
Subject(s) - peroxisome proliferator , receptor , nuclear receptor , peroxisome , peroxisome proliferator activated receptor , chemistry , peroxisome proliferator activated receptor alpha , microbiology and biotechnology , biochemistry , biology , transcription factor , gene
The identification of high-affinity ligands for PPAR gamma has revealed the role of this receptor as the molecular target for the antidiabetic activity of the thiazolidinediones. The surprising observation that agonists of an adipogenic transcription factor reverse the obesity-associated disease of diabetes highlights the power of using potent and selective ligands to study receptor-mediated biology. Similarly, the observation that PGD2 and its cyclopentenone metabolites compounds are microM PPAR ligands suggests that these receptors may have a physiological role in mediating prostaglandin signaling in the spleen.