Title : Structural basis for telmisartan-mediated partial activation of PPAR gamma.

Pub. Date : 2012 Jul

PMID : 22357520






1 Functional Relationships(s)
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1 To understand how telmisartan partially activates PPARgamma, we determined the ternary complex structure of PPARgamma, telmisartan, and a coactivator peptide from steroid receptor coactivator-1 at a resolution of 2.18 A. Crystallographic analysis revealed that telmisartan exhibits an unexpected binding mode in which the central benzimidazole ring is engaged in a non-canonical--and suboptimal--hydrogen-bonding network around helix 12 (H12). benzimidazole peroxisome proliferator activated receptor gamma Homo sapiens