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research article
Discovery of 6alpha-Ethyl-23(S)-methylcholic Acid (S-EMCA, INT-777) as a Potent and Selective Agonist for the TGR5 Receptor, a Novel Target for Diabesity
In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C(23)(S)-methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic acid (6-ECDCA, INT-747) affords selectivity for TGR5. Herein we report further lead optimization efforts that have led to the discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a novel potent and selective TGR5 agonist with remarkable in vivo activity.
Use this identifier to reference this record
Type
research article
Web of Science ID
WOS:000272712100010
Authors
Pellicciari, Roberto
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Macchiarulo, Antonio
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Thomas, Charles
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Rosatelli, Emiliano
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Natalini, Benedetto
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Sardella, Roccaldo
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Pruzanski, Mark
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Roda, Aldo
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Pastorini, Elisabetta
Publication date
2009
Published in
Volume
52
Issue
24
Start page
7958
End page
7961
Peer reviewed
REVIEWED
EPFL units
Available on Infoscience
December 22, 2009