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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2009-12-17
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pubmed:abstractText |
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.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:AuwerxJohanJ,
pubmed-author:GioielloAntimoA,
pubmed-author:MacchiaruloAntonioA,
pubmed-author:NataliniBenedettoB,
pubmed-author:PastoriniElisabettaE,
pubmed-author:PellicciariRobertoR,
pubmed-author:PruzanskiMarkM,
pubmed-author:RodaAldoA,
pubmed-author:RosatelliEmilianoE,
pubmed-author:SardellaRoccaldoR,
pubmed-author:SchoonjansKristinaK,
pubmed-author:ThomasCharlesC
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pubmed:issnType |
Electronic
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pubmed:day |
24
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
7958-61
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pubmed:meshHeading |
pubmed-meshheading:20014870-Animals,
pubmed-meshheading:20014870-CHO Cells,
pubmed-meshheading:20014870-COS Cells,
pubmed-meshheading:20014870-Cercopithecus aethiops,
pubmed-meshheading:20014870-Cholic Acids,
pubmed-meshheading:20014870-Cricetinae,
pubmed-meshheading:20014870-Cricetulus,
pubmed-meshheading:20014870-Diabetes Mellitus,
pubmed-meshheading:20014870-Humans,
pubmed-meshheading:20014870-Obesity,
pubmed-meshheading:20014870-Rats,
pubmed-meshheading:20014870-Receptors, G-Protein-Coupled,
pubmed-meshheading:20014870-Stereoisomerism
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pubmed:year |
2009
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pubmed:articleTitle |
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.
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pubmed:affiliation |
Dipartimento di Chimica e Tecnologia del Farmaco, Universita di Perugia, 06123 Perugia, Italy. rp@unipg.it
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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