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PDBsum entry 3fli
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Transcription
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PDB id
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3fli
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References listed in PDB file
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Key reference
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Title
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Discovery of xl335 (way-362450), A highly potent, Selective, And orally active agonist of the farnesoid x receptor (fxr).
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Authors
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B.Flatt,
R.Martin,
T.L.Wang,
P.Mahaney,
B.Murphy,
X.H.Gu,
P.Foster,
J.Li,
P.Pircher,
M.Petrowski,
I.Schulman,
S.Westin,
J.Wrobel,
G.Yan,
E.Bischoff,
C.Daige,
R.Mohan.
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Ref.
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J Med Chem, 2009,
52,
904-907.
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PubMed id
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Abstract
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Azepino[4,5-b]indoles have been identified as potent agonists of the farnesoid X
receptor (FXR). In vitro and in vivo optimization has led to the discovery of 6m
(XL335, WAY-362450) as a potent, selective, and orally bioavailable FXR agonist
(EC(50) = 4 nM, Eff = 149%). Oral administration of 6m to LDLR(-/-) mice results
in lowering of cholesterol and triglycerides. Chronic administration in an
atherosclerosis model results in significant reduction in aortic arch lesions.
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