3p88

FXR bound to isoquinolinecarboxylic acid

spinqualitylabelsall models 3p88, resolution 2.95Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3p88 is a 2 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: P88, SO4 Related: 3p89 Gene: hCG_20893, NR1H4 (HUMAN), BHLHE74, NCOA1, SRC1 (HUMAN) Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Publication Abstract from PubMed To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes. Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.,Bass JY, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Mills WY, Navas F 3rd, Parks DJ, Smalley TL Jr, Spearing PK, Todd D, Williams SP, Wisely GB Bioorg Med Chem Lett. 2011 Feb 15;21(4):1206-13. Epub 2010 Dec 23. PMID:21256005 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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