5xmx

Co-crystal structure of Inhibitor compound in complex with human PPARdelta LBD

spinqualitylabelsall models 5xmx, resolution 2.00Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 5xmx is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2Å Ligands: 89L Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function PPARD_HUMAN Ligand-activated transcription factor. Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Has a preference for poly-unsaturated fatty acids, such as gamma-linoleic acid and eicosapentanoic acid. Once activated by a ligand, the receptor binds to promoter elements of target genes. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the acyl-CoA oxidase gene. Decreases expression of NPC1L1 once activated by a ligand. Publication Abstract from PubMed Optimization of benzamide PPARdelta modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARdelta modulator with significantly improved exposure in multiple species following oral administration. Novel highly selective peroxisome proliferator-activated receptor delta (PPARdelta) modulators with pharmacokinetic properties suitable for once-daily oral dosing.,Lagu B, Kluge AF, Fredenburg RA, Tozzo E, Senaiar RS, Jaleel M, Panigrahi SK, Tiwari NK, Krishnamurthy NR, Takahashi T, Patane MA Bioorg Med Chem Lett. 2017 Dec 1;27(23):5230-5234. doi:, 10.1016/j.bmcl.2017.10.037. Epub 2017 Oct 27. PMID:29103972 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Peroxisome proliferator-activated receptor 3D structures

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