4lce | pdb_00004lce

CtBP1 in complex with substrate MTOB

spinqualitylabelsall models 4lce, resolution 2.38Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4lce is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: KMT, NAD Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function CTBP1_HUMAN Involved in controlling the equilibrium between tubular and stacked structures in the Golgi complex. Functions in brown adipose tissue (BAT) differentiation. Corepressor targeting diverse transcription regulators such as GLIS2. Has dehydrogenase activity. Publication Abstract from PubMed The oncogenic corepressors C-terminal Binding Protein (CtBP) 1 and 2 harbor regulatory d-isomer specific 2-hydroxyacid dehydrogenase (d2-HDH) domains. 4-Methylthio 2-oxobutyric acid (MTOB) exhibits substrate inhibition and can interfere with CtBP oncogenic activity in cell culture and mice. Crystal structures of human CtBP1 and CtBP2 in complex with MTOB and NAD+ revealed two key features: a conserved tryptophan that likely contributes to substrate specificity and a hydrophilic cavity that links MTOB with an NAD+ phosphate. Neither feature is present in other d2-HDH enzymes. These structures thus offer key opportunities for the development of highly selective anti-neoplastic CtBP inhibitors. Crystal structures of human CtBP in complex with substrate MTOB reveal active site features useful for inhibitor design.,Hilbert BJ, Grossman SR, Schiffer CA, Royer WE Jr FEBS Lett. 2014 Mar 19. pii: S0014-5793(14)00231-2. doi:, 10.1016/j.febslet.2014.03.026. PMID:24657618 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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