4ig5

Crystal Structure of Methimazole Inhibited Dimeric Goat Lactoperoxidase at 1.97A Resolution

spinqualitylabelsall models 4ig5, resolution 1.97Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4ig5 is a 2 chain structure with sequence from Capra hircus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: CA, GOL, HEM, MMZ, NAG, NO3 Related: 3sxv, 3r55 Activity: Peroxidase, with EC number 1.11.1.7 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Publication Abstract from PubMed The mammalian haem peroxidase superfamily consists of myeloperoxidase (MPO), lactoperoxidase (LPO), eosinophil peroxidase (EPO) and thyroid peroxidase (TPO). These enzymes catalyze a number of oxidative reactions of inorganic substrates such as Cl(-), Br(-), I(-) and SCN(-) as well as of various organic aromatic compounds. To date, only structures of MPO and LPO are known. The substrate-binding sites in these enzymes are located on the distal haem side. Propylthiouracil (PTU) is a potent antithyroid drug that acts by inhibiting the function of TPO. It has also been shown to inhibit the action of LPO. However, its mode of binding to mammalian haem peroxidases is not yet known. In order to determine the mode of its binding to peroxidases, the structure of the complex of LPO with PTU has been determined. It showed that PTU binds to LPO in the substrate-binding site on the distal haem side. The IC50 values for the inhibition of LPO and TPO by PTU are 47 and 30 microM, respectively. A comparision of the residues surrounding the substrate-binding site on the distal haem side in LPO with those in TPO showed that all of the residues were identical except for Ala114 (LPO numbering scheme), which is replaced by Thr205 (TPO numbering scheme) in TPO. A threonine residue in place of alanine in the substrate-binding site may affect the affinity of PTU for peroxidases. Mode of binding of the antithyroid drug propylthiouracil to mammalian haem peroxidases.,Singh RP, Singh A, Kushwaha GS, Singh AK, Kaur P, Sharma S, Singh TP Acta Crystallogr F Struct Biol Commun. 2015 Mar 1;71(Pt 3):304-10. doi:, 10.1107/S2053230X15001806. Epub 2015 Feb 19. PMID:25760705 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Lactoperoxidase

Proteopedia Page Contributors and Editors (what is this?)

OCA