6zjc

Crystal structure of Equus ferus caballus glutathione transferase A3-3 in complex with glutathione and triethyltin

spinqualitylabelsall models 6zjc, resolution 2.20Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6zjc is a 4 chain structure with sequence from Equus caballus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.2Å Ligands: GSH, MPD, QLT Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function M9ZT87_HORSE Publication Abstract from PubMed Organotin compounds are highly toxic environmental pollutants with neurotoxic and endocrine-disrupting effects. They are potent inhibitors of glutathione transferases (GSTs), thus impeding their detoxication and antioxidant functions. Several GSTs, including equine GST A3-3 (EcaGST A3-3), exhibit steroid double-bond isomerase activity and are involved in the biosynthesis of testosterone and progesterone. We have performed enzyme kinetics analyses of the inhibition of EcaGST A3-3 by organotin compounds. We have also solved crystal structures of EcaGST A3-3 in complexes with glutathione, and with glutathione together with covalently bound triethyltin. Our structural data indicate that the tin atom forms strong bonds with a covalent character not only with the glutathione, but also with a tyrosyl residue of the enzyme itself, thereby preventing the release of the glutathione-organotin adduct and completely blocking the enzyme function. This work presents a structural basis for the general mechanism of GST inhibition by organotin compounds and contributes to the understanding of their neurotoxic and endocrine disrupting effects. Structural and functional analysis of the inhibition of equine glutathione transferase A3-3 by organotin endocrine disrupting pollutants.,Skerlova J, Ismail A, Lindstrom H, Sjodin B, Mannervik B, Stenmark P Environ Pollut. 2020 Oct 29:115960. doi: 10.1016/j.envpol.2020.115960. PMID:33162212 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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