ヒトUDP-グルクロン酸転移酵素1A7の特性評価: 208番目とその周辺アミノ酸の役割

堤 諒太; 宮内 優; 江越 菜月; Peter I. MACKENZIE; 田中 嘉孝; 石井 祐次

doi:10.14869/toxpt.47.1.0_P-69E

The 47th Annual Meeting of the Japanese Society of Toxicology

Session ID : P-69E

DOI https://doi.org/10.14869/toxpt.47.1.0_P-69E

Conference information

Host: The Japanese Society of Toxicology

Name : The 47th Annual Meeting of the Japanese Society of Toxicology

Date : 2020 -

Poster

Characterization of human UDP-glucuronosyltransferase 1A7: the role of Trp208 and surrounding residues

*Ryota TSUTSUMI, Yuu MIYAUCHI, Natsuki EGOSHI, Peter I. MACKENZIE, Yoshitaka TANAKA, Yuji ISHII

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CONFERENCE PROCEEDINGS FREE ACCESS

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Abstract

Recently, we found that the W208A substitution in human UDP-glucuronosyltransferase (UGT)1A7 diminished its function, even though the corresponding residue of UGT1A6, a related active isoform, is Ala. To address this anomaly, we constructed mutants of UGT1A7 to evaluate the role of Trp208 and its surrounding residues on its SN-38 glucuronidation activity. Analyses of the mutations suggest that His210 has a negative effect on UGT1A7 activity and further, that activity of the UGT1A7(W208A) mutant is restored when the surrounding residues are mutated to mimic those of UGT1A6.

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