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RK-682, a potent inhibitor of tyrosine phosphatase, arrested the mammalian cell cycle progression at G1phase.

作者信息

Hamaguchi T, Sudo T, Osada H

机构信息

Antibiotics Laboratory, Institute of Physical and Chemical Research (RIKEN), Saitama, Japan.

出版信息

FEBS Lett. 1995 Sep 18;372(1):54-8. doi: 10.1016/0014-5793(95)00953-7.

DOI:10.1016/0014-5793(95)00953-7
PMID:7556642
Abstract

A specific inhibitor of protein tyrosine phosphatase (PTPase), RK-682 (3-hexadecanoyl-5-hydroxymethyl-tetronic acid) was isolated from microbial metabolites. In vitro, RK-682 inhibited dephosphorylation activity of CD45 and VHR with IC50 54 and 2.0 microM, respectively. In situ, sodium orthovanadate and RK-682 enhanced the phosphotyrosine level of Ball-1 cells, a human B cell leukemia, but not the phosphoserine/threonine level. The PTPase inhibitors, however, had the different arrest point on the cell cycle progression. Sodium orthovanadate inhibited the cell cycle progression at G2/M boundary phase, on the other hand, RK-682 inhibited the G1/S transition.

摘要

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