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

FEBS Letters

Osada, Hiroyuki¹  Hamaguchi, Takuya¹  Sudo, Tatsuhiko¹ 

[1] Antibiotics Laboratory, The Institute of Physical and Chemical Research (RIKEN), Hirosawa 2-1, Wako-shi, Saitama 351-01, Japan

关键词: Tyrosine phosphatase inhibitor;    Cell cycle;    cdc25B;    CD45;    VHR;    Microbial product;   

DOI  :  10.1016/0014-5793(95)00953-7

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 μM, 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.

【 授权许可】

Unknown