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RK‐682, a potent inhibitor of tyrosine phosphatase, arrested the mammalian cell cycle progression at G 1 phase
Author(s) -
Hamaguchi Takuya,
Sudo Tatsuhiko,
Osada Hiroyuki
Publication year - 1995
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(95)00953-7
Subject(s) - sodium orthovanadate , dephosphorylation , phosphoserine , chemistry , biochemistry , protein tyrosine phosphatase , cell cycle , tyrosine , serine , phosphatase , cell growth , microbiology and biotechnology , threonine , phosphorylation , cell , biology
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 IC 50 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 G 2 /M boundary phase, on the other hand, RK‐682 inhibited the G 1 /S transition.