Reference - Detail
|Author||Hamaguchi T, Sudo T, Osada H.|
|Title||RK-682, a potent inhibitor of tyrosine phosphatase, arrested the mammalian cell cycle progression at G1phase.|
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.
|MeSH||Aniline Compounds / metabolism Antifungal Agents / pharmacology Blotting, Western Cell Cycle / drug effects Cell Cycle Proteins / antagonists & inhibitors* Dual Specificity Phosphatase 3 Enzyme Inhibitors / isolation & purification Enzyme Inhibitors / pharmacology* Ethers, Cyclic / pharmacology G1 Phase / drug effects* Humans Kinetics Leukemia, B-Cell Okadaic Acid Organophosphorus Compounds / metabolism Phosphoprotein Phosphatases / antagonists & inhibitors* Phosphoprotein Phosphatases / chemistry Phosphoprotein Phosphatases / isolation & purification Phosphoprotein Phosphatases / pharmacology Phosphoproteins / metabolism Phosphotyrosine / metabolism Protein Tyrosine Phosphatases / antagonists & inhibitors* Pyrans* Spiro Compounds* Streptomyces / chemistry Tumor Cells, Cultured Vanadates / pharmacology cdc25 Phosphatases|
|WOS Category||BIOPHYSICS BIOCHEMISTRY & MOLECULAR BIOLOGY CELL BIOLOGY|
|Human and Animal Cells|