Dephostatin, a novel protein tyrosine phosphatase inhibitor produced by Streptomyces. I. Taxonomy, isolation, and characterization.
A novel inhibitor of protein tyrosine phosphatase, dephostatin, was isolated from the culture broth of a strain of Streptomyces. The active principle was extracted from the broth filtrate with ethyl acetate and purified by silica gel chromatography and by HPLC. Dephostatin inhibited protein tyrosine phosphatase prepared from a human neoplastic T-cell line with an IC50 at 7.7 microM. The inhibitory pattern of dephostatin was competitive against the substrate. Dephostatin inhibited the growth of Jurkat cells.
Imoto
M
M
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, Yokohama, Japan.
Kakeya
H
H
Sawa
T
T
Hayashi
C
C
Hamada
M
M
Takeuchi
T
T
Umezawa
K
K
D002455:Cell Division / Q000187:drug effects; D002478:Cells, Cultured; D005285:Fermentation; D006801:Humans; D006873:Hydroquinones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D013302:Streptomyces / Q000737:chemistry* / Q000145:classification / Q000254:growth & development / Q000648:ultrastructure; D013601:T-Lymphocytes / Q000201:enzymology; D014407:Tumor Cells, Cultured
D006873:Hydroquinones; C084037:dephostatin; D017027:Protein Tyrosine Phosphatases