Thyrsiferyl 23-acetate is a novel specific inhibitor of protein phosphatase PP2A.
Thyrsiferyl 23-acetate (TF23A), a cytotoxic compound from marine red alga, has been shown to potently and specifically inhibit serine/threonine protein phosphatase 2A (PP2A) with IC50 values of 4-16 microM, depending on the enzyme concentration. TF23A did not affect activity of protein phosphatase 1 (PP1), 2B (PP2B), 2C (PP2C), or protein tyrosine phosphatases (PTP) up to 1 mM. It inhibited PP2A activity in a crude extract of a human T cell line, Jurkat cell, as well as the purified catalytic subunit. Thus, TF23A proved to be a novel useful probe for clearly distinguishing the activity of PP2A from those of the other protein phosphatases in crude cell extracts and identification of cellular processes that are regulated by PP2A.
Matsuzawa
S
S
Section of Biochemistry, Institute of Immunological Science, Hokkaido University, Sapporo, Japan.
Suzuki
T
T
Suzuki
M
M
Matsuda
A
A
Kawamura
T
T
Mizuno
Y
Y
Kikuchi
K
K
D002460:Cell Line; D004988:Ethers, Cyclic / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D046911:Macromolecular Substances; D015394:Molecular Structure; D019319:Okadaic Acid; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D054645:Protein Phosphatase 1; D054648:Protein Phosphatase 2; D011714:Pyrans / Q000737:chemistry / Q000494:pharmacology*; D000461:Rhodophyta; D012969:Sodium Fluoride / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D004988:Ethers, Cyclic; D046911:Macromolecular Substances; D011714:Pyrans; D019319:Okadaic Acid; D012969:Sodium Fluoride; C091148:thyrsiferyl 23-acetate; D010749:Phosphoprotein Phosphatases; D054645:Protein Phosphatase 1; D054648:Protein Phosphatase 2