Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.3.16 (calcineurin)
 17,112 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Suramin has long been used for the treatment of Gambian and Rhodesian trypanosomiasis and oncocerciasis. More recently, the demonstration that suramin inhibits DNA polymerases, reverse transcriptase and the lymphocyte terminal deoxynucleotidyl transferase has led to its clinical trials for the treatment of AIDS and cancer. The precise nature of suramin's anti-neoplastic action is not clear at this time. Suramin rapidly alters the tyrosine-specific phosphorylation of cellular proteins in many cancer cell lines. Here we demonstrate that suramin strongly inhibits the activity of CD45, the principal tyrosine specific protein phosphatase of T lymphocytes. Suramin-induced inactivation of CD45 is noncompetitive, irreversible and complete within 10 min. The ability of suramin to block CD45 mediated phosphatase function provides both new insight into the mechanism of action of this agent and a useful new probe for studies of T cell activation.
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PMID:Suramin, an experimental chemotherapeutic drug, irreversibly blocks T cell CD45-protein tyrosine phosphatase in vitro. 833 52