The structure of protein tyrosine phosphatase-1B complexed to a high affinity inhibitor
نویسندگان
چکیده
منابع مشابه
Protein Tyrosine Phosphatase 1B Inhibitors: Catechols
As most intracellular signaling takes place via cascades of phosphorylation and dephosphorylation of tyrosines, protein tyrosine phosphatases have emerged as new and promising targets. Among them, protein tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling by dephosphorylation of key tyrosine residues within the regulatory domain of the β-subunit of the insulin receptor, ther...
متن کاملAsperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B
In the frame of studies on secondary metabolites produced by fungi from deep-sea environments we have investigated inhibitors of enzymes playing key roles in signaling cascades of biochemical pathways relevant for the treatment of diseases. Here we report on a new inhibitor of the human protein tyrosine phosphatase 1B (PTP1B), a target in the signaling pathway of insulin. A new asperentin analo...
متن کاملStearic acid serves as a potent inhibitor of protein tyrosine phosphatase 1B.
BACKGROUND/AIMS Free fatty acids (FFAs) are implicated in diverse signal transduction pathways. The present study investigated the effects of the saturated FFA stearic acid on protein tyrosine phosphatase 1B (PTP1B) activity, Akt activity, and glucose uptake into cells relevant to insulin signal. METHODS PTP1B activity was assayed under the cell-free conditions. Phosphorylation of insulin rec...
متن کاملThe Mechanism of Allosteric Inhibition of Protein Tyrosine Phosphatase 1B
As the prototypical member of the PTP family, protein tyrosine phosphatase 1B (PTP1B) is an attractive target for therapeutic interventions in type 2 diabetes. The extremely conserved catalytic site of PTP1B renders the design of selective PTP1B inhibitors intractable. Although discovered allosteric inhibitors containing a benzofuran sulfonamide scaffold offer fascinating opportunities to overc...
متن کاملDominant role of the protein-tyrosine phosphatase CD148 in regulating platelet activation relative to protein-tyrosine phosphatase-1B.
OBJECTIVE The receptor-like protein-tyrosine phosphatase (PTP) CD148 and the nontransmembrane PTP1-B have been shown to be net positive regulators of Src family kinases in platelets. In the present study, we compared the relative contributions of these PTPs in platelet activation by the major glycoprotein, glycoprotein VI, α(IIb)β(3), and C-type lectin-like receptor 2 (CLEC-2). METHODS AND RE...
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ژورنال
عنوان ژورنال: Acta Crystallographica Section A Foundations of Crystallography
سال: 1996
ISSN: 0108-7673
DOI: 10.1107/s0108767396091763