Description
Protein tyrosine phosphatase 1B (PTP1B) has critical roles in cell signaling relevant to diabetes, obesity, and cancer. PTP1B inhibitor is a cell-
permeable allosteric inhibitor of PTP1B (IC
50s = 4 and 8 μM for 403 and 298 residue PTP1B forms, respectively). It binds reversibly and non-
competitively, altering the conformation of the catalytic pocket. PTP1B inhibitor selectively increases the phosphorylation of the insulin receptor, insulin receptor substrate 1, and Akt, mimicking the action of insulin.
Uses
PTP1B Inhibitor is used as a PTP1B inhibitor blocks the activity of the Protein Tyrosine Phosphatase 1B, which is a key factor in the negative regulation of insulin and leptin signaling pathway. Protein tyrosine phosphatase 1B (PTP1B) has critical roles in cell signaling relevant to diabetes, obesity, and cancer.
References
[1] SHENG ZHANG Zhong Y Z. PTP1B as a drug target: recent developments in PTP1B inhibitor discovery.[J]. Drug Discovery Today, 2007, 12 9-10: 373-381. DOI:
10.1016/j.drudis.2007.03.011[2] TONKS N K. Protein tyrosine phosphatases – from housekeeping enzymes to master regulators of signal transduction[J]. The FEBS journal, 2012, 280 2: 346-378. DOI:
10.1111/febs.12077[3] CHRISTIAN WIESMANN. Allosteric inhibition of protein tyrosine phosphatase 1B[J]. Nature Structural & Molecular Biology, 2004, 11 8: 730-737. DOI:
10.1038/nsmb803[4] SHUAI LI. The mechanism of allosteric inhibition of protein tyrosine phosphatase 1B.[J]. ACS Applied Bio Materials, 2014: e97668. DOI:
10.1371/journal.pone.0097668
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