3zv2 | pdb_00003zv2

HUMAN PROTEIN-TYROSINE PHOSPHATASE 1B C215A, S216A MUTANT

spinqualitylabelsall models 3zv2, resolution 2.80Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3zv2 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Related: 2f6t, 2f6f, 2cnf, 2cm3, 1g1f, 2cm2, 1q6n, 1ptu, 1c84, 2veu, 1nz7, 1q1m, 2azr, 1c88, 1oet, 1c83, 1sug, 1onz, 1g1g, 1xbo, 1ptv, 2cnh, 2hnp, 1nwl, 1t49, 2f6y, 2cne, 1nl9, 1c86, 1kav, 2hnq, 1jf7, 1pxh, 1q6s, 1l8g, 2cma, 1q6m, 1bzj, 1i57, 1wax, 1ony, 1g1h, 1kak, 2cng, 1t4j, 2cni, 2b07, 2cm8, 1eeo, 1g7g, 1ptt, 1qxk, 1ecv, 1oem, 1nwe, 2cmb, 2fjn, 1aax, 2vev, 2vey, 2b4s, 2cm7, 2bgd, 1a5y, 2vex, 1c85, 2cmc, 2vew, 1lqf, 2f6w, 1c87, 1no6, 1pyn, 2bge, 1oes, 1bzc, 2f6z, 2f71, 1oeu, 1q6t, 1g7f, 1nny, 1q6j, 2f70, 1q6p, 2f6v, 1t48, 1oeo, 2fjm, 1pa1, 1ph0, 1bzh, 1gfy, 1een, 1pty, 1oev Activity: Protein-tyrosine-phosphatase, with EC number 3.1.3.48 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [PTN1_HUMAN] Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response. Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion. Publication Abstract from PubMed Protein tyrosine phosphatase 1B (PTP1B) plays important roles in downregulation of insulin and leptin signaling and is an established therapeutic target for diabetes and obesity. PTP1B is regulated by reactive oxygen species (ROS) produced in response to various stimuli, including insulin. The reversibly oxidized form of the enzyme (PTP1B-OX) is inactive and undergoes profound conformational changes at the active site. We generated conformation-sensor antibodies, in the form of single-chain variable fragments (scFvs), that stabilize PTP1B-OX and thereby inhibit its phosphatase function. Expression of conformation-sensor scFvs as intracellular antibodies (intrabodies) enhanced insulin-induced tyrosyl phosphorylation of the beta subunit of the insulin receptor and its substrate IRS-1 and increased insulin-induced phosphorylation of PKB/AKT. Our data suggest that stabilization of the oxidized, inactive form of PTP1B with appropriate therapeutic molecules may offer a paradigm for phosphatase drug development. Conformation-Sensing Antibodies Stabilize the Oxidized Form of PTP1B and Inhibit Its Phosphatase Activity.,Haque A, Andersen JN, Salmeen A, Barford D, Tonks NK Cell. 2011 Sep 30;147(1):185-98. PMID:21962515 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Tyrosine phosphatase

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