Assay Method Information | |
| Dose Response confirmation of uHTS hits from a small molecule inhibitors of LYP via a fluorescence intensity assay using pCAP substrate |
Description: | Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN) Grant Number: 1R21NS056945-01 Assay Provider: Dr. Nunzio Bottini, La Jolla Institute for Allergy and Immunology, La Jolla, CA LYP, is a lymphocyte specific protein tyrosine phosphatase that plays a critical regulatory role in T cell receptor signaling. The PTPN22 gene encodes this phosphatase. A single-nucleotide polymorphism in PTPN22 is associated with a number of autoimmune disorders, including type 1 diabetes, rheumatoid arthritis, juvenile rheumatoid arthritis, systemic lupus erythematosus and Grave's disease. The autoimmunity-predisposing allele is a gain-of-function mutant suggesting that a specific small-molecule inhibitor could eliminate its effect. Finding specific inhibitors of protein phosphatases has proven extremely difficult. The goal of th |
Affinity data for this assay | |
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