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Application: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: RET (rearranged during transfection) is a receptor tyrosine kinase for GDNF (glial cell-line derived neurotrophic factor) family ligands (GFLs), and has three isoforms, with RET51 and RET9 being the most common. For activation of RET to occur, GFLs first form a complex with a GPI (glycosylphosphatidylinositol)-anchored co-receptor, and this complex recruit two molecules of RET, which can undergo autophosphorylation, and activate RAS/MAPK (mitogen-activated protein kinase) and PI3K (phosphoinositide 3-kinase)/AKT signaling pathways. This protein is involved in kidney development, cellular proliferation, differentiation, and survival. Hereditary mutations that result in an inactive protein can lead to Hirschsprung disease, hypoventilation syndrome and malformation of the kidney and urinary tract, while activating mutations result in MEN2 syndrome (multiple endocrine neoplasia type 2). It has been shown that activating mutations or chromosome rearrangements that lead to constitutively active protein play a significant role in various cancer types, such as PTC (papillary thyroid carcinoma). In 2020, the small molecule inhibitor selpercatinib was approved for the treatment of NSCLC (non-small cell lung cancer) and thyroid cancer, however solvent front mutations (SFMs) have resulted in resistance to treatment. A deeper understanding of the roles of this protein, impact of mutations, and the development of new drugs, will improve outcomes for patients suffering from RET-related disorders.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ RET Kinase Assay Kit is designed to measure RET (rearranged during transfection) tyrosine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified RET (amino acids 658-end), kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: P07949
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Mulligan L. M., 2014 Nature Reviews Cancer 14:173-186.
Vodopivec D. and Hu M., 2022 Ther Adv Med Oncol. 14:17588359221101691.
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