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Background: Receptor tyrosine kinases (RTKs) are key molecules for the recognition and transduction of external signals across the plasma membrane. RET (rearranged during transfection) is single pass transmembrane tyrosine kinase (TK) receptor that is mutated in several human cancers. The activation of wild-type RET requires the binding of a ligand and co-receptor complex and results in an autophosphorylation of intracellular tyrosine residues acting as docking sites for SH2 and PTB domain-containing proteins. Their phosphorylation trigger the activation of downstream signaling pathways, such as the Ras/MAPK/ERK1/2, PI3K/AKT, JNK, p38SAPK, STAT3, SRC, ERK5, and phospholipase Cγ pathways. Mutations of the RET extracellular domain, lead to constitutive dimerization of mutant RET and are found in multiple endocrine neoplasia type 2A (MEN2A) and familial medullary thyroid carcinoma (FMTC). In addition, chimeric rearrangements of RET, as seen in papillary thyroid carcinoma (PTC) (RET–PTC), lung adenocarcinoma or chronic myelomonocytic leukaemia, result in constitutively active cytosolic proteins.
Protein: Purified recombinant Human RET wt, C-terminal fragment, amino acids H658-S1114, expressed in Baculovirus infected Sf9 cells, N-terminal GST-HIS6 fusion protein with a 3C cleavage site
Theoretical MW: 80.44 kDa
Expression system: Baculovirus infected Sf9 cells
Purification: Affinity purification using GST-Affinity Chromatography
Storage buffer: 50 mM HEPES pH 7.5, 100 mM NaCl, 5 mM DTT, 15 mM reduced glutathione, 20% glycerol
Protein concentration: 0.31 mg/ml (Bradford method using BSA as standard protein)
Method for determination of Km value & specific activity: Filter binding assay MSPH membrane
Specific activity: 51,000 pmol/mg x min (Substrate: TRK-C-derived Peptide)
Entrez Gene ID: 5979
UniProtKB: P0794
Ordering information: shipped on dry ice
Mulligan LM (2014) “RET revisited: expanding the oncogenic portfolio.” Nat Rev Cancer 14:173–186.
Moccia M, Liu Q, Guida T, Federico G, Brescia A, Zhao Z, Choi HG, Deng X, Tan L, Wang J, Billaud M, Gray NS, Carlomagno F, Santoro M.(2015) “Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase.” PLoS One. 5;10(:e0128364)
Romei C, Ciampi R, Elisei R.(2016) “A comprehensive overview of the role of the RET proto-oncogene in thyroid carcinoma.” Nat Rev Endocrinol. 12(4):192-202.
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