Receptor Tyrosine Kinase Panel (ROS1, TYRO3, MERTK, KIT, NTRK2, FLT3, TEK) (RTK Panel)

This target entry represents a heterogeneous group of Receptor Tyrosine Kinases (RTKs) including ROS1, the TAM family (TYRO3, MERTK), Class III RTKs (KIT, FLT3), the neurotrophin receptor TRKB (NTRK2), and the vascular receptor TIE-2 (TEK). These proteins are cell-surface receptors that transduce extracellular signals into intracellular responses via their cytoplasmic kinase domains, regulating critical processes such as cell growth, survival, differentiation, and vascular stability (UniProt P08922, P36888, P10721). Dysregulation of these kinases—through mutations, over-expression, or chromosomal rearrangements—is a primary driver in various malignancies, including non-small cell lung cancer, acute myeloid leukemia, and gastrointestinal stromal tumors (PubMed: 29245601, 30603114). Consequently, they are major therapeutic targets for small-molecule multi-kinase inhibitors. While targeting these kinases provides significant clinical benefit, the structural similarity between their kinase domains often leads to broad-spectrum activity, which can result in off-target toxicities and the rapid emergence of resistance mutations (PubMed: 31067442).

Other names

ROS1TYRO3MERMERTKKITc-KitTRKBNTRK2FLT-3FLT3TIE-2TEKTAM receptorsClass III Receptor Tyrosine Kinases

Competitive inhibition of the adenosine triphosphate (ATP) binding site within the intracellular kinase domain, preventing autophosphorylation and downstream signaling cascades.