FLT3

(redirected from FLT3 receptor tyrosine kinase)

FLT3

A gene on chromosome 13q12 that encodes a class-III receptor tyrosine kinase, which regulates haematopoiesis. FLT3 is activated by binding the fms-related tyrosine kinase 3 ligand to the extracellular domain, which induces homodimer formation in the plasma membrane leading to autophosphorylation of the receptor. The activated receptor kinase in turn phosphorylates and activates multiple cytoplasmic effectors involved in apoptosis, proliferation and differentiation of haematopoietic cells in bone marrow.

Molecular pathology
FLT3 mutations that activate the receptor are thought to induce acute (myeloid or lymphocytic) leukaemia.
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The open-label, dose-escalation study, "AC220, a Potent, Selective, Second Generation FLT3 Receptor Tyrosine Kinase Inhibitor, in a First-in-Human Phase I AML Study," was designed to evaluate the safety, tolerability, and pharmacokinetic profile of AC220 in AML patients with predominantly relapsed or refractory disease.
In this collection of 11 articles, contributors describe their work in PTKs in such areas as using PTKs as targets for cancer and other indications, targeting Src homology 2 domains in drug discovery, using P12-kinase inhibition as a target for therapeutic intervention, using an activated FLT3 receptor tyrosine kinase as a therapeutic target in leukemia and JAK kinases in leukemia, lymphomas and multiple myeloma, applying platelet-derived growth factor, using a targeted therapy for myelogenous leukemia, testing signal transduction inhibitors in animal models of cancer, and using phosphoproteomics in drug discovery and development.
Symadex (formerly C-1311) is the lead compound from a new series of agents, the imidazoacridinones, which have been shown to be potent and selective FLT3 receptor tyrosine kinase inhibitors in vitro.
Researchers from Xanthus and the Medical University of South Carolina, Charleston, previously identified Symadex as a potent and selective inhibitor of the FLT3 receptor tyrosine kinase, in addition to its topoisomerase II activity.