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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Patients harboring mutations in the FLT3 receptor tyrosine kinase have a particularly poor prognosis; however, significant progress has been made by the emergence of a variety of targeted inhibitors capable of suppressing FLT3 signaling.
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.
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.