Proto-oncogene tyrosine-protein kinase FGR (FGR) (FGR)

Proto-oncogene tyrosine-protein kinase FGR is a non-receptor tyrosine kinase belonging to the Src family, predominantly expressed in hematopoietic cells of the myeloid lineage, including neutrophils, monocytes, and macrophages [1, 4]. It serves as a key mediator in signal transduction pathways downstream of various cell surface receptors, such as integrins and Fc receptors, regulating essential cellular processes like adhesion, migration, phagocytosis, and degranulation [1, 22]. In oncology, FGR is recognized as a significant therapeutic target in acute myeloid leukemia (AML), where its overexpression drives leukemic cell growth and survival, often serving as a bypass mechanism for FLT3 inhibitor resistance [8, 15]. Additionally, FGR is involved in the pathogenesis of inflammatory and fibrotic diseases, including radiation-induced pulmonary fibrosis and atherosclerosis, by modulating macrophage activation and cytokine production [10, 14]. Small-molecule inhibitors targeting FGR, such as the selective lead compound TL02-59, are being explored for their potential to treat hematologic malignancies and chronic inflammatory conditions [8, 24].

Other names

SRC2c-fgrc-src2p55-Fgrp55c-fgrp58-Fgrp58c-fgrGardner-Rasheed feline sarcoma viral (v-fgr) oncogene homologTyrosine-protein kinase Fgr

Tyrosine kinase inhibitor