Flavonoids as receptor tyrosine kinase FLT3 inhibitors

Young-Won Chin; Jae Yang Kong; Sun-Young Han

doi:10.1016/j.bmcl.2013.01.049

Flavonoids as receptor tyrosine kinase FLT3 inhibitors

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1768-70. doi: 10.1016/j.bmcl.2013.01.049. Epub 2013 Jan 26.

Authors

Young-Won Chin¹, Jae Yang Kong, Sun-Young Han

Affiliation

¹ College of Pharmacy, Dongguk University-Seoul, Goyang, Gyeonggi-do 410-820, South Korea.

PMID: 23411073
DOI: 10.1016/j.bmcl.2013.01.049

Abstract

The Fms-like tyrosine kinase 3 (FLT3), a receptor tyrosine kinase, is involved in the proliferation, differentiation and apoptosis of hematopoietic cells. FLT3 is highly overexpressed in acute myeloid leukemia (AML) of the majority of patients. Screening for flavonoids including flavones, flavanones, flavonols, and flavanonols disclosed that luteolin was potent FLT3 enzyme inhibitor. Furthermore, luteolin suppressed cell proliferation in MV4;11 cells with constitutively activated FLT3.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cell Cycle Checkpoints / drug effects
Cell Line, Tumor
Cell Proliferation / drug effects
Flavonoids / chemistry*
Flavonoids / toxicity
Humans
Luteolin / chemistry
Luteolin / toxicity
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / toxicity
fms-Like Tyrosine Kinase 3 / antagonists & inhibitors*
fms-Like Tyrosine Kinase 3 / metabolism

Substances

Flavonoids
Protein Kinase Inhibitors
FLT3 protein, human
fms-Like Tyrosine Kinase 3
Luteolin