Selective ERK1/2 agonists isolated from Melia azedarach with potent anti-leukemic activity.

ABSTRACT:

Background

MAPK/ERK kinases transmit signals from many growth factors/kinase receptors during normal cell growth/differentiation, and their dysregulation is a hallmark of diverse types of cancers. A plethora of drugs were developed to block this kinase pathway for clinical application. With the exception of a recently identified agent, EQW, most of these inhibitors target upstream factors but not ERK1/2; no activator of ERK1/2 is currently available.

Method

A library of compounds isolated from medicinal plants of China was screened for anti-cancer activities. Three limonoid compounds, termed A1541-43, originally isolated from the plant Melia azedarach, exhibiting strong anti-leukemic activity. The anti-neoplastic activity and the biological target of these compounds were exp

SUBMITTER: Wang N 

PROVIDER: S-EPMC6679490 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature