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  • Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo.

Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo.

Nature medicine (1999-07-08)
J S Sebolt-Leopold, D T Dudley, R Herrera, K Van Becelaere, A Wiland, R C Gowan, H Tecle, S D Barrett, A Bridges, S Przybranowski, W R Leopold, A R Saltiel
ABSTRACT

The mitogen-activated protein kinase pathway is thought to be essential in cellular growth and differentiation. Here we report the discovery of a highly potent and selective inhibitor of the upstream kinase MEK that is orally active. Tumor growth was inhibited as much as 80% in mice with colon carcinomas of both mouse and human origin after treatment with this inhibitor. Efficacy was achieved with a wide range of doses with no signs of toxicity, and correlated with a reduction in the levels of activated mitogen-activated protein kinase in excised tumors. These data indicate that MEK inhibitors represent a promising, noncytotoxic approach to the clinical management of colon cancer.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
MEK1, active, GST tagged human, PRECISIO® Kinase, recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution