Frontiers | MEK inhibitors: a promising targeted therapy for cardiovascular disease
www.frontiersin.org
So far, MEKI have also shown better tolerance and success than ERK1/2 inhibitors (ERKI) in clinical trials on cancer patients. n these patients, ERKI showed scarce efficacy and quick development of drug resistance due to the compensatory activation of other functionally redundant members of the larg
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- So far, MEKI have also shown better tolerance and success than ERK1/2 inhibitors (ERKI) in clinical trials on cancer patients.
- n these patients, ERKI showed scarce efficacy and quick development of drug resistance due to the compensatory activation of other functionally redundant members of the large MAPK family (like ERK5) after the inhibition of ERK1/2
- Compared with the first generation of MEKI, the new-generation MEKI are highly selective and bind to a site near the adenosine triphosphate (ATP)-binding pocket uniquely present on MEK proteins, thus avoiding off-target effects on other kinases.
- Another reason for the short-duration efficacy of ERKI is their mechanism of action. Since most ERKI are ATP-competitive and must compete with ATP for binding to ERK, the concentration of ERKI within the cells should ideally be superior to that of ATP for optimal effect.
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