The RAF-MEK-ERK pathway: targeting ERK to overcome obstacles to effective cancer therapy
Z Yu, S Ye, G Hu, M Lv, Z Tu, K Zhou… - Future medicinal …, 2015 - Future Science
Aim: Currently, dozens of BRAF inhibitors and MEK inhibitors targeting RAF-MEK-ERK
pathway have been introduced into clinical trials for cancer therapy. However, after 6–8
months of initial response, acquired drug resistance among the majority of those treated
patients sharply diminished their clinical efficacy. Discussion: Important mechanisms
responsible for acquired resistance of BRAF inhibitors and MEK inhibitors have been
elucidated. Continually, ERK1/2 locates in the critical position and features unique …
pathway have been introduced into clinical trials for cancer therapy. However, after 6–8
months of initial response, acquired drug resistance among the majority of those treated
patients sharply diminished their clinical efficacy. Discussion: Important mechanisms
responsible for acquired resistance of BRAF inhibitors and MEK inhibitors have been
elucidated. Continually, ERK1/2 locates in the critical position and features unique …
Aim
Currently, dozens of BRAF inhibitors and MEK inhibitors targeting RAF-MEK-ERK pathway have been introduced into clinical trials for cancer therapy. However, after 6–8 months of initial response, acquired drug resistance among the majority of those treated patients sharply diminished their clinical efficacy. Discussion
Important mechanisms responsible for acquired resistance of BRAF inhibitors and MEK inhibitors have been elucidated. Continually, ERK1/2 locates in the critical position and features unique characteristics, such as activating hundreds of substrates, participating in feedback regulation, being catalyzed by MEK specifically and no acquired resistant mutation. Conclusion
Taking in account the inspiring outcomes of ERK inhibitors in preclinical research, ERK1/2 might be the optimal target to overcome acquired drug resistance in RAF-MEK-ERK pathway.
Future Science