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.
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.
Authors: Trish T Hoang; I Caglar Tanrikulu; Quinn A Vatland; Trieu M Hoang; Ronald T Raines Journal: Mol Cancer Ther Date: 2018-10-03 Impact factor: 6.261
Authors: Rui Liu; Jun-Chun Tang; Meng-Xian Pan; Yang Zhuang; Ya Zhang; Hua-Bao Liao; Dan Zhao; Yang Lei; Rui-Xue Lei; Shu Wang; An-Chun Liu; Xing-Ping Qin; Juan Chen; Zhi-Feng Zhang; Qi Wan Journal: Neurochem Res Date: 2018-06-07 Impact factor: 3.996