Increased Synthesis of MCL-1 Protein Underlies Initial Survival of EGFR-Mutant Lung Cancer to EGFR Inhibitors and Provides a Novel Drug Target

KA Song, Y Hosono, C Turner, S Jacob… - Clinical Cancer …, 2018 - AACR
… Importantly, MCL-1 can be targeted pharmaceutically to improve responses. This study
supports the use of MCL-1 inhibitors in combination with EGFR inhibitors to eliminate EGFR-…

Overcoming acquired resistance to third-generation EGFR inhibitors by targeting activation of intrinsic apoptotic pathway through Mcl-1 inhibition, Bax activation, or …

G Ma, Y Deng, L Qian, KA Vallega, G Zhang, X Deng… - Oncogene, 2022 - nature.com
… of EGFR, accompanied with Mcl-1 reduction in … direct inhibition of Mcl-1 with an Mcl-1 inhibitor
in combination with osimertinib exerts enhanced effect on decreasing the survival of EGFR

Overcoming acquired resistance to AZD9291, a third-generation EGFR inhibitor, through modulation of MEK/ERK-dependent Bim and Mcl-1 degradation

P Shi, YT Oh, L Deng, G Zhang, G Qian, S Zhang… - Clinical Cancer …, 2017 - AACR
… induced apoptosis in EGFR-mutant … Mcl-1 reduction likely due to enhanced Mcl-1 degradation
and increased Bim stability. Blocking Bim elevation by gene knockdown or enforcing Mcl-1

… inhibition sensitizes non–small cell lung cancer with T790M mutation to irreversible EGFR inhibitors via translational suppression of mcl-1 by AMPK activation

SM Kim, MR Yun, YK Hong, F Solca, JH Kim… - Molecular cancer …, 2013 - AACR
… to irreversible EGFR-TKIs linking glucose metabolism to Mcl-1inhibitor of glucose
metabolism with irreversible EGFR-TKIs in the treatment of NSCLCs with secondary EGFR

EGFR signaling defines Mcl-1 survival dependency in neuroblastoma

S Nalluri, SK Peirce, R Tanos, HA Abdella… - Cancer Biology & …, 2015 - Taylor & Francis
… To that end, we now demonstrate that EGFR regulates Bim:Mcl - 1 interactions to promote
Mcl - 1 dependence in HR NBs and that successful small molecule inhibition of EGFR or its …

Mcl-1 regulates survival and sensitivity to diverse apoptotic stimuli in human non-small cell lung cancer cells

L Song, D Coppola, S Livingston, WD Cress… - Cancer biology & …, 2005 - Taylor & Francis
Mcl-1 levels.As shown in Figure 6A, inhibition of EGFR has no effect on expression of Mcl-1
effect of these EGFR inhibitors on constitutive Stat3 activity and apoptosis in these cells.…

[HTML][HTML] Formononetin inhibits tumor growth by suppression of EGFR-Akt-Mcl-1 axis in non-small cell lung cancer

X Yu, F Gao, W Li, L Zhou, W Liu, M Li - Journal of Experimental & Clinical …, 2020 - Springer
… Overall, this study demonstrated that Formo acts as an inhibitor for the EGFR-Akt axis, and
promotes FBW7-mediated Mcl-1 ubiquitination is required for the anti-tumor activity of Formo …

Notch1 signaling promotes survival of glioblastoma cells via EGFR-mediated induction of anti-apoptotic Mcl-1

A Fassl, KE Tagscherer, J Richter, M Berriel Diaz… - Oncogene, 2012 - nature.com
… involvement of EGFR signaling in the Notch1-dependent regulation of Mcl-1, we transiently
overexpressed EGFR after Notch1 knockdown. As expected, this rescued the Mcl-1 protein …

Tyrosine kinase inhibitors increase MCL1 degradation and in combination with BCLXL/BCL2 inhibitors drive prostate cancer apoptosis

S Arai, O Jonas, MA Whitman, E Corey, SP Balk… - Clinical Cancer …, 2018 - AACR
… To identify additional ubiquitin ligases or deubiquitinases (DUB) that may regulate MCL1
degradation in response to EGFR inhibition, we carried out large-scale immunopurifications of …

[HTML][HTML] MCL-1 inhibitors, fast-lane development of a new class of anti-cancer agents

A Bolomsky, M Vogler, MC Köse, CA Heckman… - Journal of hematology & …, 2020 - Springer
… or tertiary EGFR mutations and other mechanisms [52]. After exposure to EGFR inhibitors,
EGFR-… of MCL-1 and finally become “drug-tolerant cells.” This overexpression is explained by (…