BH3-mimetic drugs: blazing the trail for new cancer medicines

D Merino, GL Kelly, G Lessene, AH Wei, AW Roberts… - Cancer cell, 2018 - cell.com
Defects in apoptotic cell death can promote cancer and impair responses of malignant cells
to anti-cancer therapy. Pro-survival BCL-2 proteins prevent apoptosis by keeping the cell …

Role played by signalling pathways in overcoming BRAF inhibitor resistance in melanoma

XY Chan, A Singh, N Osman, TJ Piva - International journal of molecular …, 2017 - mdpi.com
The discovery of the BRAFV600E mutation led to the development of vemurafenib
(PLX4032), a selective BRAF inhibitor specific to the kinase, for the treatment of metastatic …

BCL-XL and MCL-1 are the key BCL-2 family proteins in melanoma cell survival

EF Lee, TJ Harris, S Tran, M Evangelista… - Cell death & …, 2019 - nature.com
Malignant melanoma is one of the most difficult cancers to treat due to its resistance to
chemotherapy. Despite recent successes with BRAF inhibitors and immune checkpoint …

Bcl-2 family inhibitors sensitize human cancer models to therapy

E Valentini, M Di Martile, M Brignone, M Di Caprio… - Cell Death & …, 2023 - nature.com
BH3 mimetics, targeting the Bcl-2 family anti-apoptotic proteins, represent a promising
therapeutic opportunity in cancers. ABT-199, the first specific Bcl-2 inhibitor, was approved …

Non-apoptotic cell death signaling pathways in melanoma

ML Hartman - International journal of molecular sciences, 2020 - mdpi.com
Resisting cell death is a hallmark of cancer. Disturbances in the execution of cell death
programs promote carcinogenesis and survival of cancer cells under unfavorable …

Hgf/Met activation mediates resistance to BRAF inhibition in murine anaplastic thyroid cancers

JA Knauf, KA Luckett, KY Chen, F Voza… - The Journal of …, 2018 - Am Soc Clin Investig
Anaplastic thyroid carcinomas (ATCs) have a high prevalence of BRAF and TP53 mutations.
A trial of vemurafenib in nonmelanoma BRAFV600E-mutant cancers showed significant …

Countering TRAIL resistance in melanoma

J Eberle - Cancers, 2019 - mdpi.com
Melanoma of the skin has become a prime example for demonstrating the success of
targeted cancer therapy. Nevertheless, high mortality has remained, mainly related to tumor …

New insights into the roles of antiapoptotic members of the Bcl-2 family in melanoma progression and therapy

D Trisciuoglio, D Del Bufalo - Drug discovery today, 2021 - Elsevier
Highlights•The Bcl‐2 family proteins are mainly involved in the control of intrinsic apoptotic
pathway•The pro-survival members of Bcl‐2 family are over-expressed in melanoma.•Bcl‐2 …

Targeting the BCL-2-regulated apoptotic pathway for the treatment of solid cancers

WD Fairlie, EF Lee - Biochemical Society Transactions, 2021 - portlandpress.com
The deregulation of apoptosis is a key contributor to tumourigenesis as it can lead to the
unwanted survival of rogue cells. Drugs known as the BH3-mimetics targeting the pro …

BCL-XL inhibitors enhance the apoptotic efficacy of BRAF inhibitors in BRAFV600E colorectal cancer

LJ Jenkins, IY Luk, F Chionh, T Tan, K Needham… - Cell Death & …, 2024 - nature.com
Abstract Metastatic BRAF V600E colorectal cancer (CRC) carries an extremely poor
prognosis and is in urgent need of effective new treatments. While the BRAFV600E inhibitor …