BCL-2 family proteins: changing partners in the dance towards death

J Kale, EJ Osterlund, DW Andrews - Cell Death & Differentiation, 2018 - nature.com
The BCL-2 family of proteins controls cell death primarily by direct binding interactions that
regulate mitochondrial outer membrane permeabilization (MOMP) leading to the irreversible …

Indole: A privileged scaffold for the design of anti-cancer agents

Y Wan, Y Li, C Yan, M Yan, Z Tang - European journal of medicinal …, 2019 - Elsevier
In general, heterocyclic compounds are a significant source of pharmacologically active
compounds. Among them, the indole scaffold widely distributes in natural products and …

Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia

AE Tron, MA Belmonte, A Adam, BM Aquila… - Nature …, 2018 - nature.com
Mcl-1 is a member of the Bcl-2 family of proteins that promotes cell survival by preventing
induction of apoptosis in many cancers. High expression of Mcl-1 causes tumorigenesis and …

From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors

A Ashkenazi, WJ Fairbrother, JD Leverson… - Nature reviews drug …, 2017 - nature.com
Members of the B cell lymphoma 2 (BCL-2) gene family have a central role in regulating
programmed cell death by controlling pro-apoptotic and anti-apoptotic intracellular signals …

The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models

A Kotschy, Z Szlavik, J Murray, J Davidson… - Nature, 2016 - nature.com
Avoidance of apoptosis is critical for the development and sustained growth of tumours. The
pro-survival protein myeloid cell leukemia 1 (MCL1) is overexpressed in many cancers, but …

The BCL-2 arbiters of apoptosis and their growing role as cancer targets

JM Adams, S Cory - Cell Death & Differentiation, 2018 - nature.com
Impaired apoptosis plays a central role in cancer development and limits the efficacy of
conventional cytotoxic therapies. Deepening understanding of how opposing factions of the …

Therapeutic strategies to overcome taxane resistance in cancer

T Das, U Anand, SK Pandey, CR Ashby Jr… - Drug Resistance …, 2021 - Elsevier
One of the primary causes of attenuated or loss of efficacy of cancer chemotherapy is the
emergence of multidrug resistance (MDR). Numerous studies have been published …

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 …

The BCL2 family: key mediators of the apoptotic response to targeted anticancer therapeutics

AN Hata, JA Engelman, AC Faber - Cancer discovery, 2015 - AACR
The ability of cancer cells to suppress apoptosis is critical for carcinogenesis. The BCL2
family proteins comprise the sentinel network that regulates the mitochondrial or intrinsic …

Why do BCL-2 inhibitors work and where should we use them in the clinic?

J Montero, A Letai - Cell Death & Differentiation, 2018 - nature.com
Intrinsic apoptosis is controlled by the BCL-2 family of proteins but the complexity of intra-
family interactions makes it challenging to predict cell fate via standard molecular biology …