Physiological and pharmacological modulation of BAX

AZ Spitz, E Gavathiotis - Trends in pharmacological sciences, 2022 - cell.com
Bcl-2-associated X protein (BAX) is a critical executioner of mitochondrial regulated cell
death through its lethal activity of permeabilizing the mitochondrial outer membrane (MOM) …

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 …

Structures of p53/BCL-2 complex suggest a mechanism for p53 to antagonize BCL-2 activity

H Wei, H Wang, G Wang, L Qu, L Jiang, S Dai… - Nature …, 2023 - nature.com
Mitochondrial apoptosis is strictly controlled by BCL-2 family proteins through a subtle
network of protein interactions. The tumor suppressor protein p53 triggers transcription …

Acquisition of the recurrent Gly101Val mutation in BCL2 confers resistance to venetoclax in patients with progressive chronic lymphocytic leukemia

P Blombery, MA Anderson, J Gong, R Thijssen… - Cancer discovery, 2019 - AACR
The BCL2 inhibitor venetoclax induces high rates of durable remission in patients with
previously treated chronic lymphocytic leukemia (CLL). However, despite continuous daily …

Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

DE Scott, AR Bayly, C Abell, J Skidmore - Nature Reviews Drug …, 2016 - nature.com
Protein–protein interactions (PPIs) are of pivotal importance in the regulation of biological
systems and are consequently implicated in the development of disease states. Recent work …

Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy

PE Czabotar, G Lessene, A Strasser… - Nature reviews Molecular …, 2014 - nature.com
The BCL-2 protein family determines the commitment of cells to apoptosis, an ancient cell
suicide programme that is essential for development, tissue homeostasis and immunity. Too …

Mitochondrial PKM2 regulates oxidative stress-induced apoptosis by stabilizing Bcl2

J Liang, R Cao, X Wang, Y Zhang, P Wang, H Gao, C Li… - Cell research, 2017 - nature.com
Pyruvate kinase M2 isoform (PKM2) catalyzes the last step of glycolysis and plays an
important role in tumor cell proliferation. Recent studies have reported that PKM2 also …

Many players in BCL-2 family affairs

T Moldoveanu, AV Follis, RW Kriwacki… - Trends in biochemical …, 2014 - cell.com
During apoptotic cell death, cellular stress signals converge at the mitochondria to induce
mitochondrial outer-membrane permeabilization (MOMP) through B cell lymphoma-2 (BCL …

Structures of BCL-2 in complex with venetoclax reveal the molecular basis of resistance mutations

RW Birkinshaw, J Gong, CS Luo, D Lio… - Nature …, 2019 - nature.com
Venetoclax is a first-in-class cancer therapy that interacts with the cellular apoptotic
machinery promoting apoptosis. Treatment of patients suffering chronic lymphocytic …

A unified model of mammalian BCL-2 protein family interactions at the mitochondria

F Llambi, T Moldoveanu, SWG Tait, L Bouchier-Hayes… - Molecular cell, 2011 - cell.com
During apoptosis, the BCL-2 protein family controls mitochondrial outer membrane
permeabilization (MOMP), but the dynamics of this regulation remain controversial. We …