The BCL-2 inhibitor ABT-199/venetoclax synergizes with proteasome inhibition via transactivation of the MCL-1 antagonist NOXA

S Weller, A Toennießen, B Schaefer, T Beigl… - Cell death …, 2022 - nature.com
Enhanced expression of anti-apoptotic B-cell lymphoma 2 (BCL-2) protein is frequent in
cancer. Targeting of BCL-2 with the specific inhibitor ABT-199 (Venetoclax) has significant …

Targeting BCL-2-like proteins to kill cancer cells

S Cory, AW Roberts, PM Colman, JM Adams - Trends in cancer, 2016 - cell.com
Mutations that impair apoptosis contribute to cancer development and reduce the
effectiveness of conventional anti-cancer therapies. These insights and understanding of …

ABT-199 (venetoclax) and BCL-2 inhibitors in clinical development

S Cang, C Iragavarapu, J Savooji, Y Song… - Journal of hematology & …, 2015 - Springer
With the advent of new agents targeting CD20, Bruton's tyrosine kinase, and
phosphoinositol-3 kinase for chronic lymphoid leukemia (CLL), more treatment options exist …

BDA-366, a putative Bcl-2 BH4 domain antagonist, induces apoptosis independently of Bcl-2 in a variety of cancer cell models

T Vervloessem, BK Sasi, E Xerxa, S Karamanou… - Cell Death & …, 2020 - nature.com
Several cancer cell types, including chronic lymphocytic leukemia (CLL) and diffuse large B-
cell lymphoma (DLBCL) upregulate antiapoptotic Bcl-2 to cope with oncogenic stress. BH3 …

[HTML][HTML] From mitochondrial biology to magic bullet: navitoclax disarms BCL-2 in chronic lymphocytic leukemia

LD Walensky - Journal of clinical oncology: official journal of the …, 2012 - ncbi.nlm.nih.gov
Navitoclax is a selective small-molecule B-cell lymphoma 2 (BCL-2)/BCL-XL inhibitor that
represents both the fruition of nearly three decades of BCL-2 protein research and the …

Targeting BCL2 with BH3 mimetics: basic science and clinical application of venetoclax in chronic lymphocytic leukemia and related B cell malignancies

AW Roberts, DCS Huang - Clinical Pharmacology & …, 2017 - Wiley Online Library
The intracellular protein B‐cell‐lymphoma‐2 (BCL2) has been considered an attractive
target for cancer therapy since the discovery of its function as a major promoter of cell …

Bcl-2, Bcl-xL, and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells

D Mérino, SL Khaw, SP Glaser… - Blood, The Journal …, 2012 - ashpublications.org
Abstract The BH3-mimetic ABT-737 and an orally bioavailable compound of the same class,
navitoclax (ABT-263), have shown promising antitumor efficacy in preclinical and early …

Targeting BCL-2 in cancer: advances, challenges, and perspectives

S Hafezi, M Rahmani - Cancers, 2021 - mdpi.com
Simple Summary Apoptosis, a programmed form of cell death, represents the main
mechanism by which cells die. Such phenomenon is highly regulated by the BCL-2 family of …

Combining BH3-mimetics to target both BCL-2 and MCL1 has potent activity in pre-clinical models of acute myeloid leukemia

DM Moujalled, G Pomilio, C Ghiurau, A Ivey, J Salmon… - Leukemia, 2019 - nature.com
Improving outcomes in acute myeloid leukemia (AML) remains a major clinical challenge.
Overexpression of pro-survival BCL-2 family members rendering transformed cells resistant …

Synergistic activity of combined inhibition of anti-apoptotic molecules in B-cell precursor ALL

F Seyfried, FU Stirnweiß, A Niedermayer… - Leukemia, 2022 - nature.com
Targeting BCL-2, a key regulator of survival in B-cell malignancies including precursor B-cell
acute lymphoblastic leukemia, has become a promising treatment strategy. However, given …