Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia

S Peirs, V Frismantas, F Matthijssens, W Van Loocke… - Leukemia, 2017 - nature.com
Inhibition of anti-apoptotic BCL-2 (B-cell lymphoma 2) has recently emerged as a promising
new therapeutic strategy for the treatment of a variety of human cancers, including leukemia …

Reprogramming cell death: BCL2 family inhibition in hematological malignancies

L Scarfo, P Ghia - Immunology letters, 2013 - Elsevier
The BCL2 family members play a central role in regulating programmed cell death
(apoptosis) and arbitrating the cellular fate through an accurate balance between pro …

Patent landscape of inhibitors and PROTACs of the anti-apoptotic BCL-2 family proteins

P Pal, P Zhang, SK Poddar, G Zheng - Expert opinion on …, 2022 - Taylor & Francis
Introduction The anti-apoptotic BCL-2 family proteins, such as BCL-2, BCL-XL, and MCL-1,
are excellent cancer therapeutic targets. The FDA approval of BCL-2 selective inhibitor …

The Bcl-2 specific BH3 mimetic ABT-199: a promising targeted therapy for t (11; 14) multiple myeloma

C Touzeau, C Dousset, S Le Gouill, D Sampath… - Leukemia, 2014 - nature.com
Despite recent advances in the treatment of multiple myeloma (MM), including proteasome
inhibitors and immunomodulatory agents, patients invariably relapse and alternative …

Inhibition of anti-apoptotic Bcl-2 proteins in preclinical and clinical studies: current overview in cancer

S D'Aguanno, D Del Bufalo - Cells, 2020 - mdpi.com
The dynamic interplay between pro-death and pro-survival Bcl-2 family proteins is
responsible for a cell's fate. Due to the recognized relevance of this family in cancer …

Development of a novel B-cell lymphoma 6 (BCL6) PROTAC to provide insight into small molecule targeting of BCL6

W McCoull, T Cheung, E Anderson, P Barton… - ACS Chemical …, 2018 - ACS Publications
B-cell lymphoma 6 (BCL6) inhibition is a promising mechanism for treating hematological
cancers but high quality chemical probes are necessary to evaluate its therapeutic potential …

[HTML][HTML] Inhibition of CHK1 enhances cell death induced by the Bcl-2-selective inhibitor ABT-199 in acute myeloid leukemia cells

J Zhao, X Niu, X Li, H Edwards, G Wang, Y Wang… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Resistance to standard chemotherapy agents remains a major obstacle for improving
treatment outcomes for acute myeloid leukemia (AML). The Bcl-2-selective inhibitor ABT-199 …

Enhancing venetoclax activity in acute myeloid leukemia by co-targeting MCL1

TC Teh, NY Nguyen, DM Moujalled, D Segal, G Pomilio… - Leukemia, 2018 - nature.com
Targeted therapies are frequently combined with standard cytotoxic drugs to enhance
clinical response. Targeting the B-cell lymphoma 2 (BCL-2) family of proteins is an attractive …

BCL-2 as therapeutic target for hematological malignancies

GF Perini, GN Ribeiro, JV Pinto Neto… - Journal of hematology & …, 2018 - Springer
Disruption of the physiologic balance between cell proliferation and cell death is an
important step of cancer development. Increased resistance to apoptosis is a key oncogenic …

The BCL2 selective inhibitor venetoclax induces rapid onset apoptosis of CLL cells in patients via a TP53-independent mechanism

MA Anderson, J Deng, JF Seymour… - Blood, The Journal …, 2016 - ashpublications.org
BCL2 blunts activation of the mitochondrial pathway to apoptosis, and high-level expression
is required for chronic lymphocytic leukemia (CLL) survival. Venetoclax (ABT-199) is a small …