The manipulation of apoptosis for cancer therapy using BH3-mimetic drugs

ST Diepstraten, MA Anderson, PE Czabotar… - Nature Reviews …, 2022 - nature.com
Apoptosis is a form of programmed cell death that is regulated by the balance between
prosurvival and proapoptotic BCL-2 protein family members. Evasion of apoptosis is a …

MCL-1 inhibitors, fast-lane development of a new class of anti-cancer agents

A Bolomsky, M Vogler, MC Köse, CA Heckman… - Journal of hematology & …, 2020 - Springer
Cell death escape is one of the most prominent features of tumor cells and closely linked to
the dysregulation of members of the Bcl-2 family of proteins. Among those, the anti-apoptotic …

Activation of RAS/MAPK pathway confers MCL-1 mediated acquired resistance to BCL-2 inhibitor venetoclax in acute myeloid leukemia

Q Zhang, B Riley-Gillis, L Han, Y Jia, A Lodi… - Signal transduction and …, 2022 - nature.com
Despite high initial response rates, acute myeloid leukemia (AML) treated with the BCL-2–
selective inhibitor venetoclax (VEN) alone or in combinations commonly acquires …

The TP53 apoptotic network is a primary mediator of resistance to BCL2 inhibition in AML cells

T Nechiporuk, SE Kurtz, O Nikolova, T Liu, CL Jones… - Cancer discovery, 2019 - AACR
To study mechanisms underlying resistance to the BCL2 inhibitor venetoclax in acute
myeloid leukemia (AML), we used a genome-wide CRISPR/Cas9 screen to identify gene …

A novel MCL1 inhibitor combined with venetoclax rescues venetoclax-resistant acute myelogenous leukemia

HE Ramsey, MA Fischer, T Lee, AE Gorska, MP Arrate… - Cancer discovery, 2018 - AACR
Suppression of apoptosis by expression of antiapoptotic BCL2 family members is a hallmark
of acute myeloblastic leukemia (AML). Induced myeloid leukemia cell differentiation protein …

Mitochondrial reprogramming underlies resistance to BCL-2 inhibition in lymphoid malignancies

R Guièze, VM Liu, D Rosebrock, AA Jourdain… - Cancer cell, 2019 - cell.com
Mitochondrial apoptosis can be effectively targeted in lymphoid malignancies with the FDA-
approved B cell lymphoma 2 (BCL-2) inhibitor venetoclax, but resistance to this agent is …

Mitochondrial metabolism as a potential therapeutic target in myeloid leukaemia

L de Beauchamp, E Himonas, GV Helgason - Leukemia, 2022 - nature.com
While the understanding of the genomic aberrations that underpin chronic and acute
myeloid leukaemia (CML and AML) has allowed the development of therapies for these …

[HTML][HTML] Venetoclax resistance: mechanistic insights and future strategies

F Ong, K Kim, MY Konopleva - Cancer Drug Resistance, 2022 - ncbi.nlm.nih.gov
Acute myeloid leukemia (AML) is historically associated with poor prognosis, especially in
older AML patients unfit for intensive chemotherapy. The development of Venetoclax, a …

Pathways and mechanisms of venetoclax resistance

P Bose, V Gandhi, M Konopleva - Leukemia & lymphoma, 2017 - Taylor & Francis
The approval of venetoclax, a 'BH3-mimetic'antagonist of the BCL-2 anti-apoptotic protein,
for chronic lymphocytic leukemia represents a major milestone in translational apoptosis …

Treatment of older adults with FLT3-mutated AML: Emerging paradigms and the role of frontline FLT3 inhibitors

NJ Short, D Nguyen, F Ravandi - Blood cancer journal, 2023 - nature.com
FLT3 is the most frequently mutated gene in acute myeloid leukemia (AML), with FLT3
internal tandem duplication (ITD) mutations being associated with a more aggressive clinical …