Progress in understanding the mechanisms of resistance to BCL-2 inhibitors

Y Xu, H Ye - Experimental Hematology & Oncology, 2022 - Springer
Venetoclax is a new type of BH3 mimetic compound that can target the binding site in the
BCL-2 protein and induce apoptosis in cancer cells by stimulating the mitochondrial …

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 …

Targeting BCL-2 in B-cell malignancies and overcoming therapeutic resistance

I Kapoor, J Bodo, BT Hill, ED Hsi, A Almasan - Cell death & disease, 2020 - nature.com
Defects in apoptosis can promote tumorigenesis and impair responses of malignant B cells
to chemotherapeutics. Members of the B-cell leukemia/lymphoma-2 (BCL-2) family of …

Mechanisms of venetoclax resistance and solutions

J Liu, Y Chen, L Yu, L Yang - Frontiers in Oncology, 2022 - frontiersin.org
The BCL-2 inhibitor venetoclax is currently approved for treatment of hematologic diseases
and is widely used either as monotherapy or in combination strategies. It has produced …

BCL2 and MCL1 inhibitors for hematologic malignancies

AW Roberts, AH Wei… - Blood, The Journal of the …, 2021 - ashpublications.org
BCL2 and MCL1 are commonly expressed prosurvival (antiapoptotic) proteins in
hematologic cancers and play important roles in their biology either through dysregulation or …

Hematologic tumor cell resistance to the BCL-2 inhibitor venetoclax: a product of its microenvironment?

JD Leverson, D Cojocari - Frontiers in Oncology, 2018 - frontiersin.org
BCL-2 family proteins regulate the intrinsic pathway of programmed cell death (apoptosis)
and play a key role in the development and health of multicellular organisms. The dynamics …

Lymphoma cells lacking pro-apoptotic BAX are highly resistant to BH3-mimetics targeting pro-survival MCL-1 but retain sensitivity to conventional DNA-damaging …

ST Diepstraten, S Young, JE La Marca… - Cell Death & …, 2023 - nature.com
BH3-mimetic drugs are an anti-cancer therapy that can induce apoptosis in malignant cells
by directly binding and inhibiting pro-survival proteins of the BCL-2 family. The BH3-mimetic …

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 …

[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 …

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 …