[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 …

[HTML][HTML] 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 …

Dual targeting of BCL-2 and MCL-1 in the presence of BAX breaks venetoclax resistance in human small cell lung cancer

Z Valko, Z Megyesfalvi, A Schwendenwein… - British Journal of …, 2023 - nature.com
Background No targeted drugs are currently available against small cell lung cancer
(SCLC). BCL-2 family members are involved in apoptosis regulation and represent …

Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies

D Thomalla, L Beckmann, C Grimm… - Blood, The Journal …, 2022 - ashpublications.org
The BCL2 inhibitor venetoclax has been approved to treat different hematological
malignancies. Because there is no common genetic alteration causing resistance to …

[HTML][HTML] Hyperphosphorylation of BCL-2 family proteins underlies functional resistance to venetoclax in lymphoid malignancies

SJF Chong, F Zhu, O Dashevsky… - The Journal of …, 2023 - Am Soc Clin Investig
The B cell leukemia/lymphoma 2 (BCL-2) inhibitor venetoclax is effective in chronic
lymphocytic leukemia (CLL); however, resistance may develop over time. Other lymphoid …

[HTML][HTML] Co-targeting BCL-XL and BCL-2 by PROTAC 753B eliminates leukemia cells and enhances efficacy of chemotherapy by targeting senescent cells

Y Jia, L Han, CL Ramage, Z Wang, CC Weng… - …, 2023 - ncbi.nlm.nih.gov
Abstract BCL-X L and BCL-2 are key anti-apoptotic proteins and validated cancer targets.
753B is a novel BCL-X L/BCL-2 proteolysis targeting chimera (PROTAC) that targets both …

[HTML][HTML] Understanding ER homeostasis and the UPR to enhance treatment efficacy of acute myeloid leukemia

M Śniegocka, F Liccardo, F Fazi, S Masciarelli - Drug Resistance Updates, 2022 - Elsevier
Protein biogenesis, maturation and degradation are tightly regulated processes that are
governed by a complex network of signaling pathways. The endoplasmic reticulum (ER) is …

[HTML][HTML] Targeting acute myeloid leukemia with venetoclax; biomarkers for sensitivity and rationale for venetoclax-based combination therapies

MS Griffioen, DC de Leeuw, JJWM Janssen, L Smit - Cancers, 2022 - mdpi.com
Simple Summary Venetoclax has proven to be a promising therapy for newly diagnosed,
relapsed and refractory AML patients ineligible for induction chemotherapy. Current ongoing …

Single-cell genomics in AML: extending the frontiers of AML research

A Ediriwickrema, AJ Gentles, R Majeti - Blood, 2023 - ashpublications.org
The era of genomic medicine has allowed acute myeloid leukemia (AML) researchers to
improve disease characterization, optimize risk-stratification systems, and develop new …

[HTML][HTML] The emerging role of venetoclax-based treatments in acute lymphoblastic leukemia

S Aumann, A Shaulov, A Haran… - International Journal of …, 2022 - mdpi.com
Venetoclax, a B-cell lymphoma (BCL-2) inhibitor, in combination with hypomethylating
agents has become the new standard of care in elderly and unfit patients with acute myeloid …