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 …

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 …

Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy

CM Patterson, SB Balachander, I Grant… - Communications …, 2021 - nature.com
Abstract Dual Bcl-2/Bcl-xL inhibitors are expected to deliver therapeutic benefit in many
haematological and solid malignancies, however, their use is limited by tolerability issues …

Clinical experiences with venetoclax and other pro-apoptotic agents in lymphoid malignancies: lessons from monotherapy and chemotherapy combination

TE Lew, JF Seymour - Journal of Hematology & Oncology, 2022 - Springer
BH3-mimetics are a novel drug class of small molecule inhibitors of BCL2 family proteins
which restore apoptosis in malignant cells. The only currently approved BH3-mimetic, the …

[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 …

Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment

Z Zhang, L Bai, L Hou, H Deng, S Luan, D Liu… - European Journal of …, 2022 - Elsevier
Apoptosis is the major mode of programmed cell death, which conduces to maintain tissue
homeostasis, clearance of abnormal cells and development of organisms. Over the past two …

BH3 mimetics targeting BCL-XL impact the senescent compartment of pilocytic astrocytoma

F Selt, R Sigaud, G Valinciute, P Sievers… - Neuro …, 2023 - academic.oup.com
Background Pilocytic astrocytoma (PA) is the most common pediatric brain tumor and a
mitogen-activated protein kinase (MAPK)-driven disease. Oncogenic MAPK-signaling drives …

AKT-mTORC1 reactivation is the dominant resistance driver for PI3Kβ/AKT inhibitors in PTEN-null breast cancer and can be overcome by combining with Mcl-1 …

S Dunn, C Eberlein, J Yu, A Gris-Oliver, SH Ong… - Oncogene, 2022 - nature.com
The PI3K pathway is commonly activated in breast cancer, with PI3K-AKT pathway inhibitors
used clinically. However, mechanisms that limit or enhance the therapeutic effects of PI3K …

Current advances and future strategies for BCL-2 inhibitors: potent weapons against cancers

J Xu, X Dong, DCS Huang, P Xu, Q Zhao, B Chen - Cancers, 2023 - mdpi.com
Simple Summary The development of BCL-2 inhibitors as a pivotal approach in cancer
treatment lies in their ability to effectively trigger apoptosis in tumor cells. Venetoclax, a …

Dual targeting of apoptotic and signaling pathways in T-lineage acute lymphoblastic leukemia

C Saygin, G Giordano, K Shimamoto, B Eisfelder… - Clinical Cancer …, 2023 - AACR
Purpose: Relapsed T-acute lymphoblastic leukemia (T-ALL) has limited treatment options.
We investigated mechanisms of resistance to BH3 mimetics in T-ALL to develop rational …