[HTML][HTML] PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors

P Zhang, X Zhang, X Liu, S Khan, D Zhou… - Exploration of targeted …, 2020 - ncbi.nlm.nih.gov
Abstract BCL-X L is an anti-apoptotic protein that plays an important role in tumorigenesis,
metastasis, and intrinsic or therapy-induced cancer drug resistance. More recently, BCL-X L …

Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines

X Zhang, Y He, P Zhang, V Budamagunta, D Lv… - European journal of …, 2020 - Elsevier
Abstract Targeting BCL-X L via PROTACs is a promising strategy in reducing BCL-X L
inhibition associated platelet toxicity. Recently, we reported potent BCL-X L PROTAC …

[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 …

Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity

X Zhang, D Thummuri, X Liu, W Hu, P Zhang… - European journal of …, 2020 - Elsevier
Anti-apoptotic protein BCL-X L plays a key role in tumorigenesis and cancer chemotherapy
resistance, rendering it an attractive target for cancer treatment. However, BCL-X L inhibitors …

PROTAC-mediated dual degradation of BCL-xL and BCL-2 is a highly effective therapeutic strategy in small-cell lung cancer

S Khan, L Cao, J Wiegand, P Zhang, M Zajac-Kaye… - Cells, 2024 - mdpi.com
BCL-xL and BCL-2 are validated therapeutic targets in small-cell lung cancer (SCLC).
Targeting these proteins with navitoclax (formerly ABT263, a dual BCL-xL/2 inhibitor) …

Discovery of a Novel BCL-XL PROTAC Degrader with Enhanced BCL-2 Inhibition

P Pal, D Thummuri, D Lv, X Liu, P Zhang… - Journal of medicinal …, 2021 - ACS Publications
BCL-XL and BCL-2 are important targets for cancer treatment. BCL-XL specific proteolysis-
targeting chimeras (PROTACs) have been developed to circumvent the on-target platelet …

Strategies to Reduce the On‐Target Platelet Toxicity of Bcl‐xL Inhibitors: PROTACs, SNIPERs and Prodrug‐Based Approaches

A Negi, AS Voisin‐Chiret - ChemBioChem, 2022 - Wiley Online Library
Apoptosis is a highly regulated cellular process. Aberration in apoptosis is a common
characteristic of various disorders. Therefore, proteins involved in apoptosis are prime …

Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-XL

X Zhang, D Thummuri, Y He, X Liu, P Zhang… - Chemical …, 2019 - pubs.rsc.org
BCL-XL, an anti-apoptotic BCL-2 family protein, plays a key role in cancer cell survival.
However, the potential of BCL-XL as an anti-cancer target has been hampered by the on …

[HTML][HTML] Targeting BCL-XL and BCL-2 by protac 753B effectively eliminates AML cells and enhances efficacy of chemotherapy by targeting senescent cells

Y Jia, Q Zhang, W Zhang, M Andreeff, N Jain, P Zhang… - Blood, 2021 - Elsevier
Abstract BCL-XL and BCL-2 are key anti-apoptotic proteins promoting cancer survival and
chemoresistance. 753B is a novel BCL-XL/BCL-2 proteolysis targeting chimera (PROTAC) …

BCL-xL targeting to induce apoptosis and to eliminate chemotherapy-induced senescent tumor cells: from navitoclax to platelet-sparing BCL-xL PROTACs

A Skwarska, M Konopleva - Cancer research, 2023 - AACR
Restoring apoptotic cell death is a critical goal for cancer therapy. One of the primary
mechanisms by which cancer cells evade death and maintain survival in the face of stress …