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 …
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
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 …
However, the potential of BCL-XL as an anti-cancer target has been hampered by the on …
Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines
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 …
inhibition associated platelet toxicity. Recently, we reported potent BCL-X L PROTAC …
Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity
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 …
resistance, rendering it an attractive target for cancer treatment. However, BCL-X L inhibitors …
[HTML][HTML] PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
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 …
metastasis, and intrinsic or therapy-induced cancer drug resistance. More recently, BCL-X L …
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity
EJ Hennessy - Bioorganic & medicinal chemistry letters, 2016 - Elsevier
The induction of apoptosis in tumor cells represents a promising approach to the treatment
of cancer. Accordingly, compounds that interact with the Bcl-2 family of proteins, which are …
of cancer. Accordingly, compounds that interact with the Bcl-2 family of proteins, which are …
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 …
homeostasis, clearance of abnormal cells and development of organisms. Over the past two …
Small-molecule inhibitors of Bcl-2 family proteins as therapeutic agents in cancer
R Mohammad, A Giri, AS Goustin - Recent patents on anti …, 2008 - ingentaconnect.com
This review focuses on the recent patents and use of small-molecule inhibitors (SMIs) of Bcl-
2 family proteins as therapeutic agents against cancer. Bcl-2 members are crucial regulators …
2 family proteins as therapeutic agents against cancer. Bcl-2 members are crucial regulators …
Discovery of novel inhibitors of Bcl-xL using multiple high-throughput screening platforms
J Qian, MJ Voorbach, JR Huth, ML Coen, H Zhang… - Analytical …, 2004 - Elsevier
Bcl-xL is a member of the Bcl-2 family of proteins that are implicated to play a vital role in
several diseases including cancer. Bcl-xL suppresses apoptosis; thus the inhibition of Bcl-xL …
several diseases including cancer. Bcl-xL suppresses apoptosis; thus the inhibition of Bcl-xL …
Discovery of a Novel BCL-XL PROTAC Degrader with Enhanced BCL-2 Inhibition
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 …
targeting chimeras (PROTACs) have been developed to circumvent the on-target platelet …