A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
B-cell lymphoma extra large (BCL-XL) is a well-validated cancer target. However, the on-
target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as …
target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as …
DT2216—a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas
Background Patients with advanced T cell lymphomas (TCLs) have limited therapeutic
options and poor outcomes in part because their TCLs evade apoptosis through …
options and poor outcomes in part because their TCLs evade apoptosis through …
Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity
Abstract PROteolysis-TArgeting Chimeras (PROTACs) have emerged as an innovative drug
development platform. However, most PROTACs have been generated empirically because …
development platform. However, most PROTACs have been generated empirically because …
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets
AJ Souers, JD Leverson, ER Boghaert, SL Ackler… - Nature medicine, 2013 - nature.com
Proteins in the B cell CLL/lymphoma 2 (BCL-2) family are key regulators of the apoptotic
process. This family comprises proapoptotic and prosurvival proteins, and shifting the …
process. This family comprises proapoptotic and prosurvival proteins, and shifting the …
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] Co-targeting BCL-XL and BCL-2 by PROTAC 753B eliminates leukemia cells and enhances efficacy of chemotherapy by targeting senescent cells
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 …
753B is a novel BCL-X L/BCL-2 proteolysis targeting chimera (PROTAC) that targets both …
PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
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 …
Degradation of Bruton's tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas
Y Sun, N Ding, Y Song, Z Yang, W Liu, J Zhu, Y Rao - Leukemia, 2019 - nature.com
Diffuse large B-cell lymphoma (DLBCL) is the most common type of non-Hodgkin lymphoma
(NHL). In the United States and United Kingdom, the annual prevalence of DLBCL is as high …
(NHL). In the United States and United Kingdom, the annual prevalence of DLBCL is as high …
Development of a novel B-cell lymphoma 6 (BCL6) PROTAC to provide insight into small molecule targeting of BCL6
W McCoull, T Cheung, E Anderson, P Barton… - ACS Chemical …, 2018 - ACS Publications
B-cell lymphoma 6 (BCL6) inhibition is a promising mechanism for treating hematological
cancers but high quality chemical probes are necessary to evaluate its therapeutic potential …
cancers but high quality chemical probes are necessary to evaluate its therapeutic potential …