[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 …
[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 …
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 …
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 …
Targeting BCR-ABL1 in chronic myeloid leukemia by PROTAC-mediated targeted protein degradation
Although the use of ATP-competitive tyrosine kinase inhibitors of oncoprotein BCR-ABL1
has enabled durable responses in patients with chronic myeloid leukemia (CML), issues of …
has enabled durable responses in patients with chronic myeloid leukemia (CML), issues of …
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 …
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 …
Therapeutics targeting Bcl-2 in hematological malignancies
A Ruefli-Brasse, JC Reed - Biochemical Journal, 2017 - portlandpress.com
Members of the B-cell lymphoma 2 (BCL-2) gene family are attractive targets for cancer
therapy as they play a key role in promoting cell survival, a long-since established hallmark …
therapy as they play a key role in promoting cell survival, a long-since established hallmark …
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 …
Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy
JD Leverson, DC Phillips, MJ Mitten… - Science translational …, 2015 - science.org
The BCL-2/BCL-XL/BCL-W inhibitor ABT-263 (navitoclax) has shown promising clinical
activity in lymphoid malignancies such as chronic lymphocytic leukemia. However, its …
activity in lymphoid malignancies such as chronic lymphocytic leukemia. However, its …