[HTML][HTML] DT2216, a synthetic proteolytic selectively targeting Bcl-XL for ubiquitination and degradation in tumor cells but not in platelets, is a safer and more potent …
The evasion of apoptosis, or programmed cell death, is a hallmark of cancer, which
promotes tumor initiation and progression. The evasion is in part attributable to the over …
promotes tumor initiation and progression. The evasion is in part attributable to the over …
Abstract IA34: Clinical proof of concept for the first-in-class BCL-2-selective inhibitor venetoclax (ABT-199/GDC-0199)
JD Leverson - Cancer Research, 2016 - AACR
Many cancer cells maintain survival through over-expression of anti-apoptotic BCL-2 family
proteins, which sequester high levels of their pro-apoptotic counterparts. While this makes …
proteins, which sequester high levels of their pro-apoptotic counterparts. While this makes …
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 …
[HTML][HTML] DT2216, a BCL-XL proteolysis targeting chimera (PROTAC), is a potent anti T-cell lymphoma agent that does not induce significant thrombocytopenia
There is an urgent need for new therapeutic agents to treat patients with T-cell lymphoma
(TCL). Multiple hematologic malignancies evade apoptosis through overexpression of anti …
(TCL). Multiple hematologic malignancies evade apoptosis through overexpression of anti …
Selective targeting of antiapoptotic BCL‐2 proteins in cancer
AC Timucin, H Basaga, O Kutuk - Medicinal research reviews, 2019 - Wiley Online Library
Circumvention of apoptotic machinery is one of the distinctive properties of carcinogenesis.
Extensively established key effectors of such apoptotic bypass mechanisms, the …
Extensively established key effectors of such apoptotic bypass mechanisms, the …
Redefining Cancer Therapy: Toward BCL-XL/BCL-2 Dual Inhibitors with Diminished Platelet Toxicity
RB Kargbo - ACS Medicinal Chemistry Letters, 2023 - ACS Publications
This Patent Highlight focuses on the development of Bcl-xL/Bcl-2 dual inhibitors with
minimized platelet toxicity to improve cancer treatment strategies. Acknowledging the critical …
minimized platelet toxicity to improve cancer treatment strategies. Acknowledging the critical …
From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors
Members of the B cell lymphoma 2 (BCL-2) gene family have a central role in regulating
programmed cell death by controlling pro-apoptotic and anti-apoptotic intracellular signals …
programmed cell death by controlling pro-apoptotic and anti-apoptotic intracellular signals …
Current strategies to target the anti-apoptotic Bcl-2 protein in cancer cells
SME Oxford, CL Dallman, PWM Johnson… - Current medicinal …, 2004 - ingentaconnect.com
Apoptosis (or programmed cell death) is a genetically controlled “cell suicide” pathway
which plays an essential role in deleting excess, unwanted or damaged cells during …
which plays an essential role in deleting excess, unwanted or damaged cells during …
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 …
FCN-338, a novel and selective Bcl-2 inhibitor, exhibits potent anti-tumor activity in B-cell lymphoma
S Lin, X Zhao, H Liu, H Zhang, Z Chen, L Jiang, Y Liu… - Cancer Research, 2019 - AACR
Abstract B-cell lymphoma-2 (Bcl-2) family proteins are key regulators of apoptosis, which is
vital for proper tissue development and cellular homeostasis. Apoptosis occurs via activation …
vital for proper tissue development and cellular homeostasis. Apoptosis occurs via activation …