[HTML][HTML] DT2216—a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas
… (PROTAC) targeting Bcl-xL for degradation via Von Hippel-Lindau (VHL) E3 ligase, and
shown that it has better anti-tumor activity … cannot be achieved by the use of either Bcl-xl-specific …
shown that it has better anti-tumor activity … cannot be achieved by the use of either Bcl-xl-specific …
[HTML][HTML] Targeting anti-apoptotic BCL-2 family proteins for cancer treatment
… platelets, have been recruited to degrade BCL-X L [13,… PROTAC degraders. Further, the
lead candidate, DT2216, a VHL-based PROTAC derived from ABT-263, achieved better potency …
lead candidate, DT2216, a VHL-based PROTAC derived from ABT-263, achieved better potency …
[HTML][HTML] BCL-XL PROTAC degrader DT2216 synergizes with sotorasib in preclinical models of KRASG12C-mutated cancers
… BCL-X L proteolysis targeting chimera [PROTAC]) on KRAS G12C -mutated NSCLC, …
antitumor efficacy of sotorasib in vivo. Collectively, our findings suggest that due to cytostatic activity…
antitumor efficacy of sotorasib in vivo. Collectively, our findings suggest that due to cytostatic activity…
Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines
… importance of selecting suitable E3 members to achieve effective cellular activity. … degrade
BCL-X L and kill various cancer cells [[14], [15], [16]]. PROTAC 8a has similar cell killing effect …
BCL-X L and kill various cancer cells [[14], [15], [16]]. PROTAC 8a has similar cell killing effect …
[HTML][HTML] The PROTAC selectively degrading Bcl-xL represents a novel Hedgehog pathway inhibitor with capacity of combating resistance to Smoothened inhibitors …
S Zhang, Y Chen, Z Xu, J Yang, R Sun, J Wang… - Theranostics, 2022 - ncbi.nlm.nih.gov
… -225, pediatric patients whose bones have not achieved full maturity were found to develop
… Furthermore, we found that the potent antitumor activity of SIAIS316034 corresponded well …
… Furthermore, we found that the potent antitumor activity of SIAIS316034 corresponded well …
[HTML][HTML] PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
… These findings demonstrated the potentially broad utility of PROTAC technology to achieve
… in a unique mechanism of action (MOA). In brief, once the PROTAC degrader enters the cell, …
… in a unique mechanism of action (MOA). In brief, once the PROTAC degrader enters the cell, …
Resistance to the BCL-XL degrader DT2216 in T-cell acute lymphoblastic leukemia is rare and correlates with decreased BCL-XL proteolysis
A Jaiswal, A Jaiswal, EA Williamson, J Gelfond… - Cancer chemotherapy …, 2023 - Springer
… -targeting chimera (PROTAC), DT2216 as a specific BCL-XL protein degrader [6,7,8]. … of
DT2216 that exceeded what we reported could be achieved within a T-ALL xenografted tumor in …
DT2216 that exceeded what we reported could be achieved within a T-ALL xenografted tumor in …
Mivebresib synergized with PZ703b, a novel Bcl-xl PROTAC degrader, induces apoptosis in bladder cancer cells via the mitochondrial pathway
Y Xu, Z Lei, J Zhu, L Wan - Biochemical and Biophysical Research …, 2022 - Elsevier
… of Bcl-xl could confer can cells resistance against BET inhibitors [5], we hypothesized that
Bcl-xl PROTAC, when combined with BET inhibitors, may increase their anti-tumor effects. To …
Bcl-xl PROTAC, when combined with BET inhibitors, may increase their anti-tumor effects. To …
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
… not only to achieve strong antitumor activity but also mitigate … Highlighting the advantages
of PROTAC over conventional … The crystallographic information reveals that this degrader not …
of PROTAC over conventional … The crystallographic information reveals that this degrader not …
[HTML][HTML] Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells
… -X L degrader—a proteolysis-targeting chimera (PROTAC) referred to … We also developed
another similar PROTAC PZ15227 that … This can be achieved pharmacologically by applying …
another similar PROTAC PZ15227 that … This can be achieved pharmacologically by applying …