A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
… PROTAC technology to generate a cell-selective BCL-X L … The potent antitumor activity of
DT2216 was correlated with its … that DT2216 is a safer and more potent antitumor agent than …
DT2216 was correlated with its … that DT2216 is a safer and more potent antitumor agent than …
Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity
… the utility of PROTAC technology to achieve tissue … activity. Compound 17b (XZ739), which
contains a PEG linker with linker length of 11 atoms, was the most potent BCL-X L degrader …
contains a PEG linker with linker length of 11 atoms, was the most potent BCL-X L degrader …
[HTML][HTML] Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity
… , a potent VHL-based BCL-xL PROTAC, as a safer and more potent antitumor agent than its
… are located within the band region which is feasible to achieve a conformation that is close to …
… are located within the band region which is feasible to achieve a conformation that is close to …
Discovery of a Novel BCL-XL PROTAC Degrader with Enhanced BCL-2 Inhibition
… Thus, we have demonstrated that the PROTAC technology could be used to achieve tissue/cell
selectivity by targeting E3 ligases that are differentially expressed in different tissues/cells…
selectivity by targeting E3 ligases that are differentially expressed in different tissues/cells…
Structural insights into PROTAC-mediated degradation of Bcl-xL
C Chung, H Dai, E Fernandez, CP Tinworth… - ACS Chemical …, 2020 - ACS Publications
… versus inhibition, (18−20) we report the design of a chemically distinct Bcl-xL VHL degrader,
… ternary complexation to achieve selective degradation of Bcl-xL over Bcl-2, PROTAC 6 may …
… ternary complexation to achieve selective degradation of Bcl-xL over Bcl-2, PROTAC 6 may …
[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 …
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
… Unlike conventional SMIs, the PROTAC molecule can be … To achieve positive cooperatively
in PROTAC strategy, the … was selectively Bcl-x L degrader but not a Bcl-2 degrader. …
in PROTAC strategy, the … was selectively Bcl-x L degrader but not a Bcl-2 degrader. …
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 …
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 …
[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 …