Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-XL
BCL-XL, an anti-apoptotic BCL-2 family protein, plays a key role in cancer cell survival.
However, the potential of BCL-XL as an anti-cancer target has been hampered by the on …
However, the potential of BCL-XL as an anti-cancer target has been hampered by the on …
[HTML][HTML] Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells
Regulatory T cells (Tregs) play an important role in maintaining immune homeostasis and,
within tumors, their upregulation is common and promotes an immunosuppressive …
within tumors, their upregulation is common and promotes an immunosuppressive …
Prime time for PROTACs
RJ Deshaies - Nature chemical biology, 2015 - nature.com
PROTACs are heterobifunctional small molecules that simultaneously bind a target protein
and a ubiquitin ligase, enabling ubiquitination and degradation of the target. Major progress …
and a ubiquitin ligase, enabling ubiquitination and degradation of the target. Major progress …
Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently
Z Yang, Y Sun, Z Ni, C Yang, Y Tong, Y Liu, H Li… - Cell Research, 2021 - nature.com
Dear Editor, Targeted protein degradation (TPD) represents a promising research field that
has quickly attracted attention and efforts from both academia and pharmaceutical industry …
has quickly attracted attention and efforts from both academia and pharmaceutical industry …
An inhibitor of Bcl-2 family proteins induces regression of solid tumours
T Oltersdorf, SW Elmore, AR Shoemaker… - Nature, 2005 - nature.com
Proteins in the Bcl-2 family are central regulators of programmed cell death, and members
that inhibit apoptosis, such as Bcl-XL and Bcl-2, are overexpressed in many cancers and …
that inhibit apoptosis, such as Bcl-XL and Bcl-2, are overexpressed in many cancers and …
Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia
S Peirs, V Frismantas, F Matthijssens, W Van Loocke… - Leukemia, 2017 - nature.com
Inhibition of anti-apoptotic BCL-2 (B-cell lymphoma 2) has recently emerged as a promising
new therapeutic strategy for the treatment of a variety of human cancers, including leukemia …
new therapeutic strategy for the treatment of a variety of human cancers, including leukemia …
The BH3-only mimetic ABT-737 synergizes the antineoplastic activity of proteasome inhibitors in lymphoid malignancies
Overexpression of antiapoptotic members of the Bcl-2 family is observed in approximately
80% of B-cell lymphomas, contributing to intrinsic and acquired drug resistance. Nullifying …
80% of B-cell lymphomas, contributing to intrinsic and acquired drug resistance. Nullifying …
Structure-guided design of a selective BCL-XL inhibitor
The prosurvival BCL-2 family protein BCL-X L is often overexpressed in solid tumors and
renders malignant tumor cells resistant to anticancer therapeutics. Enhancing apoptotic …
renders malignant tumor cells resistant to anticancer therapeutics. Enhancing apoptotic …
ABT-199, a new Bcl-2–specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia
CJ Vandenberg, S Cory - Blood, The Journal of the American …, 2013 - ashpublications.org
BH3-only proteins trigger the stress apoptosis pathway and chemical mimetics have great
potential for cancer therapy. BH3-only proteins inhibit antiapoptotic members of the Bcl-2 …
potential for cancer therapy. BH3-only proteins inhibit antiapoptotic members of the Bcl-2 …
[HTML][HTML] BCL6 repression of EP300 in human diffuse large B cell lymphoma cells provides a basis for rational combinatorial therapy
LC Cerchietti, K Hatzi, E Caldas-Lopes… - The Journal of …, 2010 - Am Soc Clin Investig
B cell lymphoma 6 (BCL6), which encodes a transcriptional repressor, is a critical oncogene
in diffuse large B cell lymphomas (DLBCLs). Although a retro-inverted BCL6 peptide …
in diffuse large B cell lymphomas (DLBCLs). Although a retro-inverted BCL6 peptide …