PROTAC therapy as a new targeted therapy for lung cancer
Despite recent advances in molecular therapeutics, lung cancer is still a leading cause of
cancer deaths. Currently, limited targeted therapy options and acquired drug resistance …
cancer deaths. Currently, limited targeted therapy options and acquired drug resistance …
Piperlongumine conjugates induce targeted protein degradation
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that degrade target
proteins through recruiting E3 ligases. However, their application is limited in part because …
proteins through recruiting E3 ligases. However, their application is limited in part because …
Recent advances in targeted protein degraders as potential therapeutic agents
N Yang, B Kong, Z Zhu, F Huang, L Zhang, T Lu… - Molecular …, 2024 - Springer
Targeted protein degradation (TPD) technology has gradually become widespread in the
past 20 years, which greatly boosts the development of disease treatment. Contrary to small …
past 20 years, which greatly boosts the development of disease treatment. Contrary to small …
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
Purpose The BCL-2 family of anti-apoptotic proteins, BCL-2, BCL-XL and MCL-1, can
mediate survival of some types of cancer. DT2216 is a PROteolysis-TArgeting Chimera …
mediate survival of some types of cancer. DT2216 is a PROteolysis-TArgeting Chimera …
[HTML][HTML] Bcl-x short-isoform is essential for maintaining homeostasis of multiple tissues
MA Keller, C Huang, A Ivessa, S Singh… - Iscience, 2023 - cell.com
Summary BCL-2-like protein 1 (BCL2L1) is a key component of cell survival and death
mechanisms. Its dysregulation and altered ratio of splicing variants associate with …
mechanisms. Its dysregulation and altered ratio of splicing variants associate with …
Thalidomide derivatives degrade BCL-2 by reprogramming the binding surface of CRBN
Recent studies demonstrate that modified thalidomide chemically alters the binding surface
of its binding E3 ligase, CRBN, leading to the degradation of new substrate proteins. In this …
of its binding E3 ligase, CRBN, leading to the degradation of new substrate proteins. In this …
Reciprocal effects of mTOR inhibitors on pro-survival proteins dictate therapeutic responses in tuberous sclerosis complex
Summary mTORC1 is aberrantly activated in cancer and in the genetic tumor syndrome
tuberous sclerosis complex (TSC), which is caused by loss-of-function mutations in the TSC …
tuberous sclerosis complex (TSC), which is caused by loss-of-function mutations in the TSC …
HDAC3 and HDAC8 PROTAC dual degrader reveals roles of histone acetylation in gene regulation
HDAC3 and HDAC8 have critical biological functions and represent highly sought-after
therapeutic targets. Because histone deacetylases (HDACs) have a very conserved catalytic …
therapeutic targets. Because histone deacetylases (HDACs) have a very conserved catalytic …