PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein degradation tool developed in recent years that can ubiquitinate the target proteins through the ubiquitin-proteasome system (UPS) to achieve an effect on tumor growth.
Si-min Qi +5 more
semanticscholar +1 more source
Gambogic Acid Is a Tissue-Specific Proteasome Inhibitor In Vitro and In Vivo
Gambogic acid (GA) is a natural compound derived from Chinese herbs that has been approved by the Chinese Food and Drug Administration for clinical trials in cancer patients; however, its molecular targets have not been thoroughly studied.
Xiaofen Li +28 more
doaj +1 more source
An eIF4E-binding protein regulates katanin protein levels in C. elegans embryos. [PDF]
In Caenorhabditis elegans, the MEI-1-katanin microtubule-severing complex is required for meiosis, but must be down-regulated during the transition to embryogenesis to prevent defects in mitosis.
DeBella, Leah +4 more
core +2 more sources
Covalently Engineered Nanobody Chimeras for Targeted Membrane Protein Degradation.
The targeted degradation of membrane proteins would afford an attractive and general strategy for treating various diseases that remain difficult with the current proteolysis-targeting chimera (PROTAC) methodology.
Heng Zhang +9 more
semanticscholar +1 more source
Background Acquired imatinib (IM) resistance is frequently characterized by Bcr-Abl mutations that affect IM binding and kinase inhibition in patients with chronic myelogenous leukemia (CML).
Xiaoying Lan +13 more
doaj +1 more source
Regulation of CLC-1 chloride channel biosynthesis by FKBP8 and Hsp90β. [PDF]
Mutations in human CLC-1 chloride channel are associated with the skeletal muscle disorder myotonia congenita. The disease-causing mutant A531V manifests enhanced proteasomal degradation of CLC-1.
Chen, Shu-Ching +7 more
core +1 more source
Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently ...
Xin Li, Yongcheng Song
semanticscholar +1 more source
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
Bivalent proteolysis-targeting chimeras (PROTACs) drive protein degradation by simultaneously binding a target protein and an E3 ligase and forming a productive ternary complex.
Satomi Imaide +16 more
semanticscholar +1 more source
Oscillations in the expression of a self-repressed gene induced by a slow transcriptional dynamics [PDF]
We revisit the dynamics of a gene repressed by its own protein in the case where the transcription rate does not adapt instantaneously to protein concentration but is a dynamical variable.
A. Goldbeter +8 more
core +7 more sources
Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic
Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation.
Zhenyi Hu, C. Crews
semanticscholar +1 more source

