Results 1 to 10 of about 11,335 (243)
PROTAC-Splitter: a machine learning framework for automated identification of PROTAC substructures [PDF]
Journal of CheminformaticsProteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules composed of an E3 ligase ligand, a linker, and a warhead targeting a protein of interest. Despite their modular structure, accurately identifying and annotating these components in
Stefano Ribes +6 more
doaj +2 more sources
Highly efficient and long-acting split-and-mix proteolysis targeting chimera based on self-assembled polylactic acid [PDF]
Nature CommunicationsProteolysis targeting chimera (PROTAC) technology has received extensive attention due to its “event-driven” mechanism of action. However, existing chimera molecules tend to have higher molecular weight and higher polar surface area and exhibit lower ...
Mei-miao Zhan +12 more
doaj +2 more sources
Proteolysis-targeting Chimera efficacy prediction using a deep-learning–QSP model [PDF]
Journal of CheminformaticsThis study presents an integrated computational modeling framework combining deep learning and Quantitative Systems Pharmacology (QSP) to predict the efficacy of PROTAC (PROteolysis Targeting Chimera) molecules.
Sungwoo Goo +6 more
doaj +2 more sources
Recent Advances of Degradation Technologies Based on PROTAC Mechanism
Biomolecules, 2022 PROTAC (proteolysis-targeting chimeras), which selectively degrades target proteins, has become the most popular technology for drug development in recent years.
Mingchao Xiao +4 more
doaj +1 more source
Innovative developments and emerging technologies in RNA therapeutics
RNA Biology, 2022 RNA-based therapeutics are emerging as a powerful platform for the treatment of multiple diseases. Currently, the two main categories of nucleic acid therapeutics, antisense oligonucleotides and small interfering RNAs (siRNAs), achieve their therapeutic ...
François Halloy +10 more
doaj +1 more source
Degradation of proteins by PROTACs and other strategies
Acta Pharmaceutica Sinica B, 2020 Blocking the biological functions of scaffold proteins and aggregated proteins is a challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be the solution, considering its ability to selectively degrade target proteins.
Yang Wang +4 more
doaj +1 more source
PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy
Frontiers in Pharmacology, 2021 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 +6 more
doaj +1 more source
Interdisciplinary Medicine, 2023 Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD) technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells.
Xuyang Zhao +3 more
doaj +1 more source
Novel approaches for the rational design of PROTAC linkers
Exploration of Targeted Anti-tumor Therapy, 2020 Proteolysis targeting chimeras (PROTACs) represent a promising class of hetero-bivalent molecules that facilitate ubiquitination of a target protein by simultaneously binding and bringing together both the E3 enzyme and the target.
Almaz Zagidullin +3 more
doaj +1 more source
Frontiers in Oncology, 2022 Focal adhesion kinase (FAK) is highly expressed in a variety of human cancers and is a target for cancer therapy. Since FAK kinase inhibitors only block the kinase activity of FAK, they are not highly effective in clinical trials. FAK also functions as a
Xueyun Huo +15 more
doaj +1 more source