Results 11 to 20 of about 11,341 (256)
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 +5 more sources
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.
Jinyun Dong +2 more
exaly +3 more sources
Drugtamer‐PROTAC Conjugation Strategy for Targeted PROTAC Delivery and Synergistic Antitumor Therapy
Advanced ScienceProteolysis‐targeting chimeras (PROTACs) have emerged as a promising strategy for targeted protein degradation and drug discovery. To overcome the inherent limitations of conventional PROTACs, an innovative drugtamer‐PROTAC conjugation approach is ...
Guoqiang Dong, Chunquan Sheng
exaly +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
Drug Discovery Today, 2021 Targeting protein-protein interactions (PPI) is a key focus in the development of new and emerging small-molecule therapeutics. Shallow interacting surfaces can render PPI targeting notoriously difficult. This leaves many therapeutically captivating targets 'undruggable'.
Gregory R. Hughes +3 more
openaire +3 more sources
Pharmaceutics, 2022 Targeting selective estrogen subtype receptors through typical medicinal chemistry approaches is based on occupancy-driven pharmacology. In occupancy-driven pharmacology, molecules are developed in order to inhibit the protein of interest (POI), and their popularity is based on their virtue of faster kinetics.
Arvind Negi +2 more
+8 more sources
PROTAC-DB: an online database of PROTACs [PDF]
Nucleic Acids Research, 2020 Abstract Proteolysis-targeting chimeras (PROTACs), which selectively degrade targeted proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic technology with potential advantages over traditional inhibition strategies.
Gaoqi Weng +9 more
openaire +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
PROTAC-DB 2.0: an updated database of PROTACs
Nucleic Acids Research, 2022 AbstractProteolysis targeting chimeras (PROTACs), which harness the ubiquitin-proteasome system to selectively induce targeted protein degradation, represent an emerging therapeutic technology with the potential to modulate traditional undruggable targets.
Gaoqi Weng +9 more
openaire +2 more sources
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