Results 231 to 240 of about 827,025 (271)
Some of the next articles are maybe not open access.
Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras
Current Pharmaceutical Design, 2023Abstract: The most frequent mutated oncogene KRAS in lung cancer is targeted by KRAS G12C-directed drugs, such as Sotorasib and Adagrasib. Still, other alleles frequently expressed in pancreatic and colon cancer may be attacked indirectly by hitting the guanine nucleotide exchange factor (GEF) SOS1 that loads and activates KRAS.
Gerhard, Hamilton +2 more
openaire +2 more sources
Developing PROteolysis TArgeting Chimeras (PROTACs) for hematologic malignancies
Cancer Letters, 2022PROteolysis TArgeting Chimeras (PROTACs) degrade target proteins via the ubiquitin-proteasome system, providing novel insights into drug development for hematologic malignancies. PROTACs outperform conventional therapeutics and currently available small molecule inhibitors in terms of efficacy, tissue-and cell-selectivity, and side effect profile. Most
Yangping Wu +3 more
openaire +2 more sources
In vivo synthetic chemistry of proteolysis targeting chimeras (PROTACs)
Bioorganic & Medicinal Chemistry, 2021Chemical knockdown of therapeutic targets using proteolysis targeting chimeras (PROTACs) is a rapidly developing field in drug discovery, but PROTACs are bifunctional molecules that generally show poor bioavailability due to their relatively high molecular weight.
Shusuke Tomoshige, Minoru Ishikawa
openaire +2 more sources
Triazol: A Privileged Scaffold for Proteolysis Targeting Chimeras
Future Medicinal Chemistry, 2019Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists present inherent limitations due to occupancy-driven pharmacology as the mode of action. Proteolysis targeting chimeras (PROTACs) are composed of an E3 ligand, a connecting linker and a target protein ligand, and are an attractive approach to specifically knockdown ...
Li-Wen Xia +8 more
openaire +2 more sources
Progress on Small-Molecule Proteolysis-Targeting Chimeras
Future Medicinal Chemistry, 2019Proteolysis-targeting chimeras (PROTACs) have received much attention for their promising therapeutic intervention in recent years. These molecules, with the mechanism of simultaneous recruitment of target protein and an E3 ligase, can trigger the cellular ubiquitin-proteasome system to degrade the target proteins.
Wenhai, Huang +5 more
openaire +2 more sources
Advances in Proteolysis Targeting Chimeras
Proceedings of Anticancer ResearchIn recent years, proteolysis-targeting chimeras (PROTACs) have gained widespread attention as an emerging therapeutic approach. PROTACs are bifunctional molecules composed of a target protein-binding ligand, an E3 ubiquitin ligase ligand, and a linker connecting these ligands.
Shili Liu, Yu Liu
openaire +1 more source
Proteolysis Targeting Chimera (PROTAC) Design
2023In this chapter, carefully selected examples have been elaborated to illustrate how proteolysis targeting chimeras (PROTACs) can be elegantly developed based upon pre-existing active site-directed inhibitors for different types of enzymatic reactions involved in various life processes and therapeutic areas.
openaire +1 more source
Proteolysis-Targeting Chimeras: A Kaleidoscope of Targeted Protein Degradation
Future Medicinal Chemistry, 2021Yi Mou +3 more
openaire +2 more sources
Proteolysis-targeting chimera (PROTAC): A promising senolytic strategy
Ageing Research ReviewsSenescent cells (SCs) accumulate with aging and contribute to the development of age-related pathologies. These cells evade apoptosis through upregulation of senescent cell anti-apoptotic pathways (SCAPs), making their selective elimination, a strategy termed senolysis, a promising therapeutic avenue.
Gang Fan +6 more
openaire +2 more sources
Clinical application of proteolysis targeting chimeras
International Conference on Modern Medicine and Global Health (ICMMGH 2023), 2023Jinfeng Gao, Chuhan Meng, Vivian FT Yuan
openaire +1 more source