Frontiers in Pharmacology, 2022 Gastric cancer is a common malignant tumor that threatens human health, and its occurrence and development mechanism is a complex process involving multiple genes and multiple signals.
Haobin Li +14 more
doaj +1 more source
Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader [PDF]
, 2019 SGK3 is a PX domain containing protein kinase activated at endosomes downstream of class 1 and 3 PI3K family members by growth factors and oncogenic mutations.
Alessi, Dario +6 more
core +2 more sources
Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
Journal of Hematology & Oncology, 2020 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
doaj +1 more source
Selective small molecule induced degradation of the BET bromodomain protein BRD4 [PDF]
, 2015 The Bromo- and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET selective bromodomain inhibitor JQ1.
Alessio Ciulli +39 more
core +5 more sources
Targeting Protein Kinases Degradation by PROTACs
Frontiers in Chemistry, 2021 Kinase dysregulation is greatly associated with cell proliferation, migration and survival, indicating the importance of kinases as therapeutic targets for anticancer drug development.
Fei Yu +3 more
doaj +1 more source
Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast and selective von Hippel-Lindau (VHL)-based dual degrader probe of BRD9 and BRD7 [PDF]
, 2018 Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently degrade a target protein within cells can be a lengthy and unpredictable process, and it remains unclear whether any combination of E3 and target might be productive ...
Ciulli, Alessio +10 more
core +6 more sources
3-Fluoro-4-hydroxyprolines:Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation [PDF]
, 2018 Hydroxylation and fluorination of proline alters the pyrrolidine ring pucker and the trans:cis amide bond ratio in a stereochemistry-dependent fashion, affecting molecular recognition of proline-containing molecules by biological systems.
Castro, Guilherme +10 more
core +8 more sources
Applying antibodies inside cells: Principles and recent advances in neurobiology, virology and oncology [PDF]
, 2020 To interfere with cell function, many scientists rely on methods that target DNA or RNA due to the ease with which they can be applied. Proteins are usually the final executors of function but are targeted only indirectly by these methods.
Marschall, Andrea +4 more
core +1 more source
, 2018 A transcription factor called SALL4 could be the missing link between thalidomide and the limb defects caused by the ...
Borozdin +12 more
core +1 more source
PROTAC Technology: Opportunities and Challenges [PDF]
ACS Medicinal Chemistry Letters, 2020 PROTACs-induced targeted protein degradation has emerged as a novel therapeutic strategy in drug development and attracted the favor of academic institutions, large pharmaceutical enterprises (e.g., AstraZeneca, Bayer, Novartis, Amgen, Pfizer, GlaxoSmithKline, Merck, and Boehringer Ingelheim, etc.), and biotechnology companies.
Hongying Gao, Xiuyun Sun, Yu Rao
openaire +2 more sources