Results 31 to 40 of about 14,786 (290)
Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies
Journal of Hematology & Oncology, 2020 Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI).
Yonghan He +10 more
doaj +1 more source
The clinical advances of proteolysis targeting chimeras in oncology
Exploration of Targeted Anti-tumor Therapy, 2021 Proteolysis targeting chimeras (PROTACs) are a class of small molecules designed to target proteins for degradation. Their novel and unique modes of action provide PROTACs with the potential for their application in the management of both solid and ...
Hao Xie +3 more
doaj +1 more source
Targeting STAT3 in Cancer with Nucleotide Therapeutics. [PDF]
, 2019 Signal transducer and activator of transcription 3 (STAT3) plays a critical role in promoting the proliferation and survival of tumor cells. As a ubiquitously-expressed transcription factor, STAT3 has commonly been considered an "undruggable" target for ...
Grandis, Jennifer R +3 more
core +2 more sources
Pharmaceutics, 2023 Proteolysis-targeting chimeras (PROTACs) are rapidly emerging as a potential therapeutic strategy for cancer therapy by inducing the degradation of tumor-overexpressing oncogenic proteins.
Yujeong Moon +3 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
Journal of Enzyme Inhibition and Medicinal Chemistry, 2022 Proteolysis-targeting chimaeras (PROTACs) have been developed to be an emerging technology for targeted protein degradation and attracted the favour of academic institutions, large pharmaceutical enterprises, and biotechnology companies. The mechanism is
Chao Wang +5 more
doaj +1 more source
Molecular recognition of ternary complexes:a new dimension in the structure-guided design of chemical degraders [PDF]
, 2017 Molecular glues and bivalent inducers of protein degradation (also known as PROTACs) represent a fascinating new modality in pharmacotherapeutics: the potential to knockdown previously thought ‘undruggable’ targets at sub-stoichiometric concentrations in
Alessio Ciulli +68 more
core +2 more sources
Proteolysis-targeting chimeras (PROTACs) in cancer therapy
Molecular Cancer, 2022 Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits target protein and E3 ubiquitin ligase together to trigger proteasomal ...
Xinyi Li +5 more
doaj +1 more source
Reversible Covalent PROTACs: Novel and Efficient Targeted Degradation Strategy
Frontiers in Chemistry, 2021 The proteolysis targeting chimeras (PROTACs), which are composed of a target protein binding moiety, a linker, and an E3 ubiquitin ligase binder, have been a promising strategy for drug design and discovery.
Minghua Yuan +4 more
doaj +1 more source
SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate [PDF]
, 2019 Bifunctional degrader molecules, known as proteolysis-targeting chimeras (PROTACs), function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary complex.
Ciulli, Alessio +7 more
core +3 more sources