dSTORM‐Based Single‐Cell Protein Quantitative Analysis Can Effectively Evaluate the Degradation Ability of PROTACs
Sign Up to like & getrecommendations! Published in 2022 at "ChemBioChem"
DOI: 10.1002/cbic.202200680
Abstract: As an emerging therapeutic strategy, proteolysis‐targeting chimeras (PROTACs) have been proven to be superior to traditional drugs in many aspects. However, due to their unique mechanism of action, existing methods for evaluating the degradation still… read more here.
Keywords: protacs; dstorm based; analysis; based single ... See more keywords
Strategies for designing proteolysis targeting chimaeras (PROTACs)
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DOI: 10.1002/med.21877
Abstract: Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique for new drug discovery and development. Currently, the largest challenge in the molecular design and drug development of PROTACs is efficient identification of… read more here.
Keywords: protacs; chimaeras protacs; proteolysis targeting; targeting chimaeras ... See more keywords
Development of Rapid and Facile Solid‐Phase Synthesis of PROTACs via a Variety of Binding Styles
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DOI: 10.1002/open.202200131
Abstract: Abstract Optimizing linker design is important for ensuring efficient degradation activity of proteolysis‐targeting chimeras (PROTACs). Therefore, developing a straightforward synthetic approach that combines the protein‐of‐interest ligand (POI ligand) and the ligand for E3 ubiquitin ligase… read more here.
Keywords: protacs; synthesis; development rapid; solid phase ... See more keywords
Developing potent PROTACs tools for selective degradation of HDAC6 protein
Sign Up to like & getrecommendations! Published in 2019 at "Protein & Cell"
DOI: 10.1007/s13238-018-0602-z
Abstract: Histone deacetylases (HDACs) are a family of enzymes that remove acetyl groups on histone and non-histone proteins, thereby playing a vital role in the modulation of gene expression and protein activity. Eighteen HDACs have been… read more here.
Keywords: degradation; protacs; hdac6; cell ... See more keywords
Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112451
Abstract: We report the design of hetero-bifunctional small molecules that selectively target p38α and p38β for degradation. These proteolysis targeted chimeras (PROTACs) are based on an ATP competitive inhibitor of p38α and p38β, which is linked… read more here.
Keywords: degradation; target p38; protacs; p38 p38 ... See more keywords
Indomethacin-based PROTACs as pan-coronavirus antiviral agents
Sign Up to like & getrecommendations! Published in 2021 at "European Journal of Medicinal Chemistry"
DOI: 10.1016/j.ejmech.2021.113814
Abstract: Indomethacin (INM), a well-known non-steroidal anti-inflammatory drug, has recently gained attention for its antiviral activity demonstrated in drug repurposing studies against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). Although the mechanism of action of INM is… read more here.
Keywords: based protacs; pan coronavirus; inm; protacs ... See more keywords
PROTACs: a novel strategy for cancer therapy.
Sign Up to like & getrecommendations! Published in 2020 at "Seminars in cancer biology"
DOI: 10.1016/j.semcancer.2020.02.006
Abstract: Chemotherapeutic strategy has been widely used for treating malignance by targeting irregular expressed or mutant proteins with small molecular inhibitors (SMIs) or monoclonal antibodies (mAbs). However, most intracellular proteins lack of active sites or antigens… read more here.
Keywords: strategy cancer; protacs; cancer; novel strategy ... See more keywords
PROTACs As Potential Therapeutic Agents for Cancer Drug Resistance.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemistry"
DOI: 10.1021/acs.biochem.9b00848
Abstract: Cancer drug resistance becomes the major challenging problem facing current clinical treatment faced by different kinds of therapies. Proteolysis targeting chimeras (PROTACs) as a novel and powerful strategy has attracted great attentions both from academia… read more here.
Keywords: drug resistance; drug; resistance; protacs ... See more keywords
Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation.
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DOI: 10.1021/acs.jmedchem.2c00728
Abstract: Proteolysis-targeting chimeras (PROTACs) is a fast-growing technology providing many strengths over inhibition of protein activity directly and is attracting increasing interest in new drug discovery and development. However, efficiently identifying potent and drug-like degraders is… read more here.
Keywords: covalent protacs; protacs; protein degradation; trivalent ... See more keywords
A Versatile and Sustainable Multicomponent Platform for the Synthesis of Protein Degraders: Proof-of-Concept Application to BRD4-Degrading PROTACs
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01218
Abstract: The use of small molecules to induce targeted protein degradation is increasingly growing in the drug discovery landscape, and protein degraders have progressed rapidly through the pipelines. Despite the advances made so far, their synthesis… read more here.
Keywords: protacs; synthesis; protein degraders; degrading protacs ... See more keywords
Development of Stabilized Peptide-Based PROTACs against Estrogen Receptor α.
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DOI: 10.1021/acschembio.7b00985
Abstract: Peptide modulators targeting protein-protein interactions (PPIs) exhibit greater potential than small-molecule drugs in several important aspects including facile modification and relative large contact surface area. Stabilized peptides constructed by variable chemistry methods exhibit improved peptide… read more here.
Keywords: peptide; stabilized peptide; peptide based; protacs ... See more keywords