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Sulfatase-Induced In Situ Formulation of Antineoplastic Supra-PROTACs.
Journal of the American Chemical SocietyProteolysis targeting chimera (PROTAC) technology is an innovative strategy for cancer therapy, which, however, suffers from poor targeting delivery and limited capability for protein of interest (POI) degradation.
Ninglin Chen +10 more
semanticscholar +1 more source
Nano-PROTACs: state of the art and perspectives.
NanoscalePROteolysis TArgeting Chimeras (PROTACs), as a recently identified technique in the field of new drug development, provide new concepts for disease treatment and are expected to revolutionize drug discovery. With high specificity and flexibility, PROTACs
Jie Zhong +4 more
semanticscholar +1 more source
In Vivo Self-Assembly of PROTACs by Bioorthogonal Chemistry for Precision Cancer Therapy.
Angewandte ChemieProteolysis targeting chimeras (PROTACs) hold immense promise for targeted protein degradation; however, challenges such as off-target effects, poor drug-likeness properties, and the "hook effect" remain.
Shaowen Xie +13 more
semanticscholar +1 more source
Development of PROTACs using computational approaches.
TIPS - Trends in Pharmacological SciencesProteolysis-targeting chimeras (PROTACs) are drugs designed to degrade target proteins via the ubiquitin-proteasome system. With the application of computational biology/chemistry technique in drug design, numerous computer-aided drug design and ...
Jingxuan Ge +4 more
semanticscholar +1 more source
Targeted protein degradation by PROTACs
Pharmacology & Therapeutics, 2017Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases driven by the aberrant expression of a disease-causing protein. PROTAC molecules are bifunctional small molecules that simultaneously bind a target protein and an E3-ubiquitin ligase, thus causing ubiquitination and degradation of the ...
Taavi K, Neklesa +2 more
openaire +2 more sources
Degraders Upgraded: The Rise of PROTACs in Haematological Malignancies.
BloodTargeted protein degradation (TPD) is a revolutionary approach to targeted therapy in hematological malignancies that potentially circumvents many constraints of existing small molecule inhibitors. Heterobifunctional proteolysis targets chimeras (PROTACs)
Joshua M. L. Casan, J. Seymour
semanticscholar +1 more source
Photoswitchable PROTACs for Reversible and Spatiotemporal Regulation of NAMPT and NAD.
Angewandte ChemieNicotinamide adenine dinucleotide (NAD+) serves as an essential coenzyme for DNA synthesis and has diverse biological functions. Nicotinamide phosphoribosyltransferase (NAMPT) is the key rate-limiting enzyme involved in NAD+ biosynthesis in mammals ...
Junfei Cheng +5 more
semanticscholar +1 more source
Repurposing AS1411 for constructing ANM-PROTACs.
Cell Chemical BiologyProteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of two ligands joined by a linker, enabling them to simultaneously bind with an E3 ligase and a protein of interest (POI) and trigger proteasomal degradation of the POI.
Xuekun Fu +12 more
semanticscholar +1 more source