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Á¦¸ñ [Cusabio] PROTAC: HOT ¡°Target Proteins¡± and ¡°E3 Ubiquitin Ligases¡± in Research to Improve Small Mole
ÀÛ¼ºÀÚ abbabio
ÀÛ¼ºÀÏÀÚ 2022-09-07
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Proteolysis Targeting Chimera (PROTAC): A "Revolutionary" Technology in Small Molecule Drug Discovery!

Proteolysis targeting chimeras (PROTAC) as a pioneering new technology for targeted protein degradation, the existing PROTACs consist of three parts: a ligand for recruiting a target protein of interest (POI), a ligand for an E3 ubiquitin ligase, and an appropriate linker. PROTAC boasts overwhelming superiority over small molecule inhibitors, such as targeting non-druggable targets and overcoming drug resistance. It is believed that PROTAC molecular drugs will be a promising technology for cancer drug discovery (Click to Read More about PROTAC).

As of now, PROTAC has been intensively studied in the treatment of tumors, viral infections, and neurodegenerative diseases. A host of pharmaceutical companies puts more strategies on PROTACs to have successful clinical trials, including Roche, Biogen, GSK, Sanofi and others.Remarkably, over 200 targeted protein degraders are currently in the different clinical-trial stages, in which are mainly PROTAC molecules (Click to See PROTAC Clinical Progress).

Here, CUSABIO summarizes popular target proteins and E3 ubiquitin ligases in PROTAC research to help you explore the functions of PROTAC for specific targets or its potential clinical value!

¡Ü Targeted protein products

ABL1AKT2 HOTAR HOTBRD4 HOTBTK HOTCDK2
CDK4DHODHEGFR HOTERK1/2ESR1 HOTESRRA
HDAC6IRAK3KRAS HOTMETAP2PARP1RIPK2
SNCAtauTRIM24

¡Ü E3 ubiquitin ligase related protein products

CDC20 HOTCDH1CIAO1 HOTCRBN HOTDCAF16 HOTHUWE1
MDM2 HOTMIB1PELI1RFWD2/COP1RNF125RNF168
RNF5RNF8SCF/FBW7SCF/Skp2SIAH1SMURF1
SMURF2TRAF6TRIM63TRIM9 HOTUbe3aVHL HOT
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