Results 21 to 30 of about 823,777 (226)

Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets. [PDF]

J Am Chem Soc, 2022
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for degrading disease-causing proteins. While many PROTACs have been developed for numerous protein targets, current small-molecule PROTAC approaches cannot target undruggable proteins that do not have small-molecule binders.
Xiong Y, Zhong Y, Yim H, Yang X, Park KS, Xie L, Poulikakos PI, Han X, Xiong Y, Chen X, Liu J, Jin J.   +11 more
europepmc   +3 more sources

Proteolysis targeting chimeras (PROTACs) in cancer therapy [PDF]

Journal of Experimental & Clinical Cancer Research, 2020
AbstractExploitation of the protein degradation machinery as a therapeutic strategy to degrade oncogenic proteins is experiencing revolutionary advances with the development of proteolysis targeting chimeras (PROTACs). PROTACs are heterobifunctional structures consisting of a ligand that binds a protein to be degraded and a ligand for an E3 ubiquitin ...
Alberto Ocaña, Atanasio Pandiella
openaire   +5 more sources

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC). [PDF]

Chem Commun (Camb), 2017
In this manuscript, for the first time, we report the synthesis of a PROTAC that selectively degrades cyclin dependent kinase 9 (CDK9).
Robb CM, Contreras JI, Kour S, Taylor MA, Abid M, Sonawane YA, Zahid M, Murry DJ, Natarajan A, Rana S.   +9 more
europepmc   +4 more sources

Proteolysis Targeting Chimeras (PROTACs)

ACS Pharmacology and Translational Science, 2022
Targeted protein degradation (TPD) is a promising therapeutic modality to modulate protein levels and its application promises to reduce the "undruggable"proteome. Among TPD strategies, Proteolysis TArgeting Chimera (PROTAC) technology has shown a tremendous potential with attractive advantages when compared to the inhibition of the same target.
Ruffilli, Camilla, Roth, Sascha, Rodrigo, Monica, Boyd, Helen, Zelcer, Noam, Moreau, Kevin   +5 more
openaire   +3 more sources

Targeted protein degradation in cancers: Orthodox PROTACs and beyond

The Innovation, 2023
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology can be used to target proteins by hijacking the ubiquitin-proteasome ...
Jin Li, Xinxin Chen, Aiping Lu, Chao Liang   +3 more
doaj   +1 more source

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Molecular Cancer, 2022
AbstractProteolysis-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 degradation of target protein by the ubiquitin-proteasome system. PROTAC has emerged as a promising
Xinyi Li, Wenchen Pu, Qingquan Zheng, Min Ai, Song Chen, Yong Peng   +5 more
openaire   +3 more sources

Cell Morphological Profiling Enables High-Throughput Screening for PROteolysis TArgeting Chimera (PROTAC) Phenotypic Signature. [PDF]

ACS Chem Biol, 2022
PROteolysis TArgeting Chimeras (PROTACs) use the ubiquitin–proteasome system to degrade a protein of interest for therapeutic benefit. Advances made in targeted protein degradation technology have been remarkable, with several molecules having moved into
Trapotsi MA, Mouchet E, Williams G, Monteverde T, Juhani K, Turkki R, Miljković F, Martinsson A, Mervin L, Pryde KR, Müllers E, Barrett I, Engkvist O, Bender A, Moreau K.   +14 more
europepmc   +2 more sources

Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers

Nature Communications, 2022
SMARCA2 has been identified as a synthetic lethal target in SMARCA4 mutated tumors, however, homology between the two has hindered the development of selective SMARCA2 inhibitors.
Jennifer Cantley, Xiaofen Ye, Emma Rousseau, Tom Januario, Brian D. Hamman, Christopher M. Rose, Tommy K. Cheung, Trent Hinkle, Leofal Soto, Connor Quinn, Alicia Harbin, Elizabeth Bortolon, Xin Chen, Roy Haskell, Eva Lin, Shang-Fan Yu, Geoff Del Rosario, Emily Chan, Debra Dunlap, Hartmut Koeppen, Scott Martin, Mark Merchant, Matt Grimmer, Fabio Broccatelli, Jing Wang, Jennifer Pizzano, Peter S. Dragovich, Michael Berlin, Robert L. Yauch   +28 more
doaj   +1 more source

PROTACs in gastrointestinal cancers

Molecular Therapy: Oncolytics, 2022
Proteolysis targeting chimera (PROTAC) presents a powerful strategy for targeted protein degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase ligand covalently linked to a protein of interest (POI) via a linker.
Yu Chen, Qingfan Yang, Jinrun Xu, Liyao Tang, Yan Zhang, Fukuan Du, Yueshui Zhao, Xu Wu, Mingxing Li, Jing Shen, Ruilin Ding, Hongying Cao, Wanping Li, Xiaobing Li, Meijuan Chen, Zhigui Wu, Chi Hin Cho, Yu Du, Qinglian Wen, Zhangang Xiao   +19 more
doaj   +1 more source

Discovery of E3 Ligase Ligands for Target Protein Degradation

Molecules, 2022
Target protein degradation has emerged as a promising strategy for the discovery of novel therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a cellular ubiquitin-dependent proteolysis system for the efficient ...
Jaeseok Lee, Youngjun Lee, Young Mee Jung, Ju Hyun Park, Hyuk Sang Yoo, Jongmin Park   +5 more
doaj   +1 more source