Results 201 to 210 of about 8,212 (230)

Bifunctional Molecules beyond PROTACs

Journal of Medicinal Chemistry, 2020
Heterobifunctional molecules, which recruit E3 ligases to ubiquitinate a target protein of interest, have found wide application as both biological tools and molecules with the potential to have clinical effects. In their recent paper, Yamazoe et al. report a heterobifunctional molecule that recruits the phosphatase PP1 to promote the dephosphorylation
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Targeted protein degradation by PROTACs

Pharmacology & Therapeutics, 2017
Targeted 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, James D, Winkler, Craig M, Crews   +2 more
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Protecting with PROTAC

Nature Chemical Biology, 2022
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Progress in the controllability technology of PROTAC

European Journal of Medicinal Chemistry
Proteolysis-targeting chimaera (PROTAC) technology functions by directly targeting proteins and catalysing their degradation through an event-driven mode of action, a novel mechanism with significant clinical application prospects for various diseases.
Xin He, Zhibing Weng, Yi Zou
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A PROTAC for ALL

Nature Reviews Drug Discovery, 2022
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Efficient PROTAC-ing: combinational use of PROTACs with signaling pathway inhibitors

Trends in Biochemical Sciences
Targeted protein degradation is an innovative therapeutic modality for the degradation of disease-causing proteins. In a recent report combining high-throughput screening of small-molecule compounds and biochemical analyses, Mori et al. identified certain inhibitors of cellular pathways, such as PARylation and proteostatic pathways, which enhance ...
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PROTACs for prostate cancer

Nature Reviews Urology, 2023
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Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

European Journal of Medicinal Chemistry, 2021
Liyan Cheng, Zhengrong Shen, Wenhai Huang   +2 more
exaly  

Developing bacterial PROTACs

Nature Reviews Drug Discovery, 2022
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The state of the art of PROTAC technologies for drug discovery

European Journal of Medicinal Chemistry, 2022
Liangren Zhang, Zhenming Liu, Ping Xu
exaly