Results 201 to 210 of about 464,369 (258)

A real-time FRET ubiquitin transfer assay for quantitative characterization of ternary complexes in targeted protein degradation. [PDF]

Cell Rep Methods
Yu CH, Dougherty V, Lv D, Ebadi P, Dubey S, Nayak D, Nayak A, Zhou D, Olsen SK, Ivanov DN.   +9 more
europepmc   +1 more source

Small-molecule degron mimetics for targeted protein degradation. [PDF]

Essays Biochem
Liu X.
europepmc   +1 more source

Modular Assembled Targeting Chimera Enables Multimodal Targeted Protein Degradation

JACS Au
Wentao Zhu, Wenqian Zhang, Yinmiao Wang, Jian Chen, Fang Xu, Jiyan Pang   +5 more
doaj   +1 more source

Targeted Protein Degradation and Metabolic Inhibition as Complementary Therapeutic Strategies: TEAD PROTACs and NAT8L Inhibitors in Oncology. [PDF]

ACS Med Chem Lett
Renner AC, Kargbo RB.
europepmc   +1 more source

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Monomeric Targeted Protein Degraders

Journal of Medicinal Chemistry, 2020
The discovery and development of targeted protein degraders have become important areas of research in the field of medicinal chemistry. Inducing degradation of a target protein presents several advantages relative to simple inhibition including a potential for extended duration of action and more profound pharmacology.
Emily J. Hanan, Jun Liang, Xiaojing Wang, Robert A. Blake, Nicole Blaquiere, Steven T. Staben   +5 more
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Degrading the signal amplifier: ITK as a target for targeted protein degradation

Cell Chemical Biology, 2023
In this issue of Cell Chemical Biology, Jiang and colleagues show for the first time that the Tec kinase ITK can be targeted using PROTAC approaches. This new modality has implications for the treatment of T cell lymphomas, but also potentially for the treatment of T cell-mediated inflammatory diseases, that depend on ITK signaling.
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Targeted protein degradation and the enzymology of degraders

Current Opinion in Chemical Biology, 2018
Targeted protein degradation is an emerging strategy for drug discovery that employs small molecules to catalyze the ubiquitination of target proteins, ultimately causing their degradation by the proteasome. Current degrader designs employ hetero-bivalent molecules to recruit E3 ubiquitin ligases such as VHL, Cereblon, and the IAPs to the target ...
Stewart L, Fisher, Andrew J, Phillips
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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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Targeted protein degradation mechanisms

Drug Discovery Today: Technologies, 2019
Targeted protein degradation mediated by small molecule degraders represents an exciting new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit E3 ubiquitin ligases to the protein of interest and mediate its ubiquitination and subsequent proteolysis by the proteasome.
Yi, Zhang, Christine, Loh, Jesse, Chen, Nello, Mainolfi   +3 more
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Targeted Degradation of Proteins by PROTACs

Current Protocols in Chemical Biology, 2010
AbstractIn recent years, small interference RNAs (siRNAs) have greatly enhanced our understanding of protein functions by allowing knockdown of targeted proteins at the mRNA level. Similarly, in an effort to achieve degradation of targeted proteins at the post‐translational level, chimeric small molecules called “PROTACs” (PROteolysis TArgeting ...
Eun Ryoung, Jang, Wooin, Lee, Kyung Bo, Kim   +2 more
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