Results 11 to 20 of about 211,577 (291)
PROTACs: A novel strategy for cancer drug discovery and development
MedComm, 2023 Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists of three components: a small molecule that binds to a target protein, an ...
Xin Han, Yi Sun
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CUL4-DDB1-CDT2 E3 Ligase Regulates the Molecular Clock Activity by Promoting Ubiquitination-Dependent Degradation of the Mammalian CRY1. [PDF]
PLoS ONE, 2015 The CUL4-DDB1 E3 ligase complex serves as a critical regulator in various cellular processes, including cell proliferation, DNA damage repair, and cell cycle progression.
Xin Tong +6 more
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The EHEC type III effector NleL is an E3 ubiquitin ligase that modulates pedestal formation. [PDF]
PLoS ONE, 2011 Enterohemorrhagic Escherichia coli (EHEC) O157:H7 causes hemorrhagic colitis and may result in potentially fatal hemolytic uremia syndrome in humans. EHEC colonize the intestinal mucosa and promote the formation of actin-rich pedestals via translocated ...
Heather Piscatelli +7 more
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Exploring the target scope of KEAP1 E3 ligase-based PROTACs.
Cell Chemical Biology, 2022 Targeted protein degradation (TPD) uses small molecules to recruit E3 ubiquitin ligases into the proximity of proteins of interest, inducing ubiquitination-dependent degradation.
Guangyan Du +18 more
semanticscholar +1 more source
An E3 ligase guide to the galaxy of small-molecule-induced protein degradation.
Cell Chemical Biology, 2021 Induced protein degradation accomplishes elimination, rather than inhibition, of pathological proteins. Key to the success of this novel therapeutic modality is the modification of proteins with ubiquitin chains, which is brought about by molecular glues
P. Jevtić, Diane L. Haakonsen, M. Rapé
semanticscholar +1 more source
Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation.
Journal of the American Chemical Society, 2021 Proteolysis targeting chimeras (PROTACs) represent a new class of promising therapeutic modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading to selective degradation of the target proteins. However, only a very limited
Jieli Wei +15 more
semanticscholar +1 more source
Hepatology Communications, 2021 We aimed to identify a microRNA (miRNA)‐E3 ubiquitin ligase regulatory network for protein substrates enriched in cell death pathways and investigate the underlying molecular mechanisms in alcohol‐associated hepatitis (AH).
Xiude Fan +8 more
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Nature Communications, 2021 Ubiquitination is one of the most prevalent protein posttranslational modifications. Here, we show that E3 ligase Nedd4l positively regulates antiviral immunity by catalyzing K29-linked cysteine ubiquitination of TRAF3. Deficiency of Nedd4l significantly
Peng Gao +17 more
semanticscholar +1 more source
MDM2 E3 ligase activity is essential for p53 regulation and cell cycle integrity.
PLoS Genetics, 2022 MDM2 and MDM4 are key regulators of p53 and function as oncogenes when aberrantly expressed. MDM2 and MDM4 partner to suppress p53 transcriptional transactivation and polyubiquitinate p53 for degradation.
Meenalakshmi Chinnam +8 more
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Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders
Nature Chemical Biology, 2022 Targeted protein degradation is a novel pharmacology established by drugs that recruit target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target, different E3 interfaces are critically involved, thus forming defined ...
Alexander Hanzl +10 more
semanticscholar +1 more source