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Journal ArticleDOI

p97 Inhibitor CB-5083 Blocks ERAD in Trypanosoma brucei.

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TLDR
An orally bioavailable p97 inhibitor is evaluated, CB-5083, for use in T. brucei and it is suggested that CB- 5083 blocks ERAD upstream of the proteasome, as expected for inhibition of the trypanosomal p97 orthologue TbVCP.
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This article is published in Molecular and Biochemical Parasitology.The article was published on 2020-07-28. It has received 9 citations till now. The article focuses on the topics: P97 Inhibitor CB-5083 & Trypanosoma brucei.

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Citations
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Temporal proteomics reveal specific cell cycle oncoprotein downregulation by p97/VCP inhibition

TL;DR: Ye et al. as mentioned in this paper tracked HCT116 colon cancer cells using temporal proteomics to define the cellular and molecular responses to proteasome and p97 inhibition, and found that proteins specifically dysregulated by two p97 inhibitors are involved in cell cycle control.
Journal ArticleDOI

Temporal proteomics reveal specific cell cycle oncoprotein downregulation by p97/VCP inhibition

TL;DR: In this paper, the authors tracked HCT116 colon cancer cells using temporal proteomics to define the cellular and molecular responses to proteasome and p97 inhibition, and found that proteins specifically dysregulated by two p97 inhibitors are involved in cell cycle control.
Journal ArticleDOI

Potential drug discovery for COVID-19 treatment targeting Cathepsin L using a deep learning-based strategy

TL;DR: In this paper , the authors applied Chemprop, a newly trained directed-message passing deep neural network approach, to identify small molecules and FDA-approved drugs that can block CTSL activity.
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The AAA+ ATPase p97 as a novel parasite and tuberculosis drug target.

TL;DR: In this paper , the authors reviewed the current knowledge on the structure, function, and conservation of AAA+ ATPase p97 in pathogens and discussed the potential of parasite and mycobacterial p97 as a drug target against these pathogens and explore strategies in designing novel inhibitors.
References
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Journal ArticleDOI

Signal integration in the endoplasmic reticulum unfolded protein response

TL;DR: Together, at least three mechanistically distinct arms of the UPR regulate the expression of numerous genes that function within the secretory pathway but also affect broad aspects of cell fate and the metabolism of proteins, amino acids and lipids.
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One step at a time: endoplasmic reticulum-associated degradation

TL;DR: The current understanding of each step during ERAD, with emphasis on the factors that catalyse distinct activities is summarized, to highlight the importance of this pathway.
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Proteasome and p97 mediate mitophagy and degradation of mitofusins induced by Parkin

TL;DR: The Parkin ubiquitin ligase marks the mitofusins Mfn1 and Mfn2 for proteasome-dependent degradation, promoting disposal of damaged mitochondria by preventing their fusion with healthy organelles.

partners transport proteins from the ER into the cytosol

TL;DR: This work proposes that the Cdc48/p97–Ufd1–Npl4 complex extracts proteins from the ER membrane for cytosolic degradation, and demonstrates that it requires the interacting partners Ufd1 and Npl4.
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The AAA ATPase Cdc48/p97 and its partners transport proteins from the ER into the cytosol

TL;DR: In this paper, it was shown that the Cdc48/p97-Ufd1/Npl4 complex can extract proteins from the endoplasmic reticulum for cytosolic degradation.
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