publication . Other literature type . Article . 2019

Small-Molecule Modulators of the ATPase VCP/p97 Affect Specific p97 Cellular Functions

Ainoa Figuerola-Conchas; Jacques Saarbach; Jean-Pierre Daguer; Adeline Cieren; Sofia Barluenga; Nicolas Winssinger; Monica Gotta;
Open Access
  • Published: 10 Nov 2019
  • Publisher: American Chemical Society (ACS)
  • Country: Switzerland
Abstract
ABSTRACT: VCP/p97 belongs to the AAA+ ATPase family and has an essential role in several cellular processes ranging from cell division to protein homeostasis. Compounds targeting p97 inhibit the main ATPase domain and cause cell death. Here, using PNA-encoded chemical libraries, we have identified two small molecules that target the regulatory domain of p97, comprising the N-terminal and the D1 ATPase domains, and do not cause cell death. One molecule, <strong>NW1028</strong>, inhibits the degradation of a p97-dependent reporter, whereas the other, <strong>NW1030</strong>, increases it. ATPase assays show that <strong>NW1028</strong> and <strong>NW1030</strong> ...
Subjects
free text keywords: Molecular Medicine, Biochemistry, General Medicine, ddc:540, ddc:612, Chemistry, Small molecule, Protein Homeostasis, Programmed cell death, Cell division, ATPase, biology.protein, biology, Binding site, Cell biology, Cellular functions, HeLa, biology.organism_classification
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ZENODO
Article . 2019
Provider: ZENODO
Zenodo
Other literature type . 2019
Provider: Datacite
Zenodo
Other literature type . 2019
Provider: Datacite
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