Small-Molecule Modulators of the ATPase VCP/p97 Affect Specific p97 Cellular Functions.
Adenosine Triphosphatases
/ genetics
Amino Acid Sequence
Binding Sites
Drug Evaluation, Preclinical
Enzyme Inhibitors
/ chemistry
HEK293 Cells
HeLa Cells
Humans
Kinetics
Models, Molecular
Nuclear Proteins
/ genetics
Protein Binding
Protein Domains
Proteolysis
Recombinant Proteins
/ genetics
Small Molecule Libraries
/ chemistry
Structure-Activity Relationship
Journal
ACS chemical biology
ISSN: 1554-8937
Titre abrégé: ACS Chem Biol
Pays: United States
ID NLM: 101282906
Informations de publication
Date de publication:
17 01 2020
17 01 2020
Historique:
pubmed:
4
12
2019
medline:
14
1
2021
entrez:
3
12
2019
Statut:
ppublish
Résumé
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,
Identifiants
pubmed: 31790201
doi: 10.1021/acschembio.9b00832
doi:
Substances chimiques
Enzyme Inhibitors
0
Nuclear Proteins
0
Recombinant Proteins
0
Small Molecule Libraries
0
Adenosine Triphosphatases
EC 3.6.1.-
p97 ATPase
EC 3.6.1.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM