Identification of compounds that bind the centriolar protein SAS-6 and inhibit its oligomerization.
Animals
Caenorhabditis elegans
/ drug effects
Caenorhabditis elegans Proteins
/ antagonists & inhibitors
Cell Cycle Proteins
/ antagonists & inhibitors
Centrioles
/ drug effects
High-Throughput Screening Assays
/ methods
Molecular Dynamics Simulation
Protein Conformation
Protein Multimerization
Small Molecule Libraries
/ pharmacology
biophysics
centrosome
inhibitor
ligand design
nuclear magnetic resonance (NMR)
protein-drug interaction
protein-protein interaction
Journal
The Journal of biological chemistry
ISSN: 1083-351X
Titre abrégé: J Biol Chem
Pays: United States
ID NLM: 2985121R
Informations de publication
Date de publication:
25 12 2020
25 12 2020
Historique:
received:
12
06
2020
revised:
26
08
2020
pubmed:
3
9
2020
medline:
26
3
2021
entrez:
3
9
2020
Statut:
ppublish
Résumé
Centrioles are key eukaryotic organelles that are responsible for the formation of cilia and flagella, and for organizing the microtubule network and the mitotic spindle in animals. Centriole assembly requires oligomerization of the essential protein spindle assembly abnormal 6 (SAS-6), which forms a structural scaffold templating the organization of further organelle components. A dimerization interaction between SAS-6 N-terminal "head" domains was previously shown to be essential for protein oligomerization
Identifiants
pubmed: 32873708
pii: S0021-9258(17)50672-9
doi: 10.1074/jbc.RA120.014780
pmc: PMC7939395
pii:
doi:
Substances chimiques
Caenorhabditis elegans Proteins
0
Cell Cycle Proteins
0
SAS-6 protein, C elegans
0
Small Molecule Libraries
0
Banques de données
PDB
['3PYI', '4G79', '3Q0Y', '2Y3V']
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
17922-17934Subventions
Organisme : Wellcome Trust
Pays : United Kingdom
Organisme : Medical Research Council
ID : MR/N009274/1
Pays : United Kingdom
Organisme : Wellcome Trust
ID : 094872/Z/10/Z
Pays : United Kingdom
Organisme : Biotechnology and Biological Sciences Research Council
Pays : United Kingdom
Informations de copyright
© 2020 Busch et al.
Déclaration de conflit d'intérêts
Conflict of interest—The authors declare that they have no conflicts of interest with the contents of this article.
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