Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1.
Animals
Cell Cycle Proteins
/ antagonists & inhibitors
Cell Proliferation
/ drug effects
Drug Discovery
HeLa Cells
Humans
Male
Mice
Mice, Inbred C57BL
Neoplasms
/ drug therapy
Protein Binding
Protein Domains
Protein Kinase Inhibitors
/ chemistry
Protein Serine-Threonine Kinases
/ antagonists & inhibitors
Proto-Oncogene Proteins
/ antagonists & inhibitors
Structure-Activity Relationship
Tissue Distribution
Polo-Like Kinase 1
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
25 11 2020
25 11 2020
Historique:
pubmed:
12
11
2020
medline:
22
1
2021
entrez:
11
11
2020
Statut:
ppublish
Résumé
As a mitotic-specific target widely deregulated in various human cancers, polo-like kinase 1 (Plk1) has been extensively explored for anticancer activity and drug discovery. Although multiple catalytic domain inhibitors were tested in preclinical and clinical studies, their efficacies are limited by dose-limiting cytotoxicity, mainly from off-target cross reactivity. The C-terminal noncatalytic polo-box domain (PBD) of Plk1 has emerged as an attractive target for generating new protein-protein interaction inhibitors. Here, we identified a 1-thioxo-2,4-dihydro-[1,2,4]triazolo[4,3-
Identifiants
pubmed: 33175530
doi: 10.1021/acs.jmedchem.0c01669
pmc: PMC7769008
mid: NIHMS1654399
doi:
Substances chimiques
Cell Cycle Proteins
0
Protein Kinase Inhibitors
0
Proto-Oncogene Proteins
0
Protein Serine-Threonine Kinases
EC 2.7.11.1
Types de publication
Journal Article
Research Support, N.I.H., Intramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
14087-14117Subventions
Organisme : Intramural NIH HHS
ID : ZIA BC005562
Pays : United States
Organisme : Intramural NIH HHS
ID : ZIA BC005708
Pays : United States
Organisme : Intramural NIH HHS
ID : ZIA DK031117
Pays : United States
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