Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1.
Animals
Cell Cycle Proteins
/ antagonists & inhibitors
HEK293 Cells
HeLa Cells
Humans
Molecular Docking Simulation
Molecular Structure
Peptides, Cyclic
/ chemical synthesis
Peptidomimetics
/ chemical synthesis
Protein Binding
Protein Domains
Protein Kinase Inhibitors
/ chemical synthesis
Protein Serine-Threonine Kinases
/ antagonists & inhibitors
Proto-Oncogene Proteins
/ antagonists & inhibitors
Structure-Activity Relationship
Zebrafish
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:
10 02 2022
10 02 2022
Historique:
pubmed:
15
1
2022
medline:
23
2
2022
entrez:
14
1
2022
Statut:
ppublish
Résumé
The polo-box domain (PBD) of Plk1 is a promising target for cancer therapeutics. We designed and synthesized novel phosphorylated macrocyclic peptidomimetics targeting PBD based on acyclic phosphopeptide PMQSpTPL. The inhibitory activities of
Identifiants
pubmed: 35029981
doi: 10.1021/acs.jmedchem.1c01359
pmc: PMC10411393
mid: NIHMS1917421
doi:
Substances chimiques
Cell Cycle Proteins
0
Peptides, Cyclic
0
Peptidomimetics
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., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1915-1932Subventions
Organisme : NIEHS NIH HHS
ID : R35 ES028374
Pays : United States
Organisme : Intramural NIH HHS
ID : ZIA BC010681
Pays : United States
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