Accelerated Identification of Cell Active KRAS Inhibitory Macrocyclic Peptides using Mixture Libraries and Automated Ligand Identification System (ALIS) Technology.
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:
14 07 2022
14 07 2022
Historique:
pubmed:
17
6
2022
medline:
16
7
2022
entrez:
16
6
2022
Statut:
ppublish
Résumé
Macrocyclic peptides can disrupt previously intractable protein-protein interactions (PPIs) relevant to oncology targets such as KRAS. Early hits often lack cellular activity and require meticulous improvement of affinity, permeability, and metabolic stability to become viable leads. We have validated the use of the Automated Ligand Identification System (ALIS) to screen oncogenic KRAS
Identifiants
pubmed: 35707970
doi: 10.1021/acs.jmedchem.2c00154
pmc: PMC9289880
doi:
Substances chimiques
Ligands
0
Peptide Library
0
Peptides
0
Proto-Oncogene Proteins p21(ras)
EC 3.6.5.2
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
8961-8974Références
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