Accelerated Identification of Cell Active KRAS Inhibitory Macrocyclic Peptides using Mixture Libraries and Automated Ligand Identification System (ALIS) Technology

Autor: Michael Garrigou, Bérengère Sauvagnat, Ruchia Duggal, Nicole Boo, Pooja Gopal, Jennifer M. Johnston, Anthony Partridge, Tomi Sawyer, Kaustav Biswas, Nicolas Boyer
Rok vydání: 2022
Předmět:
Zdroj: Journal of medicinal chemistry. 65(13)
ISSN: 1520-4804
Popis: 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
Databáze: OpenAIRE