Accelerated Identification of Cell Active KRAS Inhibitory Macrocyclic Peptides using Mixture Libraries and Automated Ligand Identification System (ALIS) Technology
Michael Garrigou, Bérengère Sauvagnat, Ruchia Duggal, Nicole Boo, Pooja Gopal, Jennifer M. Johnston, Anthony W. Partridge, Tomi K. Sawyer, Kaustav Biswas, N. Boyer
Abstract
that inhibited pERK activity in a pancreatic cancer cell line. More broadly, this methodology offers an efficient alternative to accelerate the fastidious hit-to-lead optimization of PPI peptide inhibitors.
Topics & Concepts
ChemistryPeptideKRASComputational biologyPeptide libraryLigand (biochemistry)BiochemistryCombinatorial chemistryStructure–activity relationshipFastidious organismPeptide sequenceIn vitroBiologyMutationReceptorGeneticsBacteriaGeneProtein Kinase Regulation and GTPase SignalingChemical Synthesis and AnalysisMonoclonal and Polyclonal Antibodies Research