In vitro selection of highly N-alkylated cyclic peptides for targeting intracellular protein-protein interactions
Year: 2024
Type: conference-abstract
Abstract: Classical Peptide Drug Discovery poor bio-activity membrane permeable metabolically stable Drug potent bio-activity membrane permeable metabolically stable Undrug-like hit potent bio-activity poor membrane permeability poor metabolic stability Small conformational change Drug-like hit moderate bio-activity (potentially) membrane permeable metabolically stable Conformational change Modification without scaffold hopping Conclusion Cyclic peptides were generated from our designated library contained 5-7 NAAs in 11-residue residues for KRAS. AP8784 from our library afforded orally available LUNA18 without scaffold hopping, which supports the validity of our concept.In vitro selection of highly N-alkylated cyclic peptides for targeting intracellular protein-protein interactions
Source: European Peptide Symposium (EPS)
Authors: Takeo Iida, Atsushi Ohta, Yusuke Yamagishi, Tetsuo Kojima, Hitoshi Iikura
Institution: Chugai Pharmaceutical Co., Ltd. (Japan)
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: bronze
OpenAlex ID: W4402672803