New Class of Drug Modalities: Directed Evolution of a De Novo Designed Helix–Loop–Helix Peptide to Bind VEGF for Tumor Growth Inhibition

Autor: Masataka Michigami, Tharanga M. R. Ramanayake Mudiyanselage, Miho Suzuki, Hirotsugu Ishizako, Kunpei Notsu, Kikuya Sugiura, Ikuo Fujii
Rok vydání: 2022
Předmět:
Zdroj: ACS Chemical Biology. 17:647-653
ISSN: 1554-8937
1554-8929
DOI: 10.1021/acschembio.1c00940
Popis: As a small affinity molecule to serve as an alternative to antibodies, we have developed a conformationally constrained peptide with a de novo designed helix-loop-helix (HLH) scaffold. To evaluate its potential for biomedical applications, we performed directed evolution of HLH peptides to obtain an inhibitor for vascular endothelial growth factor-A (VEGF). A phage-displayed library of HLH peptides was constructed and screened against VEGF, giving the peptide VS42 that inhibits the VEGF/VEGF receptor-2 interaction (IC
Databáze: OpenAIRE