Identification, Characterization, and Optimization of Integrin α_vβ₆-Targeting Peptides from a One-Bead One-Compound (OBOC) Library: Towards the Development of Positron Emission Tomography (PET) Imaging Agents.

ABSTRACT: The current translation of peptides identified through the one-bead one-compound (OBOC) technology into positron emission tomography (PET) imaging agents is a slow process, with a major delay between ligand identification and subsequent lead optimization. This work aims to streamline the development process of ¹⁸F-peptide based PET imaging agents to target the integrin α_vβ₆. By directly identify α_vβ₆⁻targeting peptides from a 9-mer 4-fluorobenzoyl peptide library using the on-bead two-color (OBTC) cell-screening assay, a total of 185 peptide beads were identified and 5 beads sequenced for further evaluation. The lead peptide 1 (VGDLTYLKK(FB), IC₅₀ = 0.45 ± 0.06 μM, 25% stable in serum at 1 h) was further modified at the N-, C-, and bi-term

SUBMITTER: Tang YSC 

PROVIDER: S-EPMC6359284 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature