Discovery of peptide inhibitors targeting human programmed death 1 (PD-1) receptor

摘要: // Qiao Li 1, * , Lina Quan Jiankun Lyu 1 Zenghui He Xia Wang Jiajia Meng Zhenjiang Zhao Lili Zhu Xiaofeng Liu Honglin State Key Laboratory of Bioreactor Engineering, Shanghai New Drug Design, School Pharmacy, East China University Science and Technology, Shanghai, 200237, These Authors contributed equally to this work Correspondence to: Zhu, email: zhulfl@ecust.edu.cn Liu, xxffliu@gmail.com Li, hlli@ecust.edu.cn Keywords: immunotherapy, human programmed death peptide inhibitor, protein-protein interactions (PPIs), de novo design Received: June 06, 2016      Accepted: July 29, Published: August 12, 2016 ABSTRACT Blocking the interaction (hPD-1) its ligand hPD-L1 has been a promising immunotherapy in cancer treatment. In paper, using computational method, we designed several hPD-1 binding peptides. The most potent Ar5Y_4 showed KD value 1.38 ± 0.39 μM, comparable affinity cognate hPD-L1. A Surface Plasmon Resonance (SPR) competitive assay result indicated that could inhibit hPD-1/hPD-L1. Moreover, restore function Jurkat T cells which had suppressed by stimulated HCT116 cells. Peptides described paper provide biologic candidates for or diagnostics.