Analytical Sciences

A Dual Alkylated Peptide-ligand Enhances Affinity to Human Serum Albumin

Elnaz NAKHAEI,*1 Ko TAKEHARA,*2 Hikari SATO,*1 Khadijah ZAI,*3 Akihiro KISHIMURA,*1,*3,*4,*5 Takeshi MORI,*1,*3,*4 and Yoshiki KATAYAMA*1,*3,*4,*5,*6,*7,*8

*1 Graduate School of Systems Life Sciences, Kyushu University, 744 Motooka, Nishi, Fukuoka 819-0395, Japan
*2 Department of Chemistry, Faculty of Science, Kyushu University, 744 Motooka, Nishi, Fukuoka 819-0395, Japan
*3 Department of Applied Chemistry, Faculty of Engineering, Kyushu University, 744 Motooka, Nishi, Fukuoka 819-0395, Japan
*4 Center for Future Chemistry, Kyushu University, 744 Motooka, Nishi, Fukuoka 819-0395, Japan
*5 International Research Center for Molecular Systems, Kyushu University, 744 Motooka, Nishi, Fukuoka 819-0395, Japan
*6 Center for Advanced Medical Innovation, Kyushu University, 3-1-1 Maidashi, Higashi, Fukuoka 812-8582, Japan
*7 Innovation Center for Medical Redox Navigation, Kyushu University, 744 Motooka, Nishi, Fukuoka 819-0395, Japan
*8 Department of Biomedical Engineering, Chung Yuan Christian University, 200 Chung Pei Rd., Chung Li, 32023 ROC, Taiwan

Therapeutic peptides and diagnostic agents with their molecular size below the renal clearance threshold suffer from short blood circulation time. Here, we report a novel design of peptide-based ligand with a strong binding affinity to human serum albumin (HSA), which can be used as a tag to extend the blood circulation of small-size molecules. We designed ligands with dual alkyl groups connected with a negatively charged spacer. The ligands showed both higher binding affinity to HSA and a higher retention in mice blood than that of a single alkylated peptide.

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