Nakhaei Elnaz, Takehara Ko, Sato Hikari, Zai Khadijah, Kishimura Akihiro, Mori Takeshi, Katayama Yoshiki
Graduate School of Systems Life Sciences, Kyushu University.
Department of Chemistry, Faculty of Science, Kyushu University.
Anal Sci. 2018;34(4):501-504. doi: 10.2116/analsci.17P614.
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.
分子大小低于肾脏清除阈值的治疗性肽和诊断剂存在血液循环时间短的问题。在此，我们报告了一种新型的基于肽的配体设计，该配体与人血清白蛋白（HSA）具有很强的结合亲和力，可作为一种标签来延长小分子的血液循环时间。我们设计了带有通过带负电荷的间隔基连接的双烷基的配体。与单烷基化肽相比，这些配体对HSA表现出更高的结合亲和力以及在小鼠血液中的更高保留率。
