Saikiran Maryala, Sato Daisuke, Pandey Shyam S, Hayase Shuzi, Kato Tamaki
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, 2-4 Hibikino, Wakamatsu, Kitakyushu 808-0196, Japan.
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, 2-4 Hibikino, Wakamatsu, Kitakyushu 808-0196, Japan.
Bioorg Med Chem Lett. 2017 Sep 1;27(17):4024-4029. doi: 10.1016/j.bmcl.2017.07.057. Epub 2017 Jul 22.
Extended wavelength analyte-responsive fluorescent probes are highly desired for the imaging applications owing to their deep tissue penetration, and minimum interference from autofluorescence by biomolecules. Near infra-red (NIR) sensitive and self-quenching fluorescent probe based on the dye-peptide conjugate (SQ 1 PC) was designed and synthesized by facile and efficient one-pot synthetic route for the detection of Elastase activity. In the phosphate buffer solution, there was an efficient quenching of fluorescence of SQ 1 PC (86%) assisted by pronounced dye-dye interaction due to H-aggregate formation. Efficient and fast recovery of this quenched fluorescence of SQ 1 PC (> 50% in 30s) was observed on hydrolysis of this peptide-dye conjugate by elastase enzyme. Presently designed NIR sensitive self-quenching substrate offers the potential application for the detection of diseases related to proteases by efficient and fast detection of their activities.
由于其具有深层组织穿透能力以及生物分子自发荧光的干扰最小,扩展波长分析物响应型荧光探针在成像应用中备受青睐。基于染料 - 肽共轭物(SQ 1 PC)设计并合成了一种近红外(NIR)敏感且自猝灭的荧光探针,通过简便高效的一锅合成路线用于检测弹性蛋白酶活性。在磷酸盐缓冲溶液中,由于形成H - 聚集体,显著的染料 - 染料相互作用辅助下,SQ 1 PC的荧光发生了有效猝灭(86%)。在弹性蛋白酶水解该肽 - 染料共轭物时,观察到SQ 1 PC这种猝灭荧光的高效快速恢复(30秒内> 50%)。目前设计的近红外敏感自猝灭底物通过高效快速检测蛋白酶的活性,为与蛋白酶相关疾病的检测提供了潜在应用。