具有无偶氮猝灭剂的磷脂酶C可激活探针的非保护基团合成
Nonprotecting Group Synthesis of a Phospholipase C Activatable Probe with an Azo-Free Quencher.
作者信息
Liebov Benjamin K, Arroyo Alejandro D, Rubtsova Natalia I, Osharovich Sofya A, Delikatny E James, Popov Anatoliy V
机构信息
Department of Radiology, University of Pennsylvania, 3620 Hamilton Walk, Philadelphia, Pennsylvania 19104, United States.
出版信息
ACS Omega. 2018 Jun 30;3(6):6867-6873. doi: 10.1021/acsomega.8b00635. Epub 2018 Jun 25.
The near-infrared fluorescent activatable smart probe Pyro-phosphatidylethanolamine (PtdEtn)-QSY was synthesized and observed to selectively fluoresce in the presence of phosphatidylcholine-specific phospholipase C (PC-PLC). PC-PLC is an important biological target as it is known to be upregulated in a variety of cancers, including triple negative breast cancer. Pyro-PtdEtn-QSY features a QSY21 quenching moiety instead of the Black Hole Quencher-3 (BHQ-3) used previously because the latter contains an azo bond, which could lead to biological instability.
合成了近红外荧光可激活智能探针焦磷酸磷脂酰乙醇胺（PtdEtn）-QSY，并观察到其在磷脂酰胆碱特异性磷脂酶C（PC-PLC）存在下选择性地发出荧光。PC-PLC是一个重要的生物学靶点，因为已知它在包括三阴性乳腺癌在内的多种癌症中上调。焦磷酸磷脂酰乙醇胺（Pyro-PtdEtn）-QSY具有QSY21猝灭基团，而不是先前使用的黑洞猝灭剂-3（BHQ-3），因为后者含有偶氮键，这可能导致生物不稳定性。
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