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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >A targeted low molecular weight near-infrared fluorescent probe for prostate cancer.
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A targeted low molecular weight near-infrared fluorescent probe for prostate cancer.

机译：用于前列腺癌的靶向低分子量近红外荧光探针。

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摘要

Prostate-specific membrane antigen (PSMA) remains an active target for imaging and therapeutic applications for prostate cancer. Although radionuclide-based imaging is generally more sensitive and also has been deeply explored, near-infrared fluorescence imaging agents are simple to prepare and compatible with long-term storage conditions. In the present study, a near-infrared fluorescent imaging probe (Cy5.5-CTT-54.2) has been developed by chemical conjugation of Cy5.5N-hydroxysuccinimide ester (Cy5.5-NHS) with a potent PSMA inhibitor CTT-54.2 (IC(50)=144 nM). The probe displays a highly potency (IC(50)=0.55 nM) against PSMA and has demonstrated successful application for specifically labeling PSMA-positive prostate cancer cells in both two and three-dimensional cell culture conditions. These results suggest that the potent, near-infrared Cy5.5-PSMA inhibitor conjugate may be useful for the detection of prostate tumor cells by optical in vivo imaging.
机译：前列腺特异性膜抗原（PSMA）仍然是前列腺癌的成像和治疗应用的活性靶标。 尽管基于放射性核素的成像通常更敏感并且也已经深入探索，但是近红外荧光成像试剂简单地制备和与长期储存条件相容。 在本研究中，通过用效率的PSMA抑制剂CTT-54.2（CY5.5-NHS）的化学缀合而开发了近红外荧光成像探针（CY5.5-CTT-54.2）。 IC（50）= 144nm）。 探针显示对PSMA的高效力（IC（50）= 0.55nm），并证明了在两个和三维细胞培养条件下特别标记PSMA阳性前列腺癌细胞的成功应用。 这些结果表明，有效的近红外Cy5-PSMA抑制剂缀合物可用于通过体内成像检测前列腺肿瘤细胞。

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