A targeted low molecular weight near-infrared fluorescent probe for prostate cancer.
A targeted low molecular weight near-infrared fluorescent probe for prostate cancer.
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DOI：
10.1016/j.bmcl.2010.09.057
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发表时间：
2010-12-01
影响因子：
2.7
通讯作者：
Berkman, Clifford E.
中科院分区：
文献类型：
--
作者：
Liu, Tiancheng;Wu, Lisa Y.;Hopkins, Mark R.;Choi, Joseph K.;Berkman, Clifford E.
前列腺特异性膜抗原（PSMA）仍然是前列腺癌成像和治疗应用的活性靶标。虽然基于放射性核素的成像通常更灵敏，并且已经被深入探索，但近红外荧光成像剂制备简单，并且与长期储存条件相容。在本研究中，通过Cy5.5 N-羟基琥珀酰亚胺酯（Cy5.5-NHS）与有效的PSMA抑制剂CTT-54.2（IC 50 = 144 nM）的化学缀合开发了近红外荧光成像探针（Cy5.5-CTT-54.2）。该探针显示出对PSMA的高效力（IC 50 = 0.55 nM），并已证明在二维和三维细胞培养条件下成功应用于特异性标记PSMA阳性前列腺癌细胞。这些结果表明，有效的近红外Cy5.5-PSMA抑制剂缀合物可用于通过光学体内成像检测前列腺肿瘤细胞。
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 Cy5.5 N-hydroxysuccinimide ester (Cy5.5-NHS) with a potent PSMA inhibitor CTT-54.2 (IC50 = 144 nM). The probe displays a highly potency (IC50 = 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.
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影响因子：
4.7
作者：
Mujumdar, SR;Mujumdar, RB;Waggoner, AS
通讯作者：
Waggoner, AS
影响因子：
11.5
作者：
Morris, Michael J.;Pandit-Taskar, Neeta;Scher, Howard I.
通讯作者：
Scher, Howard I.
DOI：
10.2217/fon.09.109
发表时间：
2009-11
期刊：
Future oncology (London, England)
影响因子：
--
作者：
Kosaka N;Ogawa M;Choyke PL;Kobayashi H
通讯作者：
Kobayashi H
影响因子：
2.8
作者：
Liu, Tiancheng;Wu, Lisa Y.;Choi, Joseph K.;Berkman, Clifford E.
通讯作者：
Berkman, Clifford E.
DOI：
10.1016/j.bbrc.2009.10.017
发表时间：
2009-12-18
影响因子：
3.1
作者：
Chen, Ying;Dhara, Surajit;Banerjee, Sangeeta Ray;Byun, Youngjoo;Pullambhatla, Mrudula;Mease, Ronnie C.;Pomper, Martin G.
通讯作者：
Pomper, Martin G.