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      Dual-Responsive Molecular Probe for Tumor Targeted Imaging and Photodynamic Therapy


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          The precision oncology significantly relies on the development of multifunctional agents to integrate tumor targeting, imaging and therapeutics. In this study, a first small-molecule theranostic probe, RhoSSCy is constructed by conjugating 5′-carboxyrhodamines (Rho) and heptamethine cyanine IR765 (Cy) using a reducible disulfide linker and pH tunable amino-group to realize thiols/pH dual sensing. In vitro experiments verify that RhoSSCy is highly sensitive for quantitative analysis and imaging intracellular pH gradient and biothiols. Furthermore, RhoSSCy shows superb tumor targeted dual-modal imaging via near-infrared fluorescence (NIRF) and photoacoustic (PA). Importantly, RhoSSCy also induces strongly reactive oxygen species for tumor photodynamic therapy (PDT) with robust antitumor activity both in vitro and in vivo. Such versatile small-molecule theranostic probe may be promising for tumor targeted imaging and precision therapy.

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              A molecular imaging primer: modalities, imaging agents, and applications.

              Molecular imaging is revolutionizing the way we study the inner workings of the human body, diagnose diseases, approach drug design, and assess therapies. The field as a whole is making possible the visualization of complex biochemical processes involved in normal physiology and disease states, in real time, in living cells, tissues, and intact subjects. In this review, we focus specifically on molecular imaging of intact living subjects. We provide a basic primer for those who are new to molecular imaging, and a resource for those involved in the field. We begin by describing classical molecular imaging techniques together with their key strengths and limitations, after which we introduce some of the latest emerging imaging modalities. We provide an overview of the main classes of molecular imaging agents (i.e., small molecules, peptides, aptamers, engineered proteins, and nanoparticles) and cite examples of how molecular imaging is being applied in oncology, neuroscience, cardiology, gene therapy, cell tracking, and theranostics (therapy combined with diagnostics). A step-by-step guide to answering biological and/or clinical questions using the tools of molecular imaging is also provided. We conclude by discussing the grand challenges of the field, its future directions, and enormous potential for further impacting how we approach research and medicine.

                Author and article information

                Ivyspring International Publisher (Sydney )
                10 April 2017
                : 7
                : 7
                : 1781-1794
                [1 ]Guangdong Key Laboratory of Nanomedicine, CAS Key Lab of Health Informatics, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China;
                [2 ]University of Chinese Academy of Sciences, Beijing 100049, China;
                [3 ]College of Life Sciences, Hunan Normal University, Changsha 410081, China;
                [4 ]Guangdong Key Laboratory for Research and Development of Natural Drugs, Guangdong Medical University, Dongguan 523808, China;
                [5 ]State Key Laboratory of Chemo/Biosensing and Chemometrics, Hunan University, Changsha 410082, China.
                Author notes
                ✉ Corresponding authors: Ping Gong, E-mail: ping.gong@ 123456siat.ac.cn ; Tel: +86 755 8639 2223. Lintao Cai, E-mail: lt.cai@ 123456siat.ac.cn ; Tel: +86 755 8639 2210.

                *Equal contribution

                Competing Interests: The authors have declared that no competing interest exists.

                © Ivyspring International Publisher

                This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY-NC) license ( https://creativecommons.org/licenses/by-nc/4.0/). See http://ivyspring.com/terms for full terms and conditions.

                Research Paper

                Molecular medicine
                small-molecule theranostic probe,dual-stimuli sensing,nirf/pa imaging,tumor targeting,photodynamic therapy.


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