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Open AccessArticle [¹⁸F]-Fluorinated Carboplatin and [¹¹¹In]-Liposome for Image-Guided Drug Delivery

by Narottam Lamichhane, Gajanan K. Dewkar, Gobalakrishnan Sundaresan, Rebecca N. Mahon and Jamal Zweit

Int. J. Mol. Sci. 2017, 18(5), 1079; doi:10.3390/ijms18051079

Received: 6 March 2017 / Revised: 2 May 2017 / Accepted: 8 May 2017 / Published: 18 May 2017

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Abstract

Radiolabeled liposomes have been employed as diagnostic tools to monitor in vivo distribution of liposomes in real-time, which helps in optimizing the therapeutic efficacy of the liposomal drug delivery. This work utilizes the platform of [¹¹¹In]-Liposome as a drug delivery vehicle,

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Radiolabeled liposomes have been employed as diagnostic tools to monitor in vivo distribution of liposomes in real-time, which helps in optimizing the therapeutic efficacy of the liposomal drug delivery. This work utilizes the platform of [¹¹¹In]-Liposome as a drug delivery vehicle, encapsulating a novel ¹⁸F-labeled carboplatin drug derivative ([¹⁸F]-FCP) as a dual-molecular imaging tool as both a radiolabeled drug and radiolabeled carrier. The approach has the potential for clinical translation in individual patients using a dual modal approach of clinically-relevant radionuclides of ¹⁸F positron emission tomography (PET) and ¹¹¹In single photon emission computed tomography (SPECT). [¹¹¹In]-Liposome was synthesized and evaluated in vivo by biodistribution and SPECT imaging. The [¹⁸F]-FCP encapsulated [¹¹¹In]-Liposome nano-construct was investigated, in vivo, using an optimized dual-tracer PET and SPECT imaging in a nude mouse. The biodistribution data and SPECT imaging showed spleen and liver uptake of [¹¹¹In]-Liposome and the subsequent clearance of activity with time. Dual-modality imaging of [¹⁸F]-FCP encapsulated [¹¹¹In]-Liposome showed significant uptake in liver and spleen in both PET and SPECT images. Qualitative analysis of SPECT images and quantitative analysis of PET images showed the same pattern of activity during the imaging period and demonstrated the feasibility of dual-tracer imaging of a single dual-labeled nano-construct. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessArticle The Mechanisms and Biomedical Applications of an NIR BODIPY-Based Switchable Fluorescent Probe

by Bingbing Cheng, Venugopal Bandi, Shuai Yu, Francis D’Souza, Kytai T. Nguyen, Yi Hong, Liping Tang and Baohong Yuan

Int. J. Mol. Sci. 2017, 18(2), 384; doi:10.3390/ijms18020384

Received: 10 November 2016 / Revised: 31 December 2016 / Accepted: 26 January 2017 / Published: 11 February 2017

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Abstract

Highly environment-sensitive fluorophores have been desired for many biomedical applications. Because of the noninvasive operation, high sensitivity, and high specificity to the microenvironment change, they can be used as excellent probes for fluorescence sensing/imaging, cell tracking/imaging, molecular imaging for cancer, and so on

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Highly environment-sensitive fluorophores have been desired for many biomedical applications. Because of the noninvasive operation, high sensitivity, and high specificity to the microenvironment change, they can be used as excellent probes for fluorescence sensing/imaging, cell tracking/imaging, molecular imaging for cancer, and so on (i.e., polarity, viscosity, temperature, or pH measurement). In this work, investigations of the switching mechanism of a recently reported near-infrared environment-sensitive fluorophore, ADP(CA)₂, were conducted. Besides, multiple potential biomedical applications of this switchable fluorescent probe have been demonstrated, including wash-free live-cell fluorescence imaging, in vivo tissue fluorescence imaging, temperature sensing, and ultrasound-switchable fluorescence (USF) imaging. The fluorescence of the ADP(CA)₂ is extremely sensitive to the microenvironment, especially polarity and viscosity. Our investigations showed that the fluorescence of ADP(CA)₂ can be switched on by low polarity, high viscosity, or the presence of protein and surfactants. In wash-free live-cell imaging, the fluorescence of ADP(CA)₂ inside cells was found much brighter than the dye-containing medium and was retained for at least two days. In all of the fluorescence imaging applications conducted in this study, high target-to-noise (>5-fold) was achieved. In addition, a high temperature sensitivity (73-fold per Celsius degree) of ADP(CA)₂-based temperature probes was found in temperature sensing. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessArticle A Dual-Modality System for Both Multi-Color Ultrasound-Switchable Fluorescence and Ultrasound Imaging

by Jayanth Kandukuri, Shuai Yu, Bingbing Cheng, Venugopal Bandi, Francis D’Souza, Kytai T. Nguyen, Yi Hong and Baohong Yuan

Int. J. Mol. Sci. 2017, 18(2), 323; doi:10.3390/ijms18020323

Received: 25 October 2016 / Revised: 29 December 2016 / Accepted: 24 January 2017 / Published: 4 February 2017

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Abstract

Simultaneous imaging of multiple targets (SIMT) in opaque biological tissues is an important goal for molecular imaging in the future. Multi-color fluorescence imaging in deep tissues is a promising technology to reach this goal. In this work, we developed a dual-modality imaging system

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Simultaneous imaging of multiple targets (SIMT) in opaque biological tissues is an important goal for molecular imaging in the future. Multi-color fluorescence imaging in deep tissues is a promising technology to reach this goal. In this work, we developed a dual-modality imaging system by combining our recently developed ultrasound-switchable fluorescence (USF) imaging technology with the conventional ultrasound (US) B-mode imaging. This dual-modality system can simultaneously image tissue acoustic structure information and multi-color fluorophores in centimeter-deep tissue with comparable spatial resolutions. To conduct USF imaging on the same plane (i.e., x-z plane) as US imaging, we adopted two 90°-crossed ultrasound transducers with an overlapped focal region, while the US transducer (the third one) was positioned at the center of these two USF transducers. Thus, the axial resolution of USF is close to the lateral resolution, which allows a point-by-point USF scanning on the same plane as the US imaging. Both multi-color USF and ultrasound imaging of a tissue phantom were demonstrated. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessArticle In Vivo Follow-up of Brain Tumor Growth via Bioluminescence Imaging and Fluorescence Tomography

by Coralie Genevois, Hugues Loiseau and Franck Couillaud

Int. J. Mol. Sci. 2016, 17(11), 1815; doi:10.3390/ijms17111815

Received: 29 August 2016 / Revised: 27 September 2016 / Accepted: 21 October 2016 / Published: 31 October 2016

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Abstract

Reporter gene-based strategies are widely used in experimental oncology. Bioluminescence imaging (BLI) using the firefly luciferase (Fluc) as a reporter gene and d-luciferin as a substrate is currently the most widely employed technique. The present paper compares the performances of BLI imaging

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Reporter gene-based strategies are widely used in experimental oncology. Bioluminescence imaging (BLI) using the firefly luciferase (Fluc) as a reporter gene and d-luciferin as a substrate is currently the most widely employed technique. The present paper compares the performances of BLI imaging with fluorescence imaging using the near infrared fluorescent protein (iRFP) to monitor brain tumor growth in mice. Fluorescence imaging includes fluorescence reflectance imaging (FRI), fluorescence diffuse ^optical tomography (fDOT), and fluorescence molecular Imaging (FMT^®). A U87 cell line was genetically modified for constitutive expression of both the encoding Fluc and iRFP reporter genes and assayed for cell, subcutaneous tumor and brain tumor imaging. On cultured cells, BLI was more sensitive than FRI; in vivo, tumors were first detected by BLI. Fluorescence of iRFP provided convenient tools such as flux cytometry, direct detection of the fluorescent protein on histological slices, and fluorescent tomography that allowed for 3D localization and absolute quantification of the fluorescent signal in brain tumors. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessArticle Assessment of Amino Acid/Drug Transporters for Renal Transport of [¹⁸F]Fluciclovine (anti-[¹⁸F]FACBC) in Vitro

by Masahiro Ono, Atsumi Baden, Hiroyuki Okudaira, Masato Kobayashi, Keiichi Kawai, Shuntaro Oka and Hirokatsu Yoshimura

Int. J. Mol. Sci. 2016, 17(10), 1730; doi:10.3390/ijms17101730

Received: 28 July 2016 / Revised: 14 September 2016 / Accepted: 8 October 2016 / Published: 14 October 2016

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Abstract

[¹⁸F]Fluciclovine (trans-1-amino-3-[¹⁸F]fluorocyclobutanecarboxylic acid; anti-[¹⁸F]FACBC), a positron emission tomography tracer used for the diagnosis of recurrent prostate cancer, is transported via amino acid transporters (AATs) with high affinity (K_m: 97–230 μM). However,

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[¹⁸F]Fluciclovine (trans-1-amino-3-[¹⁸F]fluorocyclobutanecarboxylic acid; anti-[¹⁸F]FACBC), a positron emission tomography tracer used for the diagnosis of recurrent prostate cancer, is transported via amino acid transporters (AATs) with high affinity (K_m: 97–230 μM). However, the mechanism underlying urinary excretion is unknown. In this study, we investigated the involvement of AATs and drug transporters in renal [¹⁸F]fluciclovine reuptake. [¹⁴C]Fluciclovine (trans-1-amino-3-fluoro[1-¹⁴C]cyclobutanecarboxylic acid) was used because of its long half-life. The involvement of AATs in [¹⁴C]fluciclovine transport was measured by apical-to-basal transport using an LLC-PK1 monolayer as model for renal proximal tubules. The contribution of drug transporters herein was assessed using vesicles/cells expressing the drug transporters P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), multidrug resistance-associated protein 4 (MRP4), organic anion transporter 1 (OAT1), organic anion transporter 3 (OAT3) , organic cation transporter 2 (OCT2), organic anion transporting polypeptide 1B1 (OATP1B1), and organic anion transporting polypeptide 1B3 (OATP1B3). The apical-to-basal transport of [¹⁴C]fluciclovine was attenuated by l-threonine, the substrate for system alanine-serine-cysteine (ASC) AATs. [¹⁴C]Fluciclovine uptake by drug transporter-expressing vesicles/cells was not significantly different from that of control vesicles/cells. Fluciclovine inhibited P-gp, MRP4, OAT1, OCT2, and OATP1B1 (IC₅₀ > 2.95 mM). Therefore, system ASC AATs may be partly involved in the renal reuptake of [¹⁸F]fluciclovine. Further, given that [¹⁸F]fluciclovine is recognized as an inhibitor with millimolar affinity for the tested drug transporters, slow urinary excretion of [¹⁸F]fluciclovine may be mediated by system ASC AATs, but not by drug transporters. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessArticle MALDI Mass Spectrometry Imaging Reveals Decreased CK5 Levels in Vulvar Squamous Cell Carcinomas Compared to the Precursor Lesion Differentiated Vulvar Intraepithelial Neoplasia

by Chao Zhang, Georgia Arentz, Lyron Winderbaum, Noor A. Lokman, Manuela Klingler-Hoffmann, Parul Mittal, Christopher Carter, Martin K. Oehler and Peter Hoffmann

Int. J. Mol. Sci. 2016, 17(7), 1088; doi:10.3390/ijms17071088

Received: 10 May 2016 / Revised: 24 June 2016 / Accepted: 30 June 2016 / Published: 8 July 2016

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Abstract

Vulvar cancer is the fourth most common gynecological cancer worldwide. However, limited studies have been completed on the molecular characterization of vulvar squamous cell carcinoma resulting in a poor understanding of the disease initiation and progression. Analysis and early detection of the precursor

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Vulvar cancer is the fourth most common gynecological cancer worldwide. However, limited studies have been completed on the molecular characterization of vulvar squamous cell carcinoma resulting in a poor understanding of the disease initiation and progression. Analysis and early detection of the precursor lesion of HPV-independent vulvar squamous cell carcinoma (VSCC), differentiated vulvar intraepithelial neoplasia (dVIN), is of great importance given dVIN lesions have a high level of malignant potential. Here we present an examination of adjacent normal vulvar epithelium, dVIN, and VSCC from six patients by peptide Matrix-assisted laser desorption/ionization Mass Spectrometry Imaging (MALDI-MSI). The results reveal the differential expression of multiple peptides from the protein cytokeratin 5 (CK5) across the three vulvar tissue types. The difference observed in the relative abundance of CK5 by MALDI-MSI between the healthy epithelium, dVIN, and VSCC was further analyzed by immunohistochemistry (IHC) in tissue from eight VSCC patients. A decrease in CK5 immunostaining was observed in the VSCC compared to the healthy epithelium and dVIN. These results provide an insight into the molecular fingerprint of the vulvar intraepithelial neoplasia that appears to be more closely related to the healthy epithelium than the VSCC. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Review

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Open AccessReview Theranostic Probes for Targeting Tumor Microenvironment: An Overview

by Musafar Gani Sikkandhar, Anu Maashaa Nedumaran, Roopa Ravichandar, Satnam Singh, Induja Santhakumar, Zheng Cong Goh, Sachin Mishra, Govindaraju Archunan, Balázs Gulyás and Parasuraman Padmanabhan

Int. J. Mol. Sci. 2017, 18(5), 1036; doi:10.3390/ijms18051036

Received: 16 April 2017 / Revised: 6 May 2017 / Accepted: 8 May 2017 / Published: 11 May 2017

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Abstract

Long gone is the time when tumors were thought to be insular masses of cells, residing independently at specific sites in an organ. Now, researchers gradually realize that tumors interact with the extracellular matrix (ECM), blood vessels, connective tissues, and immune cells in

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Long gone is the time when tumors were thought to be insular masses of cells, residing independently at specific sites in an organ. Now, researchers gradually realize that tumors interact with the extracellular matrix (ECM), blood vessels, connective tissues, and immune cells in their environment, which is now known as the tumor microenvironment (TME). It has been found that the interactions between tumors and their surrounds promote tumor growth, invasion, and metastasis. The dynamics and diversity of TME cause the tumors to be heterogeneous and thus pose a challenge for cancer diagnosis, drug design, and therapy. As TME is significant in enhancing tumor progression, it is vital to identify the different components in the TME such as tumor vasculature, ECM, stromal cells, and the lymphatic system. This review explores how these significant factors in the TME, supply tumors with the required growth factors and signaling molecules to proliferate, invade, and metastasize. We also examine the development of TME-targeted nanotheranostics over the recent years for cancer therapy, diagnosis, and anticancer drug delivery systems. This review further discusses the limitations and future perspective of nanoparticle based theranostics when used in combination with current imaging modalities like Optical Imaging, Magnetic Resonance Imaging (MRI) and Nuclear Imaging (Positron Emission Tomography (PET) and Single Photon Emission Computer Tomography (SPECT)). Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessReview Near Infrared Fluorescence Imaging in Nano-Therapeutics and Photo-Thermal Evaluation

by Mukti Vats, Sumit Kumar Mishra, Mahdieh Shojaei Baghini, Deepak S. Chauhan, Rohit Srivastava and Abhijit De

Int. J. Mol. Sci. 2017, 18(5), 924; doi:10.3390/ijms18050924

Received: 6 March 2017 / Revised: 11 April 2017 / Accepted: 17 April 2017 / Published: 28 April 2017

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Abstract

The unresolved and paramount challenge in bio-imaging and targeted therapy is to clearly define and demarcate the physical margins of tumor tissue. The ability to outline the healthy vital tissues to be carefully navigated with transection while an intraoperative surgery procedure is performed

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The unresolved and paramount challenge in bio-imaging and targeted therapy is to clearly define and demarcate the physical margins of tumor tissue. The ability to outline the healthy vital tissues to be carefully navigated with transection while an intraoperative surgery procedure is performed sets up a necessary and under-researched goal. To achieve the aforementioned objectives, there is a need to optimize design considerations in order to not only obtain an effective imaging agent but to also achieve attributes like favorable water solubility, biocompatibility, high molecular brightness, and a tissue specific targeting approach. The emergence of near infra-red fluorescence (NIRF) light for tissue scale imaging owes to the provision of highly specific images of the target organ. The special characteristics of near infra-red window such as minimal auto-fluorescence, low light scattering, and absorption of biomolecules in tissue converge to form an attractive modality for cancer imaging. Imparting molecular fluorescence as an exogenous contrast agent is the most beneficial attribute of NIRF light as a clinical imaging technology. Additionally, many such agents also display therapeutic potentials as photo-thermal agents, thus meeting the dual purpose of imaging and therapy. Here, we primarily discuss molecular imaging and therapeutic potentials of two such classes of materials, i.e., inorganic NIR dyes and metallic gold nanoparticle based materials. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessReview Radiogenomic Analysis of Oncological Data: A Technical Survey

by Mariarosaria Incoronato, Marco Aiello, Teresa Infante, Carlo Cavaliere, Anna Maria Grimaldi, Peppino Mirabelli, Serena Monti and Marco Salvatore

Int. J. Mol. Sci. 2017, 18(4), 805; doi:10.3390/ijms18040805

Received: 30 December 2016 / Revised: 6 April 2017 / Accepted: 8 April 2017 / Published: 12 April 2017

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Abstract

In the last few years, biomedical research has been boosted by the technological development of analytical instrumentation generating a large volume of data. Such information has increased in complexity from basic (i.e., blood samples) to extensive sets encompassing many aspects of a subject

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In the last few years, biomedical research has been boosted by the technological development of analytical instrumentation generating a large volume of data. Such information has increased in complexity from basic (i.e., blood samples) to extensive sets encompassing many aspects of a subject phenotype, and now rapidly extending into genetic and, more recently, radiomic information. Radiogenomics integrates both aspects, investigating the relationship between imaging features and gene expression. From a methodological point of view, radiogenomics takes advantage of non-conventional data analysis techniques that reveal meaningful information for decision-support in cancer diagnosis and treatment. This survey is aimed to review the state-of-the-art techniques employed in radiomics and genomics with special focus on analysis methods based on molecular and multimodal probes. The impact of single and combined techniques will be discussed in light of their suitability in correlation and predictive studies of specific oncologic diseases. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessReview Advances in Molecular Imaging of Locally Delivered Targeted Therapeutics for Central Nervous System Tumors

by Umberto Tosi, Christopher S. Marnell, Raymond Chang, William C. Cho, Richard Ting, Uday B. Maachani and Mark M. Souweidane

Int. J. Mol. Sci. 2017, 18(2), 351; doi:10.3390/ijms18020351

Received: 9 November 2016 / Revised: 19 December 2016 / Accepted: 26 January 2017 / Published: 8 February 2017

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Abstract

Thanks to the recent advances in the development of chemotherapeutics, the morbidity and mortality of many cancers has decreased significantly. However, compared to oncology in general, the field of neuro-oncology has lagged behind. While new molecularly targeted chemotherapeutics have emerged, the impermeability of

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Thanks to the recent advances in the development of chemotherapeutics, the morbidity and mortality of many cancers has decreased significantly. However, compared to oncology in general, the field of neuro-oncology has lagged behind. While new molecularly targeted chemotherapeutics have emerged, the impermeability of the blood–brain barrier (BBB) renders systemic delivery of these clinical agents suboptimal. To circumvent the BBB, novel routes of administration are being applied in the clinic, ranging from intra-arterial infusion and direct infusion into the target tissue (convection enhanced delivery (CED)) to the use of focused ultrasound to temporarily disrupt the BBB. However, the current system depends on a “wait-and-see” approach, whereby drug delivery is deemed successful only when a specific clinical outcome is observed. The shortcomings of this approach are evident, as a failed delivery that needs immediate refinement cannot be observed and corrected. In response to this problem, new theranostic agents, compounds with both imaging and therapeutic potential, are being developed, paving the way for improved and monitored delivery to central nervous system (CNS) malignancies. In this review, we focus on the advances and the challenges to improve early cancer detection, selection of targeted therapy, and evaluation of therapeutic efficacy, brought forth by the development of these new agents. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessReview An Overview of Multimodal Neuroimaging Using Nanoprobes

by Sriram Sridhar, Sachin Mishra, Miklós Gulyás, Parasuraman Padmanabhan and Balázs Gulyás

Int. J. Mol. Sci. 2017, 18(2), 311; doi:10.3390/ijms18020311

Received: 24 November 2016 / Accepted: 26 January 2017 / Published: 1 February 2017

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Abstract

Nanomaterials have gained tremendous significance as contrast agents for both anatomical and functional preclinical bio-imaging. Contrary to conventional medical practices, molecular imaging plays an important role in exploring the affected cells, thus providing precision medical solutions. It has been observed that incorporating nanoprobes

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Nanomaterials have gained tremendous significance as contrast agents for both anatomical and functional preclinical bio-imaging. Contrary to conventional medical practices, molecular imaging plays an important role in exploring the affected cells, thus providing precision medical solutions. It has been observed that incorporating nanoprobes improves the overall efficacy of the diagnosis and treatment processes. These nano-agents and tracers are therefore often incorporated into preclinical therapeutic and diagnostic applications. Multimodal imaging approaches are well equipped with nanoprobes to explore neurological disorders, as they can display more than one type of characteristic in molecular imaging. Multimodal imaging systems are explored by researchers as they can provide both anatomical and functional details of tumors and affected tissues. In this review, we present the state-of-the-art research concerning multimodal imaging systems and nanoprobes for neuroimaging applications. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessReview Review: Receptor Targeted Nuclear Imaging of Breast Cancer

by Simone U. Dalm, John Fred Verzijlbergen and Marion De Jong

Int. J. Mol. Sci. 2017, 18(2), 260; doi:10.3390/ijms18020260

Received: 1 October 2016 / Revised: 17 January 2017 / Accepted: 20 January 2017 / Published: 26 January 2017

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Abstract

Receptor targeted nuclear imaging directed against molecular markers overexpressed on breast cancer (BC) cells offers a sensitive and specific method for BC imaging. Currently, a few targets such as estrogen receptor (ER), progesterone receptor (PR), human epidermal growth factor receptor 2 (HER2), somatostatin

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Receptor targeted nuclear imaging directed against molecular markers overexpressed on breast cancer (BC) cells offers a sensitive and specific method for BC imaging. Currently, a few targets such as estrogen receptor (ER), progesterone receptor (PR), human epidermal growth factor receptor 2 (HER2), somatostatin receptor (SSTR), and the gastrin releasing peptide receptor (GRPR) are being investigated for this purpose. Expression of these targets is BC subtype dependent and information that can be gained from lesion visualization is dependent on the target; ER-targeting radiotracers, e.g., can be used to monitor response to anti-estrogen treatment. Here we give an overview of the studies currently under investigation for receptor targeted nuclear imaging of BC. Main findings of imaging studies are summarized and (potential) purposes of lesion visualization by targeting these molecular markers are discussed. Since BC is a very heterogeneous disease and molecular target expression can vary per subtype, but also during disease progression or under influence of treatment, radiotracers for selected imaging purposes should be chosen carefully. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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Open AccessReview Hydroxypyridinone Chelators: From Iron Scavenging to Radiopharmaceuticals for PET Imaging with Gallium-68

by Ruslan Cusnir, Cinzia Imberti, Robert C. Hider, Philip J. Blower and Michelle T. Ma

Int. J. Mol. Sci. 2017, 18(1), 116; doi:10.3390/ijms18010116

Received: 2 November 2016 / Revised: 5 December 2016 / Accepted: 21 December 2016 / Published: 8 January 2017

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Abstract

Derivatives of 3,4-hydroxypyridinones have been extensively studied for in vivo Fe³⁺ sequestration. Deferiprone, a 1,2-dimethyl-3,4-hydroxypyridinone, is now routinely used for clinical treatment of iron overload disease. Hexadentate tris(3,4-hydroxypyridinone) ligands (THP) complex Fe³⁺ at very low iron concentrations, and their high affinities

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Derivatives of 3,4-hydroxypyridinones have been extensively studied for in vivo Fe³⁺ sequestration. Deferiprone, a 1,2-dimethyl-3,4-hydroxypyridinone, is now routinely used for clinical treatment of iron overload disease. Hexadentate tris(3,4-hydroxypyridinone) ligands (THP) complex Fe³⁺ at very low iron concentrations, and their high affinities for oxophilic trivalent metal ions have led to their development for new applications as bifunctional chelators for the positron emitting radiometal, ⁶⁸Ga³⁺, which is clinically used for molecular imaging in positron emission tomography (PET). THP-peptide bioconjugates rapidly and quantitatively complex ⁶⁸Ga³⁺ at ambient temperature, neutral pH and micromolar concentrations of ligand, making them amenable to kit-based radiosynthesis of ⁶⁸Ga PET radiopharmaceuticals. ⁶⁸Ga-labelled THP-peptides accumulate at target tissue in vivo, and are excreted largely via a renal pathway, providing high quality PET images. Full article

(This article belongs to the Special Issue Cancer Molecular Imaging in the Era of Precision Medicine)

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