Article
Medicine, Research & Experimental
Jie Zang, Xuejun Wen, Rong Lin, Xinying Zeng, Chao Wang, Mengqi Shi, Xueyuan Zeng, Jiaying Zhang, Xiaoming Wu, Xianzhong Zhang, Weibing Miao, Pengfei Xu, Zhide Guo, Jingjing Zhang, Xiaoyuan Chen
Summary: In this study, the specificity, pharmacokinetics, and dosimetry of the dual targeting PET tracer [Ga-68]Ga-FAPI-RGD were evaluated through preclinical and preliminary clinical studies. The results showed that [Ga-68]Ga-FAPI-RGD had good stability and favorable binding affinity and specificity. It also exhibited significantly improved tumor uptake and retention compared to its monomeric counterparts.
Article
Chemistry, Multidisciplinary
Floriane Mangin, Charlotte Collet, Valerie Jouan-Hureaux, Fatiha Maskali, Emilie Roeder, Julien Pierson, Katalin Selmeczi, Pierre-Yves Marie, Cedric Boura, Nadia Pellegrini-Moise, Sandrine Lamande-Langle
Summary: A new bifunctional chelating agent based on a DOTA chelator linked to a C-glycosyl compound has been successfully developed, allowing straightforward radiolabeling of biomolecules with high affinity and stability for cancer diagnosis and promising applications in imaging modalities and therapy.
Article
Radiology, Nuclear Medicine & Medical Imaging
Liang Zhao, Xuejun Wen, Weizhi Xu, Yizhen Pang, Long Sun, Xiaoming Wu, Pengfei Xu, Jingjing Zhang, Zhide Guo, Qin Lin, Xiaoyuan Chen, Haojun Chen
Summary: This study evaluated the radiolabeled FAPI-RGD heterodimer using Ga-68 for imaging in cancer patients. The results showed that Ga-68-FAPI-RGD had improved tumor uptake and tumor-to-background ratio compared to F-18-FDG and Ga-68-FAPI PET/CT. The study concluded that Ga-68-FAPI-RGD PET/CT is safe and clinically feasible for imaging various types of cancer.
JOURNAL OF NUCLEAR MEDICINE
(2023)
Article
Medicine, Research & Experimental
Rongxi Wang, Vivianne Jakobsson, Jiarou Wang, Tianzhi Zhao, Xingtong Peng, Bowen Li, Jianchao Xue, Naixin Liang, Zhaohui Zhu, Xiaoyuan Chen, Jingjing Zhang
Summary: This study evaluated the feasibility of using [Ga-68]Ga-FAPI-RGD PET/CT for the detection of lung cancer. The results showed that this method can accurately detect primary lesions with a higher detection rate and improved ability to detect metastases.
Article
Chemistry, Organic
Lucia De Rosa, Ivan Hawala, Rossella Di Stasi, Rachele Stefania, Martina Capozza, Donatella Nava, Luca Domenico D'Andrea
Summary: This article presents a chemical strategy for site-specific double modification and cyclization of a peptide probe using native chemical ligation (NCL) and thiol-maleimide addition. The synthetic strategy is straightforward and can be applied for the development of double-labeled peptide multimodality probes.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Oncology
Yu Long, Fuqiang Shao, Hao Ji, Xiangming Song, Xiaoying Lv, Xiaotian Xia, Qingyao Liu, Yongxue Zhang, Dexing Zeng, Xiaoli Lan, Yongkang Gai
Summary: Ovarian cancer has the highest mortality rate among gynecologic malignancies. Ga-68-NGR-RGD, a tracer targeting CD13 and integrin alpha(v)beta(3), shows better contrast and improved ability to differentiate inflammation compared to F-18-FDG in ovarian cancer imaging. It presents a promising imaging agent for the diagnosis, staging, and follow-up of ovarian tumors.
FRONTIERS IN ONCOLOGY
(2022)
Article
Pharmacology & Pharmacy
Yanlun Gu, Bingqi Dong, Xu He, Zhiwei Qiu, Juqi Zhang, Mo Zhang, Haitao Liu, Xiaocong Pang, Yimin Cui
Summary: Integrin alpha v beta 3 is a critical cell adhesion receptor involved in tumor progression. It has been explored as a therapeutic target, but no antagonist has been approved for human therapy yet.
PHARMACOLOGICAL RESEARCH
(2023)
Review
Pharmacology & Pharmacy
Jordan Cossu, Fabien Thoreau, Didier Boturyn
Summary: RGD peptides have gained significant attention in the past two decades for their potential in improving tumor therapy by targeting the alpha V beta 3 integrin receptor. This review focuses on the molecular design of multimeric RGD compounds and suitable linkers for drug delivery. The use of RGD constructs in enhancing binding affinity and drug uptake in tumor cells, as well as their potential as theranostic systems, is highlighted. Furthermore, ongoing and future development in comparison with large molecules like monoclonal antibodies is addressed.
Review
Biochemistry & Molecular Biology
Ewa Brzozowska, Sameer Deshmukh
Summary: Integrins are crucial for cell adhesion, migration, and positioning. Studies have shown that the expression levels of Integrin αVβ6 are closely related to malignant diseases and patient prognosis. It plays a significant role in cancer progression and the activation of transforming growth factor β(TGF-β). While essential for normal function in healthy individuals, it can also be a target for cancer treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Stefano Tomassi, Vincenzo Maria D'Amore, Francesco Saverio Di Leva, Andrea Vannini, Giacomo Quilici, Michael Weinmueller, Florian Reichart, Jussara Amato, Barbara Romano, Angelo Antonio Izzo, Salvatore Di Maro, Ettore Novellino, Giovanna Musco, Tatiana Gianni, Horst Kessler, Luciana Marinelli
Summary: Recent studies have shown that small RGD-containing cyclic pentapeptides could be a promising pharmaceutical approach for inhibiting herpes virus entry into cells, by selectively binding to alpha v beta 6/alpha v beta 8 integrins. The affinity of these compounds towards the integrins was rationalized through a combined NMR/molecular modeling approach, offering valuable insights for designing RGD integrin ligands with desired specificity.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biotechnology & Applied Microbiology
Lijun Zhong, Lin Tang, Xiaoxia He
Summary: It has been discovered that ANGPTL3 plays an oncogenic role in several types of human malignancies. This study found that ANGPTL3 is highly expressed in cervical cancer cells and silencing ANGPTL3 can inhibit cell proliferation, migration, invasion, and angiogenesis. The inhibitory effect of ANGPTL3 can be offset by upregulating the expression of alpha v beta 3, which also promotes blood vessel formation and the secretion of VEGF and VEGFR2 in cervical cancer cells.
Article
Medicine, General & Internal
Arghavan Jahandideh, Mia Stahle, Jenni Virta, Xiang-Guo Li, Heidi Liljenbaeck, Olli Moisio, Juhani Knuuti, Anne Roivainen, Antti Saraste
Summary: The study demonstrated the potential of using alpha(v)beta(3)-targeting PET imaging with [Ga-68]Ga-NODAGA-RGD to specifically detect myocardial inflammation in a rat model of autoimmune myocarditis. The results showed higher accumulation of the tracer in inflamed myocardium compared to non-inflamed tissue, indicating its efficacy in identifying active inflammatory lesions.
FRONTIERS IN MEDICINE
(2021)
Article
Biochemistry & Molecular Biology
Nicola Salvarese, Debora Carpanese, Laura Melendez-Alafort, Laura De Nardo, Andrea Calderan, Barbara Biondi, Paolo Ruzza, Antonio Rosato, Cristina Bolzati
Summary: This study compared the reactivity and impact of three [Tc(N)(PNP)] frameworks on the stability, receptor targeting properties, biodistribution, and metabolism of the corresponding [Tc-99m][Tc(N)(PNP)]-tagged cRGDfK peptide. The results showed that ws[Tc-99m][Tc(N)(PNP3OH)]- and [Tc-99m][Tc(N)(PNP3)]- frameworks had better labeling efficiency and in vivo performance compared to the [Tc-99m][Tc(N)(PNP43)] framework, making them more suitable for radiopharmaceutical applications.
Article
Chemistry, Multidisciplinary
Syed Faheem Askari Rizvi, Azam Ali, Munir Ahmad, Shuai Mu, Haixia Zhang
Summary: The synthesis of self-assembled peptide nanoparticles with a one-pot approach has attracted attention for combined therapy and diagnosis. By modifying a cyclic heptapeptide and conjugating with NIRF dye and radionuclide, novel nanoparticles were successfully developed with high targeting affinity and therapeutic potential, serving as a promising theranostic probe for brain tumor glioblastoma.
NANOSCALE ADVANCES
(2021)
Article
Chemistry, Medicinal
Danielle V. Sobral, Leonardo L. Fuscaldi, Ana Claudia R. Durante, Fernanda F. Mendonca, Larissa R. de Oliveira, Ana Claudia C. Miranda, Jorge Mejia, Wagner R. Montor, Marycel F. de Barboza, Luciana Malavolta
Summary: This study compared the radiolabeling efficiency and biological properties of two different RGD analogs and evaluated their interaction with overexpressed receptors in tumor cells. The results showed high radiochemical yields, stability, and binding ability to serum proteins for both peptides. They also exhibited binding and internalization capabilities with tumor cells and showed different localization characteristics in rat brain tissue, indicating their potential for clinical applications.
Article
Oncology
Maarten J. van der Doelen, Irma M. Oving, Dirk N. J. Wyndaele, Jean-Paul van Basten, Frederiek Terheggen, Addy C. M. van de Luijtgaarden, Wim J. G. Oyen, W. Dick van Schelven, Franchette van den Berkmortel, Niven Mehra, Marcel J. R. Janssen, Judith B. Prins, Winald R. Gerritsen, Jose A. E. Custers, Inge M. van Oort
Summary: This study evaluated the health-related quality of life, psychological distress, and fatigue in patients with metastatic castration-resistant prostate cancer (mCRPC) treated with radium-223. The study found that patients who discontinued radium-223 therapy had worse HR-QoL, psychological distress, and fatigue at baseline and more frequent deterioration over time compared to patients who completed therapy.
PROSTATE CANCER AND PROSTATIC DISEASES
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Joey Roosen, Meike W. M. van Wijk, Lovisa E. L. Westlund Gotby, Mark J. Arntz, Marcel J. R. Janssen, Daphne Lobeek, Gerrit H. van de Maat, Christiaan G. Overduin, J. Frank W. Nijsen
Summary: This study evaluated the feasibility and accuracy of MRI-based dosimetry for holmium-166 transarterial radioembolization (Ho-166 TARE). The results showed that voxelwise subtraction-based method improved the accuracy of absorbed dose estimation and corresponded better with SPECT-based dosimetry compared to the currently implemented mean subtraction method.
Article
Radiology, Nuclear Medicine & Medical Imaging
Elizabeth J. de Koster, Adriana C. H. van Engen-van Grunsven, Johan Bussink, Cathelijne Frielink, Lioe-Fee de Geus-Oei, Benno Kusters, Hans Peters, Wim J. G. Oyen, Dennis Vriens
Summary: This study explored the association between [F-18]FDG uptake and the quantitative expression of immunohistochemical markers related to glucose metabolism, hypoxia, and cell proliferation in benign and malignant thyroid nodules of indeterminate cytology. The results showed that the expression of GLUT1, HK2, and MCT4 increased in [F-18]FDG-positive benign nodules and thyroid carcinomas as compared to [F-18]FDG-negative benign nodules, and VEGF expression was higher in thyroid carcinomas.
MOLECULAR IMAGING AND BIOLOGY
(2023)
Letter
Radiology, Nuclear Medicine & Medical Imaging
Dennis Vriens, Elizabeth J. de Koster, Lioe-Fee de Geus-Oei, Wim J. G. Oyen, EfFECTS trial consortium
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Article
Chemistry, Inorganic & Nuclear
Rachel E. Nuttall, Truc Thuy Pham, Ailis C. Chadwick, Ingebjorg N. Hungnes, George Firth, Martin A. Heckenast, Hazel A. Sparkes, Michelle T. Ma, M. Carmen Galan, Paul G. Pringle
Summary: Hydrophosphination reactions can be used to derivatize diphosphines with biomolecular moieties, allowing the synthesis of ligands with fluorescence and receptor-targeting properties for disease detection and treatment. These ligands can be efficiently radiolabeled with Tc-99m and Re-188, and exhibit favorable biodistribution and stability.
INORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Johanna Pruller, Truc Thuy Pham, Julia E. Blower, Putthiporn Charoenphun, Alessia Volpe, Kavitha Sunassee, Gregory E. D. Mullen, Philip J. Blower, Richard A. G. Smith, Michelle T. Ma
Summary: This study presents a new method for cell tracking, which involves labeling peptides that bind to the cell membrane, enabling quantitative and longitudinal tracking of cells in vivo. The method has been successfully demonstrated to track the accumulation of myeloma cells in the lungs.
RSC CHEMICAL BIOLOGY
(2023)
Editorial Material
Radiology, Nuclear Medicine & Medical Imaging
Ozgul Ekmekcioglu, Samantha Y. A. Terry, Silvia Morbelli, Juliano J. Cerci, Helle D. Zacho, Steffie Peters, Xavier Boulvard Chollet, Fred Verzijlbergen
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
H. Adams, E. M. W. van de Garde, D. J. Vugts, J. C. Grutters, Wim. J. G. Oyen, R. G. Keijsers
Summary: This study investigates the use of imaging CD20-positive cells in predicting the response to anti-CD20 treatment for immune-mediated interstitial lung disease. PET/CT imaging was performed on 21 patients, and it was found that the uptake of [89Zr]-rituximab in the lungs correlated with changes in pulmonary function test results and treatment outcomes. Patients with a higher uptake of [89Zr]-rituximab had better response to treatment. Therefore, [89Zr]-rituximab PET imaging may serve as a potential predictive biomarker for anti-CD20 therapy.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Article
Chemistry, Inorganic & Nuclear
Ingebjorg N. Hungnes, Truc Thuy Pham, Charlotte Rivas, James A. Jarvis, Rachel E. Nuttall, Saul M. Cooper, Jennifer D. Young, Philip J. Blower, Paul G. Pringle, Michelle T. Ma
Summary: We have developed a diphosphine (DP) platform for radiolabeling peptides with 99mTc and 64Cu for molecular SPECT and PET imaging, respectively. The platform enables straightforward functionalization of targeting peptides with a diphosphine chelator, leading to bioconjugates that can be radiolabeled with high radiochemical yield. The DP platform offers versatility and potential for the development of new receptor-targeted imaging radiotracers.
INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Charlotte Rivas, Jessica A. Jackson, Alex Rigby, James A. Jarvis, Andrew J. P. White, Philip J. Blower, Andreas Phanopoulos, Michelle T. . Ma
Summary: Hydroxypyridinone-based chelators have been found to be useful in incorporating radioactive metal ions into nuclear medicine diagnostic and therapeutic agents. In this study, two novel chelators with hydroxypyridinone groups were prepared and their reactivity towards radiometal-mediated hydrolysis was investigated. The results showed that the L1 complex exhibited a higher reactivity towards hydrolysis compared to the L2 complex. These findings were further supported by density functional theory calculations. This study highlights the importance of proper characterization of radiolabeled products.
INORGANIC CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Volker Morath, Corinna Brandt, Friedrich-Christian Deuschle, Claudia T. Mendler, Birgit Blechert, Dominik Summer, Cyril Barinka, Clemens Decristoforo, Wolfgang A. Weber, Markus Schwaiger, Arne Skerra
Summary: Anticalin proteins targeting PSMA with tailored plasma half-life using PASylation technology are promising radioligands for PET imaging of xenograft tumors in mice. PET imaging using the FsC radiochelator is superior to Dfo radiochelator and adjusting the plasma half-life of Anticalin radioligands using PASylation technology can increase radioisotope accumulation within the tumor.
MOLECULAR PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Doroteja Novak, Barbara Janota, Anton Amadeus Hoermann, Agnieszka Sawicka, Marko Kroselj, Alicja Hubalewska-Dydejczyk, Melpomeni Fani, Renata Mikolajczak, Petra Kolenc, Clemens Decristoforo, Piotr Garnuszek
Summary: The broad availability and cost-effectiveness of Mo-99/Tc-99m generators worldwide have supported the use and development of novel Tc-99m-labelled radiopharmaceuticals. This study aimed to provide a reliable method for the facile preparation of a Tc-99m-labelled SST2 antagonist, [Tc-99m]Tc-TECANT-1, in a hospital radiopharmacy setting for a multi-centre clinical trial. A freeze-dried three-vial kit was successfully developed to ensure successful and reproducible on-site preparation of the radiopharmaceutical for human use shortly before administration.
Article
Chemistry, Medicinal
Martin Kraihammer, Piotr Garnuszek, Andreas Bauman, Michael Maurin, Manuel Alejandre Lafont, Roland Haubner, Elisabeth von Guggenberg, Michael Gabriel, Clemens Decristoforo
Summary: The study validated a method for quality control of [Lu-177]Lu-PSMA I&T, including determination of radiochemical purity, identity testing and limit test for PSMA I&T by HPLC and TLC. The combination of HPLC and TLC provides a reliable tool for quality control of [Lu-177]Lu-PSMA I&T.
EJNMMI RADIOPHARMACY AND CHEMISTRY
(2023)
Article
Oncology
Elizabeth J. de Koster, Willem E. Corver, Lioe-Fee de Geus-Oei, Wim J. G. Oyen, Dina Ruano, Abbey Schepers, Marieke Snel, Tom van Wezel, Dennis Vriens, Hans Morreau
Summary: This study described the patterns of copy number alterations (CNA) in benign and malignant oncocytic cell thyroid neoplasms (OCN) using a next-generation sequencing (NGS) panel. The study found that the CNA patterns differed between benign and malignant cases, and suggested the application of CNA-LOH analysis using the NGS panel in the molecular diagnostics of OCN.
ENDOCRINE-RELATED CANCER
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Julie Bolcaen, Mohamed A. Gizawy, Samantha Y. A. Terry, Antonio Paulo, Bart Cornelissen, Aruna Korde, Jonathan Engle, Valery Radchenko, Roger W. Howell
Summary: Auger electron (AE) radiopharmaceutical therapy (RPT) may have therapeutic efficacy similar to α-particles for small oncologic diseases, with lower risks of normal tissue toxicity. Despite accumulating knowledge about AE research, the promise of AE RPT has not yet been realized, with only a few agents evaluated in clinical trials.
JOURNAL OF NUCLEAR MEDICINE
(2023)
