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)
Article
Chemistry, Organic
Kelly Bugatti, Andrea Sartori, Lucia Battistini, Jessica Ruzzolini, Chiara Nediani, Claudio Curti, Francesca Bianchini, Franca Zanardi
Summary: Melanoma, the deadliest form of skin cancer, is increasing in incidence. New studies have shown the potential of combining nintedanib with immuno- and/or targeted therapy drugs in melanoma treatment.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2022)
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.
Review
Cell Biology
Tsai-Mu Cheng, Wong-Jin Chang, Hsiu-Yi Chu, Roberto De Luca, Jens Z. Pedersen, Sandra Incerpi, Zi-Lin Li, Ya-Jung Shih, Hung-Yun Lin, Kuan Wang, Jacqueline Whang-Peng
Summary: Integrin alpha v beta 3 plays a crucial role in cancer cell proliferation and metastasis, with its ligands and crosstalk with other signaling pathways regulating cancer growth. Inhibition of signals related to integrin alpha v beta 3 has shown promise as a target for cancer therapies. Nanotechnologies, such as the use of nanomaterial carriers, are being increasingly explored for their potential potentiation in cancer treatments targeting integrin alpha v beta 3.
Review
Biochemistry & Molecular Biology
Christos Liolios, Christos Sachpekidis, Antonios Kolocouris, Antonia Dimitrakopoulou-Strauss, Penelope Bouziotis
Summary: Multimeric ligands consisting of multiple pharmacophores connected to a single backbone have been widely studied for diagnostic and therapeutic purposes. In targeting integrin alpha(v)beta(3) receptors on cancer cells for molecular imaging and diagnostic applications, multimeric radioligands have shown superiority over monomers. Structural characteristics, binding avidity, pharmacodynamic properties, and PET imaging features of these multimeric ligands have been comprehensively analyzed and discussed in this review.
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
Chemistry, Medicinal
Hiroyuki Suzuki, Mari Araki, Kouki Tatsugi, Kento Ichinohe, Tomoya Uehara, Yasushi Arano
Summary: The interposition of a cleavable linkage by enzymes on the renal brush border membrane is a promising approach for reducing renal radioactivity levels. By adding cleavable linkers to low-molecular-weight antibodies, lower radioactivity levels can be achieved without affecting tumor accumulation.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biology
Na Li, Simei Qiu, Ying Fang, Jianhua Wu, Quhuan Li
Summary: The study found that the cyclic RGD peptide has a more stable configuration in binding to integrins α(v)β(3), while the linear RGD peptide triggers instability in configurational changes. The main interaction energy between cyclic RGD and integrins α(v)β(3) is stronger, resulting in a slower dissociation process, whereas linear RGD is easier to dissociate from the active site.
Editorial Material
Radiology, Nuclear Medicine & Medical Imaging
Henrik Ullman, Karoly Viragh, Mariam Thomas, Chiayi Ni
Summary: A 55-year-old woman with multiple medical problems, including anuric, dialysis-dependent, end-stage renal disease, presented with persistent fever of unknown origin. Despite extensive workup, including cross-sectional imaging and panculture, the etiology was not found. Eventually, an In-111-labeled WBC scan revealed intense heterogeneous uptake in the urinary bladder, leading to the discovery of Klebsiella pneumoniae infection. The fevers resolved with adjustment of therapy, highlighting the importance of considering uncommon sources of infection in complex medical cases.
CLINICAL NUCLEAR MEDICINE
(2021)
Article
Medicine, Research & Experimental
Shimpei Iikuni, Ichiro Kamei, Takaki Ohara, Hiroyuki Watanabe, Masahiro Ono
Summary: A GLP-1R imaging probe [In-111]In-E4DA1 has been developed, which can detect the location of insulinomas in vivo and has reduced renal accumulation.
MOLECULAR PHARMACEUTICS
(2022)
Article
Medicine, General & Internal
Malene Martini Clausen, Esben Andreas Carlsen, Camilla Christensen, Jacob Madsen, Malene Brandt-Larsen, Thomas Levin Klausen, Soren Holm, Annika Loft, Anne Kiil Berthelsen, Niels Kroman, Ulrich Knigge, Andreas Kjaer
Summary: Arginine-Glycine-Aspartate (RGD)-recognizing cell surface integrins play important roles in tumor growth and angiogenesis. Positron emission tomography (PET) allows evaluation of integrin α(v)β(3) expression in tumors. In this first-in-human phase I study, researchers assessed the use of [Ga-68]Ga-NODAGA-E[c(RGDyK)](2) PET in patients with neuroendocrine neoplasms and breast cancer, and found it to be safe and effective for imaging integrin α(v)β(3) with low radiation exposure.
Review
Radiology, Nuclear Medicine & Medical Imaging
Thomas Ebenhan, Janke Kleynhans, Jan Rijn Zeevaart, Jae Min Jeong, Mike Sathekge
Summary: This review highlights the new non-oncologic applications of RGD-based tracers, focusing on scientific literature from the past 10 years. These imaging agents offer options for monitoring diseases where approved tracers are lacking, such as Crohn's disease or osteoporosis. Fundamental science investigations have revealed the role of integrin in diseases not related to oncology.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2021)
Article
Virology
Antonella Bugatti, Federica Filippini, Marta Bardelli, Alberto Zani, Paola Chiodelli, Serena Messali, Arnaldo Caruso, Francesca Caccuri
Summary: Integrins serve as a gateway for SARS-CoV-2 to enter lung endothelial cells, promoting angiogenesis. Alpha(v)beta(3) integrin is identified as the key molecule responsible for this infection. Vaccination-induced antibodies do not inhibit the interaction between SARS-CoV-2 and integrins.
Article
Biochemical Research Methods
Nobuki Kazuta, Hiroyuki Watanabe, Masahiro Ono
Summary: Novel In-111-labeled granzyme B-targeting SPECT imaging probes, [In-111]IDT and [In-111]IDAT, were designed with moderate radiochemical yield and high stability in mouse plasma. Biodistribution experiment in tumor-bearing mice showed moderate accumulation of the probes in tumor, which was confirmed by ex vivo autoradiography correlated with granzyme B expression.
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
(2023)
Article
Oncology
Tao Wu, Xuefeng Zhao, Huiqin Xu
Summary: Abnormal radioiodine uptake in pelvic lesions can occur in patients with differentiated thyroid cancer, requiring timely intervention. This study presented a case of a 51-year-old woman with abnormal uptake in the left pelvic cavity on postablative I-131 scintigraphy, which was treated with laparoscopic bilateral adnexectomy. Post-surgery, the patient showed a significant decrease in Tg levels, highlighting the importance of prompt measures for patients with ovarian cysts and elevated Tg levels.
FRONTIERS IN ONCOLOGY
(2021)
Article
Medicine, Research & Experimental
Francois Bulteau, Michel Thepaut, Maxime Henry, Amandine Hurbin, Laetitia Vanwonterghem, Corinne Vives, Aline Le Roy, Christine Ebel, Olivier Renaudet, Franck Fieschi, Jean-Luc Coll
Summary: This study found that recombinant MGL fragments can efficiently target Tn-positive human tumors without inducing toxicity, making it a promising candidate for in vivo diagnosis and imaging of human tumors and potentially for therapeutic applications.
MOLECULAR PHARMACEUTICS
(2022)
Review
Chemistry, Analytical
Vincent Gardette, Vincent Motto-Ros, Cesar Alvarez-Llamas, Lucie Sancey, Ludovic Duponchel, Benoit Busser
ANALYTICAL CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Amlia Godard, Laura Abad Galan, Jean Rouillon, Shaymaa Al Shehimy, Wassima Tajani, Charlotte Cave, Raluca Malacea-Kabbara, Yoann Rousselin, Pierre Le Gendre, Arnaud Fihey, Mohamed Bendellaa, Benoit Busser, Lucie Sancey, Boris Le Guennic, Christophe Bucher, Olivier Maury, Christine Goze, Ewen Bodio
Summary: Aza-boron-dipyrromethenes (Aza-BODIPYs) are a class of fluorophores with azadipyrromethene (aza-DIPY) ligand rigidified by a boron atom. Complexes of group 13 metals (aluminum and gallium) were synthesized and their properties were investigated. AzaGaDIPY and azaAlDIPY exhibited significant red-shifted fluorescence compared to aza-BODIPY, making them promising for optical medical imaging.
INORGANIC CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Iryna Moskalevska, Virginie Faure, Lucie Haye, Marion Mercey-Ressejac, Arindam K. Dey, Benoit Chovelon, Lohona K. Soro, Loic J. Charbonniere, Andreas Reisch, Andrey S. Klymchenko, Patrice N. Marche, Jean-Luc Coll, Zuzana Macek Jilkova, Xavier le Guevel
Summary: This study developed hydrophobic photoluminescent polymeric nanoparticles and investigated their interaction with macrophages. The nanoparticles were efficiently engulfed by macrophages and showed anti-inflammatory properties when activated, making them potentially useful for treating inflammatory diseases.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(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.
Editorial Material
Pharmacology & Pharmacy
Elisabeth Garanger, Nathalie Mignet, Chantal Pichon, Marie-Pierre Rols, Lucie Sancey
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Chemistry, Medicinal
Amelie Godard, Ghadir Kalot, Malorie Privat, Mohamed Bendellaa, Benoit Busser, K. David Wegner, Franck Denat, Xavier Le Guevel, Jean-Luc Coll, Catherine Paul, Ewen Bodio, Christine Goze, Lucie Sancey
Summary: Using fluorescence-guided surgery (FGS) with NIR-II dyes targeting human epidermal growth factor receptor 2 (HER2)-positive ovarian tumors showed favorable tumor accumulation and selective targeting of HER2 positive tumors. These bioconjugated NIR-II-emitting dyes displayed prolonged stability in serum and maintained affinity toward HER2 in vitro, indicating their potential for NIR-II FGS in the cancer setting. This study suggests that the use of NIR-II dyes in FGS can improve the complete resection of microscopic ovarian tumors.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Multidisciplinary Sciences
Maxime Nachit, Christopher Montemagno, Romain Clerc, Mitra Ahmadi, Francois Briand, Sandrine Bacot, Nick Devoogdt, Cindy Serdjebi, Catherine Ghezzi, Thierry Sulpice, Alexis Broisat, Isabelle A. Leclercq, Pascale Perret
Summary: In this study, researchers found that molecular imaging of VCAM-1 could be a non-invasive alternative to biopsy for detecting liver inflammation in chronic liver disease. By using radiolabeled anti-VCAM-1 nanobody and SPECT, they were able to quantify liver uptake and correlate it with histological inflammatory scores and molecular markers. The diagnostic power of this imaging tool to detect liver inflammation was excellent, suggesting its potential for clinical use.
NATURE COMMUNICATIONS
(2023)
Review
Oncology
Mohamed Bendellaa, Pierre Lelievre, Jean-Luc Coll, Lucie Sancey, Aurelien Deniaud, Benoit Busser
Summary: Zinc is a crucial element involved in various cellular processes and dysregulation of zinc homeostasis occurs in certain cancers. This review explores the role of zinc in cancer, including its related proteins as potential biomarkers and the use of zinc-based strategies for tumor treatment. Targeting zinc and its pathways offers therapeutic approaches, while direct utilization of zinc as a therapeutic agent holds promise for improving cancer prognosis.
INTERNATIONAL JOURNAL OF CANCER
(2023)
Article
Medicine, Research & Experimental
Thibault Leger, Aurelien Brun, Kassandra Lanchais, Jean-Paul Rigaudiere, Arnaud Briat, Yann Guitton, Fabien Marchand, Anne Tournadre, Frederic Capel
Summary: This study found that nutritional supplementation with omega 3 fatty acids can alleviate symptoms of rheumatoid arthritis and be an effective preventive treatment for patients who do not need pharmacological therapy.
Correction
Biochemistry & Molecular Biology
Asma Boudria, Cherine Abou Faycal, Tao Jia, Stephanie Gout, Michelle Keramidas, Chloe Didier, Nicolas Lemaitre, Sandra Manet, Jean-Luc Coll, Anne-Claire Toffart, Denis Moro-Sibilot, Corinne Albiges-Rizo, Veronique Josserand, Eva Faurobert, Christian Brambilla, Elisabeth Brambilla, Sylvie Gazzeri, Beatrice Eymin
Correction
Anesthesiology
A. Jurczak, L. Delay, J. Barbier, N. Simon, E. Krock, K. Sandor, N. M. Agalave, R. Rudjito, G. Wigerblad, K. Rogoz, A. Briat, E. Miot-Noirault, A. Martinez-Martinez, D. Bromme, C. Gronwall, V Malmstrom, L. Klareskog, S. Khoury, T. Ferreira, B. Labrum, E. Deval, J. M. Jimenez-Andrade, F. Marchand, C. Svensson
Article
Materials Science, Multidisciplinary
Walaa Mohammad, K. David Wegner, Clothilde Comby-Zerbino, Vanessa Trouillet, Marina Paris Ogayar, Jean-luc Coll, Riccardo Marin, Daniel Jaque Garcia, Ute Resch-Genger, Rodolphe Antoine, Xavier Le Guevel
Summary: In this study, ultra-small gold nanoparticles stabilized by co-ligands were synthesized, and their physicochemical properties were controlled by the amount of reducing agent used. The absorption cross-section was significantly increased by precisely controlling the reducing agent, which in turn influenced the photoluminescence quantum yield. The results suggest that the physicochemical properties of the ligand shell can be tuned to control the near-infrared absorption and photoluminescence of the gold nanoparticles.
JOURNAL OF MATERIALS CHEMISTRY C
(2023)
Meeting Abstract
Radiology, Nuclear Medicine & Medical Imaging
Arnaud Briat, Sebastien Schmitt, Sophie Besse, Marine Delmas, Nancy Ty, Sebastien Tarrit, Mercedes Quintana
NUCLEAR MEDICINE AND BIOLOGY
(2022)