Article
Medicine, General & Internal
Robert Pichler, Ognian Kalev, Berndt Tomancok, Michael Sonnberger, Daniela Ehrlich, Marina Hodolic
Summary: Somatostatin analogues, including first-generation analogues and pasireotide, are considered the first-line treatment for acromegaly, targeting different SSTR subtypes to improve therapeutic outcomes. Immunohistochemical analysis of SSTR subtypes may have predictive value for treatment response in patients with acromegaly, especially those with clinical relapse and complex clinical courses.
Article
Medicine, Research & Experimental
Servando Hernandez Vargas, Solmaz AghaAmiri, Sukhen C. Ghosh, Michael P. Luciano, Luis C. Borbon, Po Hien Ear, James R. Howe, Jennifer M. Bailey-Lundberg, Gregory D. Simonek, Daniel M. Halperin, Hop S. Tran Cao, Naruhiko Ikoma, Martin J. Schnermann, Ali Azhdarinia
Summary: Charge-balanced near-infrared fluorescent dye FNIR-Tag enhances the imaging properties of fluorescently labeled imaging agents, showing great potential for fluorescent probe development.
MOLECULAR PHARMACEUTICS
(2022)
Article
Chemistry, Multidisciplinary
Li-Tao Tan, Ting-Xiao Shen, Jing-Yi Jiang, Yu-Jie Zhong, Fang-Qi Lin, Hong Xue, Yu-Xin Yao, Xin Jiang, Lei Shen, Xin He
Summary: Transition metal coordination complexes have the potential to overcome the limitations of current chemotherapeutic agents in cancer treatment. The utilization of bifunctional ligands resulted in the formation of self-assembled complexes and complex nanoparticles with excellent water dispersion. The experimental results showed high cytotoxicity and sensitivity of the nanoparticles towards cancer cells, indicating their potential as anticancer candidates.
Review
Biochemistry & Molecular Biology
Guang Huang, Tomasz Cierpicki, Jolanta Grembecka
Summary: Cancer is a leading cause of death and disease globally, and efforts have been made to develop new compounds with improved anticancer properties. 2-Aminobenzothiazole is a class of important heterocycles with various medical and pharmacological activities. Recent research has discovered potent and low-toxicity 2-aminobenzothiazole compounds as new anticancer agents. This article provides a comprehensive review of the activities, design strategies, mechanisms of action, and pre-clinical development of these compounds, highlighting their advantages over other heterocyclic systems.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Physical
Qichen Chen, Zilin Li, Jiangyuan Yu, Qing Xie, Haizhen Lu, Yiqiao Deng, Jinghua Chen, Wenjia Zhu, Li Huo, Yizhou Zhang, Wei Song, Jianqiang Lan, Jianqiang Cai, Zhen Huang, Zixi Wang, Hong Zhao
Summary: This study combines nanomaterials and targeted therapy for neuroendocrine tumors, showing good photothermal conversion efficiency and significant antitumor effects, with potential for further applications.
Article
Oncology
Teresa Pecere, Eleonora Ponterio, Enzo Di Iorio, Modesto Carli, Matteo Fassan, Luisa Santoro, Maicol Bissaro, Giulia Bernabe, Stefano Moro, Ignazio Castagliuolo, Giorgio Palu
Summary: The study demonstrates that aloe-emodin enters tumor cells through somatostatin receptors SSTR2 and SSTR5. SSTR2 expression was found in all surgical neuroblastoma specimens analyzed, highlighting the potential clinical application of aloe-emodin as an antitumor agent.
INTERNATIONAL JOURNAL OF CANCER
(2021)
Article
Chemistry, Medicinal
Melpomeni Fani, Viktoria Weingaertner, Petra Kolenc Peitl, Rosalba Mansi, Raghuvir H. Gaonkar, Piotr Garnuszek, Renata Mikolajczak, Doroteja Novak, Urban Simoncic, Alicja Hubalewska-Dydejczyk, Christine Rangger, Piriya Kaeopookum, Clemens Decristoforo
Summary: Recently, radiolabelled antagonists targeting somatostatin receptors subtype 2 (SST2) in neuroendocrine neoplasms demonstrated certain superior properties over agonists. Within the ERA-PerMED project TECANT two Tc-99m-Tetramine (N4)-derivatized SST2 antagonists (TECANT-1 and TECANT-2) were studied for the selection of the best candidate for clinical translation. The preclinical study provided the basis of selection of [Tc-99m]Tc-TECANT-1 for clinical translation of the first Tc-99m-based SST2 antagonist.
Article
Chemistry, Inorganic & Nuclear
Priyanka Devi, Kiran Singh, Bhupender Kumar, Jahnavi Kumari Singh
Summary: Many pyrazoles-based Schiff bases were reported to exhibit high activity against bacterial, parasitic strains, and cancer cells. A new pyrazole based 'NO' bidentate ligand was synthesized and metal complexes with Co+2, Ni+2, Cu+2, and Zn+2 were also prepared. The characterization of the compounds and their metal complexes was performed, and the metal complexes showed enhanced activity compared to the ligand. They exhibited significant anticancer and antibacterial activity, as well as antifungal activity.
INORGANIC CHEMISTRY COMMUNICATIONS
(2023)
Article
Oncology
David J. Perez, Rodrigo S. Razo-Hernandez, Miguel A. Avila-Rodriguez
Summary: The objective of this study was to theoretically investigate the binding interactions between F-18-labeled SSTA and somatostatin receptor subtype 2. The results revealed that the interaction between Lys and Asp122 was the strongest and considered as the key interaction driving the binding between F-18-SSTA and SSTR-2.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Nishigandha Mone, Shital Harihar, Sunita Salunke-Gawali, Surekha Satpute, Archana Patil, Vivek Mokashi, Mahesh Jadhav, Ray J. Butcher
Summary: The Mn(II), Co(II), Ni(II), Cu(II) and Zn(II) complexes of Henna; 2-hydroxy-1,4-naphthoquinone (Lw) were synthesized and characterized. The composition of all complexes was [M(Lw)(2)(H2O)(2)]. The geometry of the complexes synthesized at 0°C was trans, while cis for complex 4 at 26°C. The crystal structures of copper complexes 4A and its pyridine adduct (4Apy) were determined by single crystal X-ray diffraction studies. The complexes synthesized at 0°C showed enhanced anticancer activity against the A549 cell line. Cell cycle analysis, mitochondrial potential, Reactive Oxygen Species (ROS), peripheral blood mononuclear cells (PBMCs), and Tunnel assay were performed on complex 1A.
INORGANICA CHIMICA ACTA
(2023)
Review
Oncology
Valery V. Veselov, Alexander E. Nosyrev, Laszlo Jicsinszky, Renad N. Alyautdin, Giancarlo Cravotto
Summary: This article discusses the current main technological strategies for delivering anticancer drugs and introduces several drug-delivery systems that have been successfully applied in cancer therapy. Cell-targeted delivery can reduce toxicity and increase effectiveness and selectivity. Besides traditional liposomal and micellar formulations, nanocarrier systems have recently become the focus of developmental interest.
Article
Biochemistry & Molecular Biology
Shuangshuang Gai, Liqin He, Mingxian He, Xuwei Zhong, Caiyun Jiang, Yiming Qin, Ming Jiang
Summary: Developing a new generation of anticancer metal-based drugs that can both kill tumor cells and inhibit cell migration is a promising strategy. In this study, we synthesized three Cu(II), Zn(II), and Mn(II) complexes derived from 5-chloro-2-N-(2-quinolylmethylene)aminophenol (C1-C3). Among them, the Cu(II) complex (C1) showed superior cytotoxicity to lung cancer cell lines compared to cisplatin. Furthermore, C1 demonstrated inhibitory effects on A549 cell metastasis and tumor growth in vivo, and its anticancer mechanism involved multiple pathways such as inducing mitochondrial apoptosis, acting on DNA, blocking cell cycle arrest, inducing cell senescence, and causing DNA damage.
Review
Chemistry, Inorganic & Nuclear
Christopher C. Rennie, Robert M. Edkins
Summary: Phototherapy, using light to selectively ablate cancerous tissue, shows promising prospects. The use of Pc-drug conjugates as targeted anticancer phototherapeutic systems has shown potential in improving treatment specificity and achieving precise, synergistic phototherapy.
DALTON TRANSACTIONS
(2022)
Article
Biochemistry & Molecular Biology
Akiharu Ishida, Yasuyuki Okabe, Takeshi Matsushita, Tetsuya Sekiguchi, Takuya Nishio, Tatsuya Komagata, Masanori Iwaki, Hidenori Miyata, Jun Katagi, Atsushi Naganawa, Toru Maruyama, Akira Imagawa
Summary: This study investigated the relationship between in silico physicochemical properties and hERG and PLD, and found that the value of (cLogP) [2] + (pKa) [2] needs to be less than 110 to mitigate the toxicological liabilities. As a result, wellbalanced agonists such as amide 19 and benzimidazole 30 were identified.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Jiayi Zhu, Yan Liu, Zhao Zhang, Xili Yang, Feng Qiu
Summary: In this study, we designed and synthesized two complexes as photosensitizers, which exhibited strong phosphorescence and high toxicity against cancer cells. These complexes rapidly accumulated in lysosomes after entering cancer cells, and when exposed to light irradiation, they produced a large amount of oxidizing stress substances, eventually leading to cancer cell death. This provides promising potential application in photodynamic therapy.
Article
Biochemistry & Molecular Biology
Andrey Aralov, Nina Gubina, Cristina Cabrero, Vladimir B. Tsvetkov, Anton Turaev, Bogdan Fedeles, Robert G. Croy, Ekaterina A. Isaakova, Denis Melnik, Svetlana Dukova, Dmitriy Y. Ryazantsev, Alexei A. Khrulev, Anna M. Varizhuk, Carlos Gonzalez, Timofei S. Zatsepin, John M. Essigmann
Summary: This study investigated the properties of DNA containing a synthetic base called 7,8-dihydro-8-oxo-1,N-6-ethenoadenine (oxo-epsilon A). The results showed that this base adopts a non-canonical conformation and mimics the natural base thymine, leading to high mutagenicity and strong fluorescence. It was also found to be resistant to repair enzymes and did not affect DNA replication efficiency in living cells.
NUCLEIC ACIDS RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Joaquin Bonelli, Enrique Ortega-Forte, Anna Rovira, Manel Bosch, Oriol Torres, Cristina Cusco, Josep Rocas, Jose Ruiz, Vicente Marchan
Summary: Encapsulation of mitochondria-targeted coumarin photosensitizers within nanocapsules improves their photoactivity and reduces cytotoxicity, making them promising agents for nano-photodynamic therapy.
Review
Biochemistry & Molecular Biology
Nuria Escaja, Bartomeu Mir, Miguel Garavis, Carlos Gonzalez
Summary: Tetrads are arrangements of four nucleobases commonly used to stabilize nucleic acid structures. In addition to the well-known G-quadruplex, non-G tetrads formed by different nucleobases have been observed in experimental structures. They are mostly found in the context of G-quadruplex structures but also occur in other unusual four-stranded structures.
Article
Chemistry, Multidisciplinary
Laura Diaz-Casado, Andres G. Santana, Irene Gomez-Pinto, Alejandro Villacampa, Francisco Corzana, Jesus Jimenez-Barbero, Carlos Gonzalez, Juan Luis Asensio
Summary: NMR spectroscopy is a robust and reliable method for binding detection in drug discovery, but analyzing DNA/RNA targets remains challenging. In this study, the authors explore the perturbation of ligand reactivity caused by complex formation as a binding indicator to identify the best binders within complex mixtures, providing a novel reactivity-based alternative within NMR screening methods.
COMMUNICATIONS CHEMISTRY
(2022)
Article
Chemistry, Applied
Jorge Leal, Gema Dura, Felix A. Jalon, Elisenda Zafon, Anna Massaguer, Jose Vicente Cuevas, Lucia Santos, Ana M. Rodriguez, Blanca R. Manzano
Summary: Luminescent platinum cyclometalated complexes have applications in optoelectronic and biological fields, especially in anticancer activity. A series of these complexes with different ligands were synthesized, and their emission wavelengths could be tuned. Density-functional theory provided descriptions of their molecular orbital characteristics, and time-dependent DFT calculations showed different excited states for different complexes. Biological studies demonstrated that some complexes exhibited cytotoxic activity against human cervical and lung carcinoma cells, and microscopy assays showed their accumulation in cytoplasmic organelles. The disruption of mitochondrial metabolism was observed, leading to a decrease in cellular ATP content. These complexes may have potential as alternative anticancer drugs.
APPLIED ORGANOMETALLIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Eduardo Izquierdo, Marta L. opez-Corrales, Diego Abad-Montero, Anna Rovira, Gemma Fabria, Manel Bosch, Jose Luis Abad, Vicente Marchan
Summary: Researchers have developed a series of new fluorescent sphingolipid probes with excellent emission quantum yields and different subcellular localization patterns.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Joaquin Bonelli, Maria Velasco-de Andres, Neus Isidro, Cristina Bayo, Sergi Chumillas, Laura Carrillo-Serradell, Sergi Casado-Llombart, Cheryl Mok, Daniel Benitez-Ribas, Francisco Lozano, Josep Rocas, Vicente Marchan
Summary: This study reports a technology that encapsulates water-soluble bioactive compounds in double-walled polyurethane-polyurea hybrid nanocapsules (NCs) loaded with indocyanine green (ICG). The NCs demonstrate specific accumulation in tumor tissues while avoiding premature clearance in the bloodstream, making them promising for cancer theragnosis.
Article
Chemistry, Organic
Marta Lopez-Corrales, Anna Rovira, Albert Gandioso, Santi Nonell, Manel Bosch, Vicente Marchan
Summary: Releasing bioactive molecules in specific subcellular locations from caged precursors using visible light is a promising approach in photopharmacology. A series of COUPY-caged model compounds with inherent affinity for mitochondria and absorption in the visible region were synthesized and characterized. The incorporation of a methylgroup near the photocleavable bond was found to be crucial for fine-tuning the photochemical properties of the caging group. The use of a COUPY-caged protonophore confirmed the possibility of photoactivation within mitochondria of living cells under low-dose yellow light irradiation. These new photolabile protecting groups have potential in facilitating the delivery of photocages of biologically active compounds into mitochondria.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Israel Serrano-Chacon, Bartomeu Mir, Lorenzo Cupellini, Francesco Colizzi, Modesto Orozco, Nuria Escaja, Carlos Gonzalez
Summary: We studied a DNA oligonucleotide that forms two different i-motif structures depending on pH and temperature. At neutral pH, the major structure is stabilized by C:C+ base pairs and G:C:G:C tetrads. At pH 5, a more elongated i-motif structure with C:C+ base pairs and G:T:G:T tetrads is observed. Molecular dynamics calculations showed that the conformational transition between the two structures is driven by the protonation state of key cytosines. This study reveals the pH-dependent plasticity and conformational switch of i-motif structures.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Biochemistry & Molecular Biology
Vito Genna, Javier Iglesias-Fernandez, Laura Reyes-Fraile, Nuria Villegas, Kevin Guckian, Punit Seth, Brad Wan, Cristina Cabrero, Montserrat Terrazas, Isabelle Brun-Heath, Carlos Gonzalez, Simone Sciabola, Anabella Villalobos, Modesto Orozco
Summary: Phosphorothioates (PS) have demonstrated their effectiveness in therapeutic oligonucleotides for various applications. However, little is known about the structural changes and the role of PS chirality in DNA center dot RNA hybrids. In this study, computational investigations and experimental measurements revealed the impact of PS chirality on DNA-based antisense oligonucleotides and explained the origin of nuclease resistance conferred by PS-linkages, providing crucial information to improve current ASOs-based therapies.
NUCLEIC ACIDS RESEARCH
(2023)
Article
Chemistry, Multidisciplinary
Roberto El-Khoury, Veronica Macaluso, Christopher Hennecker, Anthony K. Mittermaier, Modesto Orozco, Carlos Gonzalez, Miguel Garavis, Masad J. Damha
Summary: G-quadruplex and i-motif nucleic acid structures can fold through kinetic partitioning mechanisms. While G-quadruplex metastable intermediates are structurally heterogeneous, i-motif folding is considered predictable. This study shows that substitutions of 2'-deoxy-2'-fluoroarabinocytidine can induce the formation of a dimeric i-motif with novel structural features and exceptional stability.
COMMUNICATIONS CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Albert Gandioso, Eduardo Izquierdo-Garcia, Pierre Mesdom, Philippe Arnoux, Nurikamal Demeubayeva, Pierre Burckel, Bruno Saubamea, Manel Bosch, Celine Frochot, Vicente Marchan, Gilles Gasser
Summary: A novel strategy for developing near infrared (NIR)-activatable Ru(II) polypyridyl-based photosensitizers (PSs) was successfully developed, enabling high photocytotoxicities towards cancer cell lines under both normoxic and hypoxic conditions. The lead PS exhibited good photocytotoxic activity under low-oxygen concentration conditions and has potential for the treatment of deep-seated hypoxic tumors. This study presents a promising PDT agent with the ability to be photoactivated at 770nm under hypoxic conditions.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Biochemistry & Molecular Biology
Sergi Chumillas, Saurabh Loharch, Manuela Beltran, Mateusz P. Szewczyk, Silvia Bernal, Maria C. Puertas, Javier Martinez-Picado, Jose Alcami, Luis M. Bedoya, Vicente Marchan, Jose Gallego
Summary: This study explored the optimization of the antiretroviral properties of benfluron and found that both the benzo[c] and cyclopentanone components are essential for its activity. The results provide insights for the design of new anti-HIV agents targeting the inhibition of Rev function.
Article
Chemistry, Multidisciplinary
Israel Serrano-Chacon, Bartomeu Mir, Lorenzo Cupellini, Francesco Colizzi, Modesto Orozco, Nu'ria Escaja, Carlos Gonzalez
Summary: We studied a DNA oligonucleotide that can form two different i-motif structures, with their stability depending on pH and temperature. The structure at neutral pH is stabilized by C:C+ base pairs and G:C:G:C tetrads. At pH 5, a more elongated structure consisting of C:C+ base pairs and G:T:G:T tetrads is observed. The transition between these two structures is driven by the protonation state of key cytosines.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Chemistry, Inorganic & Nuclear
Joaquin Bonelli, Enrique Ortega-Forte, Gloria Vigueras, Manel Bosch, Natalia Cutillas, Josep Rocas, Jose Ruiz, Vicente Marchan
Summary: By encapsulating poorly soluble cyclometalated Ir(III) complexes using polyurethane-polyurea hybrid nanocapsules, their solubility is improved and the nanocapsules can enhance cellular uptake and cytotoxicity, leading to inhibition of tumor growth.
INORGANIC CHEMISTRY FRONTIERS
(2022)