Article
Biochemistry & Molecular Biology
Valentina Pirota, Enrico Lunghi, Alessandra Benassi, Emmanuele Crespan, Mauro Freccero, Filippo Doria
Summary: The study demonstrated the selective interaction of two new Cu(II)-NDI complexes towards parallel G4 structures, providing promising results for the development of new selective functional ligands for binding and restructuring parallel G4s.
Article
Biochemistry & Molecular Biology
Pegah Fazelifar, Anne Cucchiarini, Zahra Khoshbin, Jean-Louis Mergny, Sakineh Kazemi Noureini
Summary: G-rich sequences can fold into G-quadruplexes and have potential implications in anti-cancer drug design. A study found that palmatine can increase the stability of different G-rich sequences and has the strongest interaction with TRF2.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Multidisciplinary
Haomiao Su, Jinglei Xu, Yuqi Chen, Qi Wang, Ziang Lu, Yage Chen, Kun Chen, Shaoqing Han, Zhentian Fang, Ping Wang, Bi-Feng Yuan, Xiang Zhou
Summary: This study reported a genome-wide strategy for identifying G4RPs and successfully identified a large number of G4RPs. Using this method, new G4 binding proteins were discovered, confirming the interaction of SERBP1 with G4. This developed a new strategy for studying the biological roles of nucleic secondary structures interacting with proteins in cells.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Biochemistry & Molecular Biology
Hijiri Hasegawa, Ikkei Sasaki, Kaori Tsukakoshi, Yue Ma, Kazuo Nagasawa, Shusuke Numata, Yuuki Inoue, Yeji Kim, Kazunori Ikebukuro
Summary: Genomic DNA methylation is studied as a potential biomarker for disease diagnosis. This study focuses on detecting CpG methylation in G4-forming oligonucleotides using G4 ligands, which show significant differences in fluorescence and chemiluminescence intensities between methylated and unmethylated DNAs. This research provides a new method for detecting DNA methylation based on structural changes using G4 ligands.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Kun Chen, Zhiyong He, Wei Xiong, Chun-Jiang Wang, Xiang Zhou
Summary: This study utilized left-handed G-quadruplex (L-G4) structure to catalyze enantioselective reactions, showing good enantioselectivity under certain conditions and further enhanced enantioselectivity with the addition of G4 ligands. Ligands that have regulatory effects on G4 can adjust the enantiomeric excess (ee) value of the product.
CHINESE CHEMICAL LETTERS
(2021)
Article
Biology
Shuntaro Takahashi, Sudipta Bhowmik, Shinobu Sato, Shigeori Takenaka, Naoki Sugimoto
Summary: The relationship between G4 structures and DNA replication was studied, and it was found that different ligands have different effects on the topology of G4. Some ligands can inhibit the replication of G4 with anti-parallel topology, while others selectively inhibit G4 with anti-parallel and hybrid topology. The experiments suggest that native human telomere G4 is more flexible than the modified sequence and can interact with ligands.
Article
Biochemistry & Molecular Biology
Lukas Trizna, Ladislav Janovec, Andrea Halaganova, Viktor Viglasky
Summary: The involvement of G-quadruplex structures in various molecular processes in cells is well known. Rhodamine 6G (RhG) has shown potential as a highly selective ligand for G-quadruplex structures.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Bo-Xin Zheng, Wei Long, Meng-Ting She, Yakun Wang, Dong Zhao, Jie Yu, Alan Siu-Lun Leung, Ka Hin Chan, Jinqiang Hou, Yu-Jing Lu, Wing-Leung Wong
Summary: The development of site-specific, target-selective and biocompatible small molecule ligands as a fluorescent tool for real-time study of cellular functions of RNA G-quadruplexes (G4s), which are associated with human cancers, is significant in cancer biology. We report a cytoplasm-specific and RNA G4-selective fluorescent biosensor in live HeLa cells. The ligand shows high selectivity targeting RNA G4s associated with human cancer hallmarks and can visualize and monitor the dynamic resolving process of RNA G4s in live HeLa cells.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Medicinal
Domen Oblak, Hadzi, Crtomir Podlipnik, Jurij Lah
Summary: The authors investigated the (un)folding and binding process of a human telomeric fragment with ligands through calorimetry and spectroscopy. The results showed that the presence of specific ligands can alter the topology of G-quadruplex nucleic acids. By analyzing thermodynamic parameters and conducting molecular modeling, the driving forces behind the topological transformations were clarified.
Article
Chemistry, Physical
Valeria Libera, Elena A. Andreeva, Anne Martel, Aurelien Thureau, Marialucia Longo, Caterina Petrillo, Alessandro Paciaroni, Giorgio Schiro, Lucia Comez
Summary: This study employed a structure-based strategy to investigate the interaction between TMPyP4 porphyrin and a human telomeric sequence, revealing that porphyrin binding promotes dimerization and light irradiation can control the dimer fraction. Changes in quaternary structure were found to be closely correlated with modifications at the secondary structure level.
JOURNAL OF PHYSICAL CHEMISTRY LETTERS
(2021)
Article
Microbiology
Elishiba Muturi, Fei Meng, Huan Liu, Mengwei Jiang, Hongping Wei, Hang Yang
Summary: The study found that functional PQSs in the ASFV genome, which can form stable G4s in the presence of K+ and be stabilized by G4 ligands such as NMM and PDS, could serve as potential targets for antiviral drugs. Experimental results showed that NMM and PDS can significantly suppress the expression of ASFV genes and inhibit the replication of ASFV in Porcine Alveolar Macrophages.
FRONTIERS IN MICROBIOLOGY
(2021)
Article
Chemistry, Medicinal
Efres Belmonte-Reche, Alessandra Benassi, Pablo Penalver, Anne Cucchiarini, Aurore Guedin, Jean Louis Mergny, Frederic Rosu, Valerie Gabelica, Mauro Freccero, Filippo Doria, Juan Carlos Morales
Summary: Glycosyl conjugation to drugs is a strategy that takes advantage of the overexpression of glucose transporters (GLUT) in cancer cells to achieve targeted therapy. In this study, a series of thiosugar naphthalene diimide conjugates were synthesized and the effects of modifications to the amino sidechain on their antiproliferative activity, antiparasitic activity, ability to bind quadruplexes, cellular uptake, and location were investigated.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
David Moreira, Daniela Leitao, Jessica Lopes-Nunes, Tiago Santos, Joana Figueiredo, Andre Miranda, Daniela Alexandre, Candida Tomaz, Jean-Louis Mergny, Carla Cruz
Summary: In this study, the formation and stability of G-quadruplex structure of a G-rich DNA aptamer AT11-L2 were explored under different experimental conditions, along with its interactions with various G4 ligands and nucleolin (NCL). The results showed that AT11-L2 adopted different topologies depending on the KCl concentration, and the addition of ligands significantly stabilized the G-quadruplex structure. Furthermore, a specific interaction between AT11-L2 G-quadruplex and NCL was identified, and co-localization of these two molecules was observed in certain cell lines.
Review
Pharmacology & Pharmacy
Andrea Criscuolo, Ettore Napolitano, Claudia Riccardi, Domenica Musumeci, Chiara Platella, Daniela Montesarchio
Summary: G-quadruplexes are important targets for anticancer/antiviral therapies. Over 3000 small-molecule ligands have been described, which exert their activity by damaging telomeres or altering gene expression in cancer cells and viruses. Detailed knowledge on the interactions between ligands and G-quadruplexes has been obtained through NMR and crystallographic studies.
Article
Biochemistry & Molecular Biology
Manuel Perez-Soto, Pablo Penalver, Steven T. G. Street, Dora Weenink, Michael P. O'Hagan, Javier Ramos-Soriano, Y. Jennifer Jiang, Gregory J. Hollingworth, M. Carmen Galan, Juan C. Morales
Summary: Naphthalene diimide (NDI) has been widely used in the design of G-quadruplex (G4) ligands. This study explored the structure-activity relationship of a disubstituted NDI derivative in terms of its anticancer and antiparasitic activity. The results showed that certain N-methylpiperazine propyl NDIs exhibited sub-micromolar activity against specific parasites with selective cytotoxicity. However, there was no clear correlation between the G4 binding ability of the NDI derivatives and their biological activity, suggesting the involvement of other mechanisms.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Organic
Faiza Diaba, Gisela Trenchs
Summary: The first violet light-mediated synthesis of gamma- and delta-lactams from N-alkenyl trichloroacetamides is reported in this paper. The reactions are conducted in tetrahydrofuran or 2-methyltetrahydrofuran as the sole solvent without catalysts or additives, under non-anhydrous conditions in an air atmosphere where the solvent serves as the radical initiator.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Feroze Hussain, Sajjad Ahmed, Ashiq Hussain Padder, Qazi Naveed Ahmed
Summary: This study reports a novel and efficient one-pot synthesis method for mixed phosphorotrithioates, which does not require supplementary additives and shows broad applicability.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Hyunjin Oh, Ikyon Kim
Summary: A new 1,2,4-triazole-pyrrolo[1,2-a]pyrazine hybrid system, 6-acylpyrrolo[1,2-a][1,2,4]triazolo[5,1-c]pyrazine, was synthesized using a catalyst-free method. This method involved sequential exposure of pyrrole-2-carbonitrile-derived substrates to DMF-DMA and acyl hydrazide, resulting in the formation of acylated pyrazine and 1,2,4-triazole rings, enabling the installation of various substituents at specific positions on the core skeleton.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Ming Yan, Si-fan Wang, Yong-po Zhang, Jin-zhong Zhao, Zhuo Tang, Guang-xun Li
Summary: Here we developed an efficient photocatalytic approach for the convenient preparation of sulfinamides. The reaction allows for the gram-scale preparation of sulfinamides and the one-pot synthesis of various sulfonyl amides.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Farzaneh Bandehali-Naeini, Zahra Tanbakouchian, Noushin Farajinia-Lehi, Nicolas Mayer, Morteza Shiri, Martin Breugst
Summary: Two tandem catalytic systems were developed for the synthesis of novel 3,4-disubstituted maleimides using the same Ugi adducts. Different maleimide structures can be synthesized using either Pd or Cu catalysis.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Tanya Raghava, Anjan Chattopadhyay, Subhadeep Banerjee, Nivedita Sarkar
Summary: Amine substitution of two ortho fluorine atoms of tetrafluoroterephthalonitrile through SNAr chemistry is easily achievable. But further fluorine substitution is only possible under forcing conditions, yielding valuable fluorophores for bioimaging.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Review
Chemistry, Organic
Anju Chadha, Santosh Kumar Padhi, Selvaraj Stella, Sowmyalakshmi Venkataraman, Thangavelu Saravanan
Summary: Alcohol dehydrogenases are enzymes that use cofactors for oxidation or reduction reactions of alcohols or carbonyl compounds. They are utilized in green chemistry and have applications in the production of pharmaceuticals. Recombinant enzymes have solved the challenge of producing purified enzymes in large quantities. Engineered alcohol dehydrogenases have been used in asymmetric synthesis in industry. Various methods have been established for regenerating expensive cofactors to make the enzymatic process more efficient and economically viable.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
