Article
Biochemistry & Molecular Biology
Samir Mohamed Awad, Shima Mahmoud Ali, Yara Essam Mansour, Samar Said Fatahala
Summary: Newly synthesized nucleoside drugs show promising activity against HSV-1, offering a potential solution to the problems associated with current medications.
Article
Chemistry, Multidisciplinary
Yong Woong Jun, Melis Kant, Erdem Coskun, Takamitsu A. A. Kato, Pawel Jaruga, Elizabeth Palafox, Miral Dizdaroglu, Eric T. T. Kool
Summary: High-temperature cooking damages DNA in food, which can then enter the cellular DNA and lead to genetic risks.
ACS CENTRAL SCIENCE
(2023)
Article
Chemistry, Organic
Ya-Han Hsu, Che-Chien Chang
Summary: This study presents a straightforward method for converting a low-cost carbohydrate into an important carbohydrate building block through specific chemical reactions and enzymatic hydrolysis, with a short and efficient synthesis process.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Yuqing Xu, Elisabetta Groaz, Jerome Rihon, Piet Herdewijn, Eveline Lescrinier
Summary: Molecular dynamics simulations revealed the favorable interactions between xylose nucleosides with a phosphonate moiety and specific residues at the active site of the RNA-dependent RNA-polymerase of Enterovirus 71. Xylosyl nucleoside phosphonates containing different nucleobases were synthesized and tested for antiviral activity, with the adenine-containing analogue showing good activity against measles virus and enterovirus-68 without cytotoxicity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Dmitry A. Makarov, Sergey D. Negrya, Maxim V. Jasko, Inna L. Karpenko, Pavel N. Solyev, Vladimir O. Chekhov, Dmitry N. Kaluzhny, Olga V. Efremenkova, Byazilya F. Vasilyeva, Alexander O. Chizhov, Darya A. Avdanina, Alexander A. Zhgun, Sergey N. Kochetkov, Liudmila A. Alexandrova
Summary: The emergence of drug-resistant strains of pathogenic microorganisms necessitates the creation of new drugs. In this study, a series of uridine derivatives with extended substituents at the C-5 position were obtained and their antimicrobial properties and solubility were explored. It was found that these new ribonucleoside derivatives have significantly higher solubility in water than their 2'-deoxy analogues and effectively inhibit the growth of several drug-resistant Gram-positive bacteria.
Article
Biochemistry & Molecular Biology
Yaqing Zuo, Rongrong Li, Yan Zhang, Guochen Bao, Yi Le, Longjia Yan
Summary: A series of 5-trifluoromethylpyrimidine derivatives were designed and synthesised as EGFR inhibitors, showing excellent antitumor activities, especially compound 9u. Further research revealed that compound 9u could induce cell apoptosis and arrest the cell cycle, suggesting its potential as an antitumor reagent.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Muhammad Saqib, Eugene Arthur-Baidoo, Farhad Izadi, Adrian Szczyrba, Magdalena Datta, Sebastian Demkowicz, Janusz Rak, Stephan Denifl
Summary: This study investigates the dissociative electron attachment of 5-iodo-4-thio-2'-deoxyuridine and demonstrates that low-energy electrons can effectively decompose the molecule, forming iodine anions and creating radical sites that may induce DNA strand breaks.
JOURNAL OF PHYSICAL CHEMISTRY LETTERS
(2023)
Article
Nanoscience & Nanotechnology
Yufei Feng, Guozhao Qin, Shuyuan Chang, Zhongxu Jing, Yanyan Zhang, Yanhong Wang
Summary: The novel dual-functional liposome system possessing both extracellular charge reversal and mitochondrial targeting properties significantly enhances drug accumulation in mitochondria and triggers apoptosis of cancer cells. The results demonstrate that the charge reversed and mitochondria-targeted liposomes facilitate cellular internalization and mitochondrial accumulation for enhanced antitumor effect. Therefore, this liposome system represents a promising anticancer drug delivery system for improved therapeutic efficacy.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
Article
Biochemistry & Molecular Biology
Sunbok Jang, Sripriya J. Raja, Vera Roginskaya, Matthew A. Schaich, Simon C. Watkins, Bennett Van Houten
Summary: UV-DDB has a non-canonical role in the processing of 8-oxoG and 5-hmdU. It stimulates the activities of OGG1, MUTYH, APE1, and SMUG1, and reduces the stability of SMUG1 on DNA. Furthermore, UV-DDB and SMUG1 interact transiently in cells.
NUCLEIC ACIDS RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Barbara Kutryb-Zajac, Ada Kawecka, Alicja Braczko, Marika Franczak, Ewa M. Slominska, Roberto Giovannoni, Ryszard T. Smolenski
Summary: Chronic hypoxia impairs vascular function through various mechanisms, including changes in mitochondrial respiration. Our study found that the hypoxia-mimetic agent CoCl2 reduces nitric oxide (NO) production, depletes intracellular ATP levels, and increases extracellular nucleotide and adenosine breakdown in endothelial cells (ECs). Supplementation of nucleotide precursors and inhibition of adenosine deaminase can restore ATP levels and protect endothelial function.
Article
Chemistry, Medicinal
Dilip K. Tosh, Maggie M. Calkins, Marko S. Ivancich, Hailey A. Bock, Ryan G. Campbell, Sarah A. Lewicki, Eric Chen, Zhan-Guo Gao, John D. Mccorvy, Kenneth A. Jacobson
Summary: Derivatives of (N)-Methanocarba adenosine were modified to target 5-HT2B serotonin receptors as antagonists, showing affinity enhancement with the bicyclic ring system. Compound 43 (MRS7925) exhibited potential for anti-fibrotic therapy due to its affinity and moderate 5-HT2BR binding selectivity. The compounds also demonstrated dual action as 5-HT2B antagonists and A(1)AR agonists.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Yanli Wang, Xiaowan Huang, Xiao Zhang, Jingchen Wang, Keyan Li, Guotao Liu, Kexin Lu, Xiang Zhang, Chengping Xie, Teresa Zheng, Yung-Yi Cheng, Qiang Wang
Summary: Allobetulin is a compound similar in structure to betulinic acid, and it has a low toxicity but induces apoptosis in cancer cells. However, it shows weak antiproliferative effects in several tumor cell lines. In this study, a new series of allobetulon/allobetulin-nucleoside conjugates were designed and synthesized to enhance its potency. Compound 10d exhibited superior antiproliferative activity in comparison to cisplatin and oxaliplatin against multiple human cancer cell lines, and it achieved this through the regulation of protein expression levels.
Article
Biochemistry & Molecular Biology
Romina Fernandez Varela, Ana Laura Valino, Eman Abdelraheem, Rosario Medici, Melisa Saye, Claudio A. Pereira, Peter-Leon Hagedoorn, Ulf Hanefeld, Adolfo Iribarren, Elizabeth Lewkowicz
Summary: The utility of different variants of DERA enzyme in synthesizing drug side chains and industrial applications was analyzed. One variant was found to efficiently produce the desired products under optimized conditions and exhibited tolerance to high acetaldehyde concentrations.
Article
Chemistry, Multidisciplinary
Esteban Rodriguez-Arce, Eric Gavrilov, Ximena Alvite, Nazia Nayeem, Ignacio E. Leon, Michelle C. Neary, Lucia Otero, Dinorah Gambino, Claudio Olea Azar, Maria Contel
Summary: This work reports the synthesis and stability study of four gold(I) [AuClL] compounds containing chloro and biologically active protonated thiosemicarbazones based on 5-nitrofuryl (L=HSTC). The cytotoxicity of these compounds was evaluated against cancer cell lines, and one compound showed significant antimigratory and anti-angiogenic properties on a renal cancer cell line (Caki-1), along with preferential accumulation in the cell nuclei. Its mode of action seems to involve interaction with DNA and induction of apoptosis.
Article
Chemistry, Multidisciplinary
Fenghua Chen, Jie Fan, Xiuzhi Chen, Yanping Li, Chengfeng Liang, Shizhao Ren, Rongrong Xue
Summary: Polymorph control of 5-fluorouracil was achieved through ball milling, resulting in the synthesis of Forms II and III. Form II was obtained through one-step grinding of raw material, while Form III required two rounds of grinding, with the addition of ethanol as an additive during the preparation process.
Article
Biochemistry & Molecular Biology
Zeljka Ban, Josipa Matic, Biserka Zinic, Anders Foller Fuchtbauer, L. Marcus Wilhelmsson, Ivo Piantanida
Article
Biochemistry & Molecular Biology
Josipa Matic, Marijana Jukic, Hamit Ismaili, Dijana Saftic, Zeljka Ban, Tana Tandaric, Robert Vianello, Teuta Opacak-Bernardi, Ljubica Glavas-Obrovac, Biserka Zinic
Summary: Novel 6-chloro/morpholino/amino/-9-sulfonylpurine derivatives were synthesized through two approaches, with some derivatives showing antiproliferative activity on human carcinoma, lymphoma, and leukemia cells. The presence of certain substituents was found to promote the predominance of desired tautomers and ensure the stability of the final products.
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
(2021)
Article
Chemistry, Analytical
Marta Koscak, Ivona Krosl, Biserka Zinic, Ivo Piantanida
Summary: In this study, novel peptidoids were synthesized by replacing and extending amino acids in a peptide sequence, and these peptidoids demonstrated similar metal ion binding properties as the parent peptide. Some of the peptidoids showed high affinity to Cu2+ ions and exhibited fluorescent and chiral circular dichroism responses upon Cu2+ ion binding. Additionally, these peptidoids were capable of binding to DNA and RNA, and Cu2+ ions were found to enhance the stability of the peptidoid-DNA/RNA complexes. These findings provide important insights for further investigations on the interaction between peptides and metal ions.
Article
Chemistry, Medicinal
Amalyn Nain-Perez, Anders Foller Fuchtbauer, Liliana Haversen, Aleksei Lulla, Chunxia Gao, Josipa Matic, Leticia Monjas, Alexandra Rodriguez, Paul Brear, Woonghee Kim, Marko Hyvonen, Jan Boren, Adil Mardinoglu, Mathias Uhlen, Morten Grotli
Summary: This study reports the first ADP-competitive inhibitors of liver pyruvate kinase (PKL) and identifies a specific PKL inhibitor through optimization. A structure-activity relationship study of 47 novel synthetic derivatives reveals PKL inhibitors with inhibitory activity in the nanomolar range. These results expand the understanding of the structural requirements for interactions with the ADP-binding site of PKL.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Marta Narczyk, Marta Ilona Wojtys, Ivana Lescic Asler, Biserka Zinic, Marija Luic, Elzbieta Katarzyna Jagusztyn-Krynicka, Zoran Stefanic, Agnieszka Bzowska
Summary: Helicobacter pylori is a global health threat, infecting around 50% of the world's population. This study suggests that purine nucleoside phosphorylase (PNP) could be a new drug target for H. pylori eradication. The inhibition constants of PNP inhibitors were in the micromolar range, with 6-benzylthio-2-chloropurine having the lowest constant. X-ray structures of PNP-inhibitor complexes provided insights into possible tighter binding structures.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Ivona Krosl, Marta Koscak, Karla Ribicic, Biserka Zinic, Dragomira Majhen, Ksenija Bozinovic, Ivo Piantanida
Summary: This study investigated three novel peptidoids based on the tryptophan-histidine-tryptophan (WHW) peptide, wherein the central histidine was replaced by Ala-(triazole), and two derivatives had one tryptophan replaced with pyrene-alkyls. The peptidoids showed strong affinity for Cu2+ cation and exhibited distinct interactions with ds-DNA and ds-RNA compared to metal-free analogues. The pyrene peptidoids efficiently entered living cells with no cytotoxic effect and allowed intracellular confocal microscopy imaging.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Organic
Josipa Matic, Tana Tandaric, Marijana Radio Stojkovic, Filip Supljika, Zrinka Karacic, Ana Tomasio Paic, Lucija Horvat, Robert Vianello, Lidija-Marija Tumir
Summary: Two novel conjugate molecules, pyrene and phenanthridine-amino acid units, were designed with different linker lengths between the aromatic fragments. Molecular modelling and spectrophotometric experiments showed that the conjugates predominantly exist in intramolecularly stacked conformations due to the pi-pi stacking interaction between pyrene and phenanthridine moieties. The pH-dependent excimer formation of these conjugates was significantly red-shifted compared to the pyrene and phenanthridine fluorescence. The conjugate with a longer and more flexible linker exhibited binding affinity for ds-polynucleotides and inactivated a mutant of dipeptidyl peptidase enzyme E451A.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Umberto Maria Battisti, Leticia Monjas, Fady Akladios, Josipa Matic, Eric Andresen, Carolin H. Nagel, Malin Hagkvist, Liliana Haversen, Woonghee Kim, Mathias Uhlen, Jan Boren, Adil Mardinoglu, Morten Grotli
Summary: The inhibition of liver pyruvate kinase is a potential strategy for treating or reversing non-alcoholic fatty liver disease (NAFLD). Urolithin C has been identified as a promising scaffold for developing allosteric inhibitors of liver pyruvate kinase. A comprehensive structure-activity analysis of urolithin C and its analogues was conducted, revealing important chemical features for the desired activity. These findings may facilitate the discovery of more potent and selective PKL allosteric inhibitors.
Article
Biochemistry & Molecular Biology
Marijana Leventic, Teuta Opacak-Bernardi, Vesna Rastija, Josipa Matic, Dijana Pavlovic Saftic, Zeljka Ban, Biserka Zinic, Ljubica Glavas-Obrovac
Summary: The aim of this study was to investigate the antitumor mechanism of two derivatives, 6-Morpholino-SPD and 6-Amino-SPD. The results showed that both derivatives have potential as effective antitumor agents with apoptotic-inducing properties. In addition, the derivatives exhibited activation of the Akt/HIF pathway and disruption of mitochondrial function, suggesting their involvement in tumor growth inhibition.
Article
Biotechnology & Applied Microbiology
Josipa Matic, Isak Bogwald, Erik Tengstrand, Sissel Beate Ronning, Nils Kristian Afseth, Sileshi Gizachew Wubshet
Summary: This study used different commercial proteases and endogenous C. finmarchicus proteases to produce a set of protein hydrolysates and characterized their properties. The results showed that endogenous enzymes had a significant impact on the hydrolysis process, with subtle variations in composition observed among hydrolysates produced using different enzymes. In addition, the hydrolysates exhibited higher bioactivity and antioxidant activity compared to the unhydrolyzed control.
BIOCATALYSIS AND AGRICULTURAL BIOTECHNOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Sara Liljenberg, Amalyn Nain-Perez, Oscar Nilsson, Josipa Matic, Morten Grotli
Summary: This study reports an environmentally friendly route for the synthesis of sulfonamides containing a catechol function using water as a solvent. The reaction is robust and reproducible, and eight different sulfonamides were successfully synthesized.
NEW JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Antonija Erben, Josipa Matic, Nikola Basaric, Ivo Piantanida
CROATICA CHEMICA ACTA
(2019)
Article
Chemistry, Multidisciplinary
Hamit Ismaili, Zeljka Ban, Josipa Matic, Dijana Saftic, Marijana Jukic, Ljubica Glavas-Obrovac, Biserka Zinic
CROATICA CHEMICA ACTA
(2019)
