Article
Infectious Diseases
David Gur, Theodor Chitlaru, Emanuelle Mamroud, Ayelet Zauberman
Summary: Yersinia pestis is a deadly pathogen causing plague, and timely antibiotic treatment is crucial for saving lives. A study exploring FDA-approved drugs identified potential alternative compounds with antibacterial activity against Y. pestis, aiming to combat antibiotic resistance.
Review
Pharmacology & Pharmacy
Davide Benedetto Tiz, Luana Bagnoli, Ornelio Rosati, Francesca Marini, Claudio Santi, Luca Sancineto
Summary: This review describes recently FDA-approved drugs, many of which contain active moieties that have not been previously approved by the FDA. These drugs provide important new therapies for patients with multiple unmet diseases.
Letter
Medicine, General & Internal
S. Sean Tu, Aaron S. Kesselheim, Kathrine Wetherbee, William B. Feldman
Summary: This study evaluates the frequency of continuation patents on brand-name drugs approved by the US Food and Drug Administration from 2000 to 2015.
JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION
(2023)
Article
Pharmacology & Pharmacy
Zara Ahmad Khan, Yuli Hu, Behafarid Ghalandari, Mashaal Ahmad, Aynur Abdullah, Lai Jiang, Xianting Ding
Summary: This study aimed to investigate the synthetic cytotoxicity interaction between Paxlovid and 100 frequently used small molecule drugs and further explore the structural modulation through molecular docking simulation with Caspase-8.
TOXICOLOGY AND APPLIED PHARMACOLOGY
(2023)
Article
Health Care Sciences & Services
Victor L. Van de Wiele, Andrew W. Torrance, Aaron S. Kesselheim
Summary: Newly approved drugs are mostly protected by patents, which mainly cover chemical compounds and methods of use. The median time for patents to expire after the approval of original drugs is 10.3 years. About one in five patents have no counterparts in other major jurisdictions, suggesting different manufacturer strategies or patent standards in the US compared to other comparable settings. Patent protection for newly approved drugs largely focuses on product and its uses, indicating that patent reform is crucial for timely entry of generic drugs.
Review
Chemistry, Medicinal
Sheng Han, Yiming Lu
Summary: Human immunodeficiency virus (HIV) is the cause of acquired immunodeficiency syndrome (AIDS). The FDA has approved over thirty antiretroviral drugs, one-third of which contain fluorine atoms. The addition of fluorine to drug compounds is a well-known strategy in medicinal chemistry. This review summarizes 11 fluorine-containing anti-HIV drugs, focusing on their efficacy, resistance, safety, and the role of fluorine in their development. These examples may aid in the discovery of new drug candidates with fluorine-containing structures.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Chandani T. Muleva, Sonali S. Bharate
Summary: Salification is an important method to modulate the properties of poorly water-soluble drugs, and halogen acids play a significant role in the process. Analyzing data from the orange book, it was found that -600 pharmaceutical salts of new chemical entities have been approved in the past nine decades, with halides being the most common counterion. Among the halides, salts prepared with hydrochloric acid are the most dominant. Despite their corrosive and hazardous nature, halogen acids are necessary in salt screening experiments for drug discovery and development.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Jingrui He, Ziyi Li, Gagan Dhawan, Wei Zhang, Alexander E. Sorochinsky, Greg Butler, Vadim A. Soloshonok, Jianlin Han
Summary: This review article presents nine newly approved fluorine-containing drugs by the US Food and Drug Administration (FDA) in 2021. These small molecule drugs feature aromatic fluo-rine, trifluoromethyl, and chlorodifluoro groups. The therapeutic areas of these fluorine-containing drugs include multiple myeloma, lymphoma, HIV, chronic heart failure, chronic myeloid leukemia, (ANCA)-associated vasculitis, migraines, von Hippel-Lindau disease, and non-small cell lung cancer. The review also discusses the brief biological activities and synthetic methods for each of these nine drugs.
CHINESE CHEMICAL LETTERS
(2023)
Article
Virology
Madhura Punekar, Bhagyashri Kasabe, Poonam Patil, Mahadeo B. Kakade, Deepti Parashar, Kalichamy Alagarasu, Sarah Cherian
Summary: This study utilized transcriptomics-based bioinformatics approach to identify drugs with significant anti-DENV activity. The results showed that these drugs can interact with multiple protein targets of DENV and decrease virus production.
Article
Oncology
Yifei Xie, Ke Yao, Zigang Dong, Kangdong Liu
Summary: Proliferating cancer cells have metabolic alterations and specific nutritional needs, making targeting metabolic abnormalities for cancer chemoprevention promising. Many FDA-approved anti-metabolic drugs have been shown to decrease tumor risk, inhibit tumor growth, or enhance the effect of chemotherapy drugs, with fewer side effects compared to chemotherapeutic drugs.
Review
Medicine, Research & Experimental
Ademola C. Famurewa, Anirban Goutam Mukherjee, Uddesh Ramesh Wanjari, Aarthi Sukumar, Reshma Murali, Kaviyarasi Renu, Balachandar Vellingiri, Abhijit Dey, Abilash Valsala Gopalakrishnan
Summary: Platinum-based anticancer drugs have been widely used for treating various cancer types, but their toxicity to non-targeted organs is a concern. Research has shown that this toxicity is associated with free radical generation, DNA impairment, mitochondrial dysfunctions, and other factors. Repurposing non-anticancer drugs has emerged as a strategy to mitigate the side effects of platinum-based drugs.
Article
Virology
Cuiling Ding, Wanda Tang, Binghui Xia, Haoran Peng, Yan Liu, Jiaqi Wang, Xu Zheng, Yangang Liu, Lanjuan Zhao, Yanhua He, Zhongtian Qi, Hao Ren, Hailin Tang, Ping Zhao
Summary: The emergence and spread of arboviruses pose a significant threat to global public health. Currently, there are no approved drugs for the treatment of these viruses. However, a study found that the clinically approved drugs ixazomib and ixazomib citrate showed antiviral activity against multiple arboviruses, including chikungunya virus, at low concentrations. These findings suggest that ixazomib could be a potential broad-spectrum agent against arboviruses.
Review
Engineering, Chemical
Aathira Sujathan Nair, Ashutosh Kumar Singh, Astik Kumar, Sunil Kumar, Sunitha Sukumaran, Vishal Payyalot Koyiparambath, Leena K. Pappachen, T. M. Rangarajan, Hoon Kim, Bijo Mathew
Summary: As people around the world consider 2020 as the year dominated by COVID-19, the medical community acknowledges it as one of the most successful years for drug approvals by the FDA, along with 1996. Both years witnessed the approval of 53 new drug molecules. In 2020, 53 new chemical entities and 13 biological medicines were approved, with a significant number of them containing fluorine or fluorine-containing functional groups and exhibiting diverse pharmacological activities.
Article
Biochemistry & Molecular Biology
Jenna R. James, Johnathan Curd, Jennifer C. Ashworth, Mays Abuhantash, Martin Grundy, Claire H. Seedhouse, Kenton P. Arkill, Amanda J. Wright, Catherine L. R. Merry, Alexander Thompson
Summary: A 3D model of the bone marrow niche has been developed using a synthetic peptide hydrogel (SAPH) to screen FDA-approved drugs for acute myeloid leukemia (AML). The optimized stiffness of SAPH affects AML cell proliferation and Salinomycin shows efficacy in AML patient samples. Vidofludimus is not sensitive to AML cells in the hydrogel models.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Pharmacology & Pharmacy
Mohini Chaurasia, Romi Singh, Srija Sur, S. J. S. Flora
Summary: This article summarizes the therapeutic agents approved or being used in the treatment or mitigation of breast cancer by the US FDA. More than 300 peer-reviewed papers were included to provide comprehensive information on 39 drugs, including their current status, dose protocols, mechanism of action, pharmacokinetics, possible side effects, and marketed formulations. The article also focuses on novel formulations of these drugs currently in clinical trials or in the process of approval, serving as a one-stop solution for researchers in formulation development.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Multidisciplinary Sciences
Mafalda Concilli, Raffaella Petruzzelli, Silvia Parisi, Federico Catalano, Francesco Sirci, Francesco Napolitano, Mario Renda, Luis J. Galietta, Diego Di Bernardo, Roman S. Polishchuk
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2020)
Review
Biochemistry & Molecular Biology
Ludmila V. Puchkova, Irina V. Kiseleva, Elena V. Polishchuk, Massimo Broggini, Ekaterina Yu. Ilyechova
Summary: Three main approaches to combat severe viral respiratory infections include preemptive vaccination, chemical agents inhibition of viral proteins, and targeting host metabolism. The challenge lies in the evolving nature of the viral genome which impacts the effectiveness of vaccines and drugs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Francesco Bellomo, Ester De Leo, Anna Taranta, Laura Giaquinto, Gianna Di Giovamberardino, Sandro Montefusco, Laura Rita Rega, Anna Pastore, Diego Luis Medina, Diego Di Bernardo, Maria Antonietta De Matteis, Francesco Emma
Summary: The article discusses a drug repurposing strategy for nephropathic cystinosis, a rare inherited disorder, using mechanism-based and cell-based screenings coupled with computational analysis to predict therapeutic responses. Through comparing gene-expression signatures of drugs and the disease, potential drugs and metabolic pathways relevant to the pathophysiology were identified.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Magdalena Wesierska, Anna Kloska, Diego L. Medina, Joanna Jakobkiewicz-Banecka, Magdalena Gabig-Ciminska, Marta Radzinska, Marta Moskot, Marcelina Malinowska
Summary: Flavonoids, specifically genistein and kaempferol, have been found to have therapeutic effects on mucopolysaccharidosis, a metabolic disorder. The combination of these two flavonoids can inhibit glycosaminoglycan synthesis, regulate lysosomal number and distribution, and modulate gene expression. The type of interaction between flavonoids varies depending on concentration and component ratios.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Cell Biology
Raffaella Petruzzelli, Marta Mariniello, Rossella De Cegli, Federico Catalano, Floriana Guida, Elia Di Schiavi, Roman S. Polishchuk
Summary: ATP7B is a key player in the regulation of copper homeostasis and signaling as well as chemoresistance in cancer. This study found that transcription factor EB (TFEB) binds to specific regions of ATP7B, promoting its transcription and contributing to drug resistance in cancer cells.
Article
Immunology
Mohammad Al Farroukh, Irina Kiseleva, Ekaterina Bazhenova, Ekaterina Stepanova, Ludmila Puchkova, Larisa Rudenko
Summary: This study evaluated the evolution and key properties of A(H1N1)pdm09 influenza virus and identified the molecular basis for its high pathogenicity. The findings showed that high pathogenicity strains must express toxic effects, have a non-ts phenotype, and have thermally stable HA. Additionally, the A/South Africa/3626/2013 strain was found to have high pathogenicity in a mouse model and had three unique mutations.
Article
Medicine, Research & Experimental
Agnese Padula, Raffaella Petruzzelli, Sasha A. Philbert, Stephanie J. Church, Federica Esposito, Severo Campione, Marcello Monti, Filomena Capolongo, Claudia Perna, Edoardo Nusco, Hartmut H. Schmidt, Alberto Auricchio, Garth J. S. Cooper, Roman Polishchuk, Pasquale Piccolo
Summary: This study successfully used split intein technology to design a dual AAV vector approach for gene therapy of Wilson disease. The results demonstrated the efficacy of split intein technology in reconstituting full-length human ATP7B protein and improving liver damage and copper homeostasis in ATP7B mice.
MOLECULAR THERAPY-METHODS & CLINICAL DEVELOPMENT
(2022)
Retraction
Biochemistry & Molecular Biology
Alessandro Fraldi, Fabio Annunziata, Alessia Lombardi, Hermann-Josef Kaiser, Diego Luis Medina, Carmine Spampanato, Anthony Olind Fedele, Roman Polishchuk, Nicolina Cristina Sorrentino, Kai Simons, Andrea Ballabio
Review
Engineering, Environmental
Alexey N. Skvortsov, Ekaterina Yu. Ilyechova, Ludmila V. Puchkova
Summary: The increasing application of silver nanoparticles (AgNPs) raises concerns among ecologists and health specialists due to their release into the environment. This paper focuses on the interference of silver with copper metabolism, the potential health effects, and the risk of low silver concentrations to humans. The chemical properties of AgNPs are discussed in relation to their release in mammals, and the potential use of silver in treating severe diseases is addressed based on its impact on copper status.
JOURNAL OF HAZARDOUS MATERIALS
(2023)
Article
Pharmacology & Pharmacy
Daria N. Magazenkova, Ekaterina A. Skomorokhova, Mohammad Al Farroukh, Maria S. Zharkova, Zena M. Jassem, Valeria E. Rekina, Olga V. Shamova, Ludmila V. Puchkova, Ekaterina Y. Ilyechova
Summary: The use of silver nanoparticles (AgNPs) can potentially lower bioavailable copper by interfering with copper metabolism. In this study, mice with ascitic or solid Ehrlich adenocarcinoma (EAC) were treated with AgNPs, and various copper-related indicators and gene expressions were monitored. The results showed that intraperitoneal and topical AgNPs treatments improved mice survival, reduced tumor growth, and influenced gene expressions that play a role in neovascularization.
Review
Biochemistry & Molecular Biology
Marina N. Karpenko, Zamira M. Muruzheva, Ekaterina Yu. Ilyechova, Polina S. Babich, Ludmila V. Puchkova
Summary: In the last 15 years, the relationship between copper imbalance and the development of idiopathic Parkinson's disease (PD) has been extensively studied. Despite the large number of papers on the subject, the correlation between copper status and PD development is still debated. Based on published literature, meta-analysis, and new research findings, it is clear that there is a weak connection between the number of copper atoms and the development of PD symptoms. This work also discusses the link between inborn errors related to copper metabolism and the risk of developing PD.
Article
Chemistry, Inorganic & Nuclear
Iurii A. Orlov, Tatiana P. Sankova, Alexey N. Skvortsov, Sergey A. Klotchenko, Elena I. Sakhenberg, Aleksandra A. Mekhova, Irina V. Kiseleva, Ekaterina Yu. Ilyechova, Ludmila V. Puchkova
Summary: High-affinity copper transporter 1 (CTR1) is essential for transferring copper from the extracellular environment into cells, but the mechanism of copper transfer via CTR1 is not well understood. Mutations or dysregulation of CTR1 expression can result in copper imbalance, leading to various physiological effects.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Multidisciplinary
Ludmila Puchkova, Tatiana P. Sankova, Daria N. Magazenkova, Ekaterina A. Skomorokhova, Iurii A. Orlov, Elena Sakhenberg, Ilya M. Sosnin, Mohammad Al Farroukh, Alexey E. Romanov, Ekaterina Yu Ilyechova
Summary: This study assessed the effect of the shape of silver nanoparticles (AgNPs) on their antibacterial activity, cytotoxicity, and interference with copper metabolism in mice. The results showed that quasi-spherical AgNPs had stronger antibacterial activity than spherical AgNPs, but both had a similar effect on the copper status in mouse blood serum.
ENVIRONMENTAL SCIENCE-NANO
(2022)