Article
Biochemistry & Molecular Biology
Dimitrios Tsikas, Stepan Gambaryan
Summary: The carbonic anhydrase (CA) family not only catalyzes the reversible hydration of CO2 to bicarbonate, but also possesses esterase and phosphatase activity. Recent studies have shown that CA II can convert inorganic nitrite to nitric oxide and nitrous anhydride, potentially representing a bioactivation of nitrite. The key role of L-cysteine in this bioactivation process is supported by new experimental data.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Eric Bernabeu, Jose Maria Miralles-Robledillo, Micaela Giani, Elena Valdes, Rosa Maria Martinez-Espinosa, Carmen Pire
Summary: Research on using haloarchaea for denitrification in saline environments is still in the early stages and requires further investigation to understand the molecular mechanisms and optimize their use in bioremediation.
Article
Chemistry, Multidisciplinary
Gayathri Kolliyedath, Taraknath Chattopadhyay, Aditesh Mondal, Aiswarya Panangattu, Girish Muralikrishnan, Subrata Kundu
Summary: This study systematically investigates the reactivity of nitrite anions, nitrous acid, and organonitrite at the redox-inactive zinc(II) site, revealing the transformation mechanism to nitric oxide on the zinc(II) coordination motif.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Biochemistry & Molecular Biology
Toni C. Denner, Niels Heise, Julian Zacharias, Oliver Kraft, Sophie Hoenke, Rene Csuk
Summary: Acetylated triterpenoids were transformed into succinyl-spacered acetazolamide conjugates and tested for their inhibitory actvity on carbonic anhydrase II and cytotoxicity on human tumor cell lines and non-malignant fibroblasts. The conjugates derived from betulin and glycyrrhetinic acid showed the strongest inhibition, while those derived from ursolic or oleanolic acid were weaker inhibitors but had lower cytotoxicity. A betulin-derived conjugate displayed a Ki value of 0.129 μM and an EC50 value of 8.5 μM for human A375 melanoma cells.
Article
Biochemistry & Molecular Biology
Emilio Bueno, Daniel Mania, Socorro Mesa, Eulogio J. Bedmar, Asa Frostegard, Lars R. Bakken, Maria J. Delgado
Summary: The paper investigates the nitrogen-fixing ability of Bradyrhizobium diazoefficiens, a symbiotic bacterium found in soybeans. It explores the regulatory mechanisms and factors affecting nitrogen fixation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Agriculture, Multidisciplinary
Taobing Yu, Xiangyang Fang, Yan Liu, Huadong Zang, Zhaohai Zeng, Yadong Yang
Summary: This study examined the impact of long-term fertilization and irrigation on soil denitrifier communities. The results showed that irrigation significantly increased the abundance of denitrifier genes and had a dominant role in altering community structure. Soil moisture and pH were also found to be closely related to gene abundance and community structure.
AGRICULTURE ECOSYSTEMS & ENVIRONMENT
(2023)
Article
Engineering, Environmental
Yiyihui Hong, Qianqian Tu, Hong Cheng, Xiaoliu Huangfu, Ziwei Chen, Qiang He
Summary: Silver nanoparticles (Ag-NPs) can generate nitrous oxide (N2O). Low doses of Ag-NPs slightly inhibit N2O generation, while high doses stimulate N2O emissions. Accumulated high Ag-NP content on biofilm surfaces creates anaerobic micro-environments, promoting N2O release through the nitrite reduction pathway. Metagenomic analysis links high dose Ag-NP exposure to increased expression of narB and nirK genes, resulting in higher N2O emissions.
Article
Chemistry, Medicinal
Gustavo Provensi, Alessia Costa, Barbara Rani, Maria Vittoria Becagli, Fabio Vaiano, Maria Beatrice Passani, Damiano Tanini, Antonella Capperucci, Simone Carradori, Jacobus P. Petzer, Anel Petzer, Daniela Vullo, Gabriele Costantino, Patrizio Blandina, Andrea Angeli, Claudiu T. Supuran
Summary: This study reported the synthesis of β-arylchalcogeno amines with structural similarity to amphetamine, which showed good activation properties for certain enzymes in the brain. In vivo evaluation demonstrated the procognitive effects of these compounds without causing unwanted side effects. These findings suggest the potential utility of these compounds for improving cognitive decline associated with neurodegenerative and psychiatric diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Ozlem Akgul, Srishti Singh, Jacob T. Andring, Robert McKenna, Silvia Selleri, Fabrizio Carta, Andrea Angeli, Claudiu T. Supuran
Summary: A series of taurine substituted sulfonamide derivatives with ureido moiety at the tail section were synthesized as selective inhibitors of tumor associated human Carbonic Anhydrase (CA) IX and XII. These derivatives showed a strong dependence on the presence of ureido moiety and demonstrated highly stabilized ligand-protein complex with specific amino acid residues in both hCA II and hCA IX-mimic.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Davide Moi, Serena Vittorio, Andrea Angeli, Gianfranco Balboni, Claudiu T. Supuran, Valentina Onnis
Summary: A series of hydrazonobenzenesulfonamides were designed, synthesized and evaluated for their inhibitory activity against human carbonic anhydrase (hCA) isoforms. The synthesized compounds showed inhibitory activity at low nanomolar levels against hCA I, II, IX and XII, with selectivity against hCA II isoform, as well as hCA IX and XII isoforms. Docking studies were conducted to understand the activity and selectivity of the most potent and selective hydrazones towards different CA isoforms.
Article
Biochemistry & Molecular Biology
Javier Quero, Jose Carlos Royo, Beatrice Fodor, Maria Concepcion Gimeno, Jesus Osada, Maria Jesus Rodriguez-Yoldi, Elena Cerrada
Summary: Two new families of dithiocarbamate gold(I) complexes derived from benzenesulfonamide with phosphine or carbene as ancillary ligands have been synthesized. These complexes showed high anticancer activity and cancer cell selectivity, with the more lipophilic complexes displaying the highest activity. The complexes induced cell death through intrinsic apoptosis and caused cell cycle arrest with p53 activation. Additionally, the complexes acted as multi-target anticancer drugs by inhibiting the activity of enzymes and altering the redox balance.
Article
Multidisciplinary Sciences
Huijuan Guo, Yanjing Zhang, Bingyu Li, Chenwei Li, Qingyun Shi, Keyan Zhu-Salzman, Feng Ge, Yucheng Sun
Summary: The difference in virus transmission between winged and wingless aphids is correlated with the secretion of the salivary protein CA-II, which enhances the vector role of winged aphids.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Chemistry, Medicinal
Ayse Halic Poslu, Safak Esra Aslan, Gamze Koz, Esra Senturk, Omer Koz, Murat Senturk, Ayse Nalbantsoy, Aykut Oztekin, Deniz Ekinci
Summary: This study synthesized a series of derivatives and evaluated their cytotoxic activity and enzyme inhibitory potency. The results showed that one newly synthesized derivative exhibited high toxicity against prostate adenocarcinoma cells, and most derivatives had more effective inhibitory action than existing drugs. Therefore, these derivatives are potential drug candidates.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Medicinal
Krishna Kartheek Chinchilli, Ravikumar Akunuri, Shaik Mahammad Ghouse, Devandla Soujanya, Andrea Angeli, Ramulu Parupalli, Mohammed Arifuddin, Venkata Madhavi Yaddanapudi, Claudiu T. Supuran, Srinivas Nanduri
Summary: Rhodanine and its derivatives are a valuable class of heterocycles with diverse biological properties, including anticancer, antibacterial, and anti-mycobacterial activities. In this study, new Rhodanine derivatives were synthesized and evaluated for their inhibitory activity against carbonic anhydrase isoforms. The compounds showed good inhibitory activity against cytosolic isoform hCA II and tumor-associated hCA IX. The mechanism of action was supported by molecular docking studies.
ARCHIV DER PHARMAZIE
(2023)
Review
Chemistry, Medicinal
Shubham Kumar, Sandeep Rulhania, Shalini Jaswal, Vikramdeep Monga
Summary: Carbonic anhydrase is an important enzyme involved in various physiological and pathological processes, with 16 different isoforms in humans. Inhibitors targeting different isoforms of carbonic anhydrase have clinical applications in treating various diseases, but current drugs lack selectivity leading to undesired side effects. Efforts are being made to develop novel isoform-selective inhibitors of carbonic anhydrase for therapeutic implications.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Alessio Nocentini, Mariangela Ceruso, Silvia Bua, Carrie L. Lomelino, Jacob T. Andring, Robert McKenna, Cecilia Lanzi, Silvia Sgambellone, Riccardo Pecori, Rosanna Matucci, Luca Filippi, Paola Gratteri, Fabrizio Carta, Emanuela Masini, Silvia Selleri, Claudiu T. Supuran
JOURNAL OF MEDICINAL CHEMISTRY
(2018)
Article
Endocrinology & Metabolism
Stephanie J. Sacharow, Elizabeth E. Dudenhausen, Carrie L. Lomelino, Lance Rodan, Christelle Moufawad El Achkar, Heather E. Olson, Casie A. Genetti, Pankaj B. Agrawal, Robert McKenna, Michael S. Kilberg
MOLECULAR GENETICS AND METABOLISM
(2018)
Review
Biochemistry & Molecular Biology
Srishti Singh, Carrie L. Lomelino, Mam Y. Mboge, Susan C. Frost, Robert McKenna
Article
Chemistry, Medicinal
Carrie L. Lomelino, Akilah B. Murray, Claudiu T. Supuran, Robert McKenna
ACS MEDICINAL CHEMISTRY LETTERS
(2018)
Article
Biochemical Research Methods
Carrie L. Lomelino, Jin Kyun Kim, Cheol Lee, Seon Woo Lim, Jacob T. Andring, Brian P. Mahon, Moses Chung, Chae Un Kim, Robert McKenna
ACTA CRYSTALLOGRAPHICA SECTION F-STRUCTURAL BIOLOGY COMMUNICATIONS
(2018)
Article
Chemistry, Medicinal
Alessio Nocentini, Elena Trallori, Srishti Singh, Carrie L. Lomelino, Gianluca Bartolucci, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Robert McKenna, Paola Gratteri, Claudiu T. Supuran
JOURNAL OF MEDICINAL CHEMISTRY
(2018)
Article
Immunology
Guan Yang, Bianca L. Artiaga, Carrie L. Lomelino, Anitha D. Jayaprakash, Ravi Sachidanandam, Robert Mckenna, John P. Driver
JOURNAL OF IMMUNOLOGY
(2019)
Article
Biochemical Research Methods
Carrie L. Lomelino, Robert McKenna
ACTA CRYSTALLOGRAPHICA SECTION F-STRUCTURAL BIOLOGY COMMUNICATIONS
(2019)
Article
Genetics & Heredity
Aruna S. Jaiswal, Elizabeth A. Williamson, Gayathri Srinivasan, Kimi Kong, Carrie L. Lomelino, Robert McKenna, Christi Walter, Patrick Sung, Satya Narayan, Robert Hromas
Article
Chemistry, Medicinal
Andrea Petreni, Alessandro Bonardi, Carrie Lomelino, Sameh M. Osman, Zeid A. ALOthman, Wagdy M. Eldehna, Radwan El-Haggar, Robert McKenna, Alessio Nocentini, Claudiu T. Supuran
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Medicinal
Silvia Bua, Carrie Lomelino, Akilah B. Murray, Sameh M. Osman, Zeid A. ALOthman, Murat Bozdag, Hatem A. Abdel-Aziz, Wagdy M. Eldehna, Robert McKenna, Alessio Nocentini, Claudiu T. Supuran
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Medicinal
Alessandro Bonardi, Alessio Nocentini, Silvia Bua, Jacob Combs, Carrie Lomelino, Jacob Andring, Laura Lucarini, Silvia Sgambellone, Emanuela Masini, Robert McKenna, Paola Gratteri, Claudiu T. Supuran
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Medicinal
Gioele Vannozzi, Daniela Vullo, Andrea Angeli, Marta Ferraroni, Jacob Combs, Carrie Lomelino, Jacob Andring, Robert Mckenna, Gianluca Bartolucci, Marco Pallecchi, Laura Lucarini, Silvia Sgambellone, Emanuela Masini, Fabrizio Carta, Claudiu T. Supuran
Summary: A one-pot procedure was developed for synthesizing asymmetrical ureido-containing benzenesulfonamides, generating a library of new compounds that were evaluated for their inhibitory properties against carbonic anhydrases in vitro. The best compounds were then screened for their ability to reduce intraocular pressure in glaucomatous rabbits. X-ray crystallography was used to assess the binding modes of selected compounds.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Alessandro Bonardi, Silvia Bua, Jacob Combs, Carrie Lomelino, Jacob Andring, Sameh Mohamed Osman, Alessandra Toti, Lorenzo Di Cesare Mannelli, Paola Gratteri, Carla Ghelardini, Robert McKenna, Alessio Nocentini, Claudiu T. Supuran
Summary: Human carbonic anhydrase isoforms IX and XII have been confirmed as anticancer targets, with three-tails approach showing higher selectivity against tumor-associated isoforms and demonstrating anti-proliferative effects in various cancer cell lines. X-ray crystallography studies have been conducted to investigate the binding mode of these inhibitors, providing valuable insights for potential cancer treatments.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Carrie L. Lomelino, Jacob T. Andring, Robert McKenna
INTERNATIONAL JOURNAL OF MEDICINAL CHEMISTRY
(2018)
Correction
Biochemistry & Molecular Biology
Siew Chin Chan, Chih-Wei Tung, Chia-Wei Lin, Yun-Shiuan Tung, Po-Min Wu, Pei-Hsun Cheng, Chuan-Mu Chen, Shang-Hsun Yang
FREE RADICAL BIOLOGY AND MEDICINE
(2024)
Article
Biochemistry & Molecular Biology
Suyuan Liu, Meiling Tan, Jiangxue Cai, Chenxuan Li, Miaoxin Yang, Xiaoxiao Sun, Bin He
Summary: This study reveals that the antibiotic doxycycline effectively inhibits NLRP3 inflammasome activation by targeting mitochondrial translation and mtDNA synthesis, offering potential for the treatment of NLRP3-related diseases.
FREE RADICAL BIOLOGY AND MEDICINE
(2024)
Article
Biochemistry & Molecular Biology
Hao Liu, Nana Li, Ge Kuang, Xia Gong, Ting Wang, Jun Hu, Hui Du, Minxuan Zhong, Jiashi Guo, Yao Xie, Yang Xiang, Shengwang Wu, Yiling Yuan, Xinru Yin, Jingyuan Wan, Ke Li
Summary: Protectin D1 (PTD1) improves hepatic steatosis, inflammation and fibrosis in a NASH mouse model by inhibiting the activation of TLR4 downstream signaling pathway, possibly through upregulation of IRAK-M expression, suggesting a potential new treatment for NASH.
FREE RADICAL BIOLOGY AND MEDICINE
(2024)