Article
Chemistry, Medicinal
Heba T. Abdel-Mohsen, Ahmed M. El Kerdawy, Andrea Petreni, Claudiu T. Supuran
Summary: Novel benzenesulfonamide derivatives were synthesized as carbonic anhydrase inhibitors, demonstrating potent inhibitory activity against multiple CA isoforms at the nanomolar range. The compounds displayed selectivity towards specific isoforms and adopted similar binding modes through molecular docking simulations.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Md. Abu Sufian, Sabina Zamanova, Ahmed M. Shabana, Brianna Kemp, Utpal K. Mondal, Claudiu T. Supuran, Marc A. Ilies
Summary: Carbonic anhydrase IX (CA IX) is an important enzyme involved in tumor survival, metastasis, and resistance to therapy in hypoxic tumor cells. The expression dynamics of CA IX in different oxygen conditions were investigated, along with its correlation with extracellular pH and cell viability. The study found that CA IX expression is retained in hypoxic cancer cells upon reoxygenation to preserve their proliferation ability. The sensitivity of cancer cells to CA IX inhibitors is higher in hypoxia and intermittent hypoxia compared to normoxia.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Hyeong jae Kim, Jeong Hee Hong
Summary: This study found that histamine stimulation leads to mislocalization of carbonic anhydrase 12 (CA12) and induces cellular acidification by enhancing AE2 expression and suppressing NBCn1 expression. Activation of histamine receptors also promotes CA12 endocytosis and restores cellular pH through CaMKII inhibition. Additionally, histamine induces cellular acidification through increased bicarbonate efflux via upregulated AE2 expression and by internalized CA12 and NBCn1.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Ulviye Acar Cevik, Aysen Isik, Ravikumar Kapavarapu, Kaan Kucukoglu, Hayrunnisa Nadaroglu, Hayrani Eren Bostanci, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: In this study, a series of benzimidazole-triazole derivatives were synthesized and evaluated for their inhibitory activity against hCA-I and hCA-II. These compounds displayed good inhibitory activities against both enzymes, with compound 6j being the most active. The cytotoxic effects of compounds 6a-6k on normal cells were also assessed, and non-competitive enzyme inhibition kinetics were observed. Molecular docking studies confirmed the binding interactions between compound 6j and the enzyme's active site, supporting the experimental findings.
JOURNAL OF MOLECULAR STRUCTURE
(2024)
Article
Engineering, Environmental
Yatao Xu, Ziye Wei, Wanlan Yang, Yuxin Guo, Jinjun Shao, Weili Si, Huae Xu, Wenjun Wang, Xiaochen Dong
Summary: Researchers have developed a novel CO therapeutic platform consisting of a carbonic anhydrase IX (CA IX) inhibitor and intelligent responsive CO-releasing molecules (CORMs). The platform actively targets CA IX overexpressed tumor cells for targeted delivery of CORMs. After activation by endogenous H2O2, CORMs can achieve light-induced excited-state intramolecular proton transfer (ESIPT) effect and spatiotemporal controllable release of CO. The constructed CO gas therapeutic platform significantly inhibits tumor growth and metastasis, providing a new direction for tumor gas therapy.
CHEMICAL ENGINEERING JOURNAL
(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)
Review
Biochemistry & Molecular Biology
Anna Maria Reuss, Dominik Groos, Michael Buchfelder, Nicolai Savaskan
Summary: Malignant glioma is a fatal disease with a poor prognosis, characterized by adaptations to hypoxia, glycolytic and angiogenic switch leading to more aggressive and malignant behavior. The acidic tumor microenvironment and metabolic communication between cancer cells enhance invasiveness. The study also highlights the functional consequences of the glycolytic switch on glioma malignancy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Yi Zhang, Chunhong Zhu, Jian Shi, Shigeru Yamanaka, Hideaki Morikawa
Summary: In this study, a structure that facilitates the effective collection of water through biomimicry of fungi is proposed. The structure consists of heterogeneous fiber diameters and a hierarchical structure that provides both hydrophobic and hydrophilic properties. The composite water-collection material was fabricated using a hydrophobic, hierarchical-structured, polyurethane (PU), nanofiber membrane, and hydrophilic filter paper. The water-collection efficiency achieved a rate of 1018.6 mg cm(-2) h(-1) under specific environmental conditions. This research provides new inspiration and effective methods for the development of bioinspired water-collection materials aimed at solving water shortages.
ACS SUSTAINABLE CHEMISTRY & ENGINEERING
(2022)
Article
Urology & Nephrology
An-Ping Xiang, Xiao-Nong Chen, Peng-Fei Xu, Si-Hai Shao, Yue-Fan Shen
Summary: This study investigated the expression intensity of carbonic anhydrase IX (CA-IX) in bladder urothelial carcinoma and its predictive value for the recurrence after transurethral resection of bladder tumor. The results showed that CA-IX is highly expressed in bladder urothelial carcinoma and is associated with tumor stage, differentiation, number, and recurrence. Patients with positive expression of CA-IX had a higher recurrence rate and shorter recurrence time compared to those with negative expression.
Article
Biotechnology & Applied Microbiology
Hui-Min Hao, Yan-Hui Bi, Ning-Ning Wei, Pei-Chong Lin, Shou-Hua Mei, Zhi-Gang Zhou
Summary: This study describes the cloning, characterization, and subcellular localization of Sj beta-CA in Saccharina japonica. The recombinant Sj beta-CA exhibited CO2 hydration and dehydration activities, and was located in the periplasmic space of kelp gametophyte cells. Additionally, a positive correlation between gene transcription and exogenous HCO3- utilization was observed.
JOURNAL OF APPLIED PHYCOLOGY
(2023)
Article
Fisheries
Xiaopeng Wang, Wei Fang, Lei Liu, Yuanyuan Fu, Yueyue Zhou, Dongping Zhou, Xinlian Huang, Changkao Mu, Chunlin Wang
Summary: This study investigated the adaptability of the mud crab to carbonate-alkali waters and cloned the carbonic anhydrase (CA) gene in the mud crab for the first time. The research also explored the mRNA expression and DNA methylation profile of the CA gene under stress in a saline-alkali environment, providing new insights into the adaptation and tolerance mechanisms of the mud crab.
AQUACULTURE REPORTS
(2023)
Article
Immunology
Xianqin Song, Yu Song, Quanping Ma, Kehua Fang, Xiaotian Chang
Summary: This study found that M1 macrophages can increase the expression of CA1 and CA2 to promote atherosclerotic calcification in vascular smooth muscle cells (VSMCs) by secreting TNF-a.
JOURNAL OF INFLAMMATION RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Marta Venturella, Alessandro Falsini, Federica Coppola, Gaia Giuntini, Fabio Carraro, Davide Zocco, Antonio Chiesi, Antonella Naldini
Summary: This study investigated the effects of hypoxia on the release of small extracellular vesicles (sEVs) in two melanoma in vitro models. It was found that melanoma cells release sEVs under both normoxic and hypoxic conditions, but only hypoxia-induced sEVs express CA-IX mRNA and protein. An optimized ELISA assay provided evidence for CA-IX protein expression on the membranes of the sEVs. These CA-IX-positive sEVs may serve as potential biomarkers for liquid biopsy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Andrea Angeli, Niccolo Paoletti, Claudiu T. Supuran
Summary: The development of heterocyclic derivatives, particularly five-membered heterocyclic sulfonamides, as carbonic anhydrase inhibitors (CAIs) has been significant in the field of medicinal chemistry. Oxygen and nitrogen five-membered heterocyclic aromatic rings are important, but the installation of sulfonamide moiety on such heterocycles has not been widely studied. On the other hand, 1,3,4-thiadiazole/thiadiazoline ring-bearing sulfonamides have been extensively used in a variety of pharmaceutically important CAIs. This review focuses on the diverse biological activities and pharmacological/clinical applications of these CAIs.
Article
Environmental Sciences
Imad Hammoudan, Mohammed Chafi
Summary: In this study, the efficacy of 34 pyrazoline derivatives as carbonic anhydrase inhibitors was investigated using computational methods. Quantum descriptors were calculated, and four models were created to predict the pIC50 values of six chemicals in a test set. Each model was validated internally and externally, and Model 3 was chosen based on its higher R-2, R-test(2), and Q(cv)(2) values (R-2 = 0.79, R-test(2) = 0.95, Q(cv)(2) = 0.64). New molecules with significant inhibitory activity could be proposed based on the descriptors of the model.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2023)