Article
Chemistry, Medicinal
Niccolo Chiaramonte, Andrea Angeli, Silvia Sgambellone, Alessandro Bonardi, Alessio Nocentini, Gianluca Bartolucci, Laura Braconi, Silvia Dei, Laura Lucarini, Elisabetta Teodori, Paola Gratteri, Bernhard Wuensch, Claudiu T. Supuran, Maria Novella Romanelli
Summary: Targeting carbonic anhydrases is a strategy for treating various diseases. In this study, a new series of chiral piperazine compounds was synthesized to widen the structure-activity relationships of potent human carbonic anhydrase inhibitors. Some of the synthesized compounds showed high inhibitory activity.
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)
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
Biochemistry & Molecular Biology
Morteza Abdoli, Viviana De Luca, Clemente Capasso, Claudiu T. Supuran, Raivis Zalubovskis
Summary: A series of novel compounds were synthesized and evaluated for their inhibition of eukaryotic and human carbonic anhydrases. The results showed good inhibition against some target enzymes and weaker inhibition against others. These findings are important for the search for potential antifungal drugs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Volodymyr Brovarets, Sergii Slyvchuk, Stepan Pilyo, Athina Geronikaki, Claudiu T. Supuran
Summary: Carbonic anhydrases play a crucial role in living organisms and a series of new compounds were synthesized and tested as potential inhibitors in this study. Some of the derivatives showed interesting inhibitory activity towards tumor-associated isoforms. Computational procedures were also used to investigate the binding mode of these compounds within the active site.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Amarjyoti Das Mahapatra, Aarfa Queen, Mohd Yousuf, Parvez Khan, Afzal Hussain, Md. Tabish Rehman, Mohamed F. Alajmi, Bhaskar Datta, Md. Imtaiyaz Hassan
Summary: Inhibitors of carbonic anhydrase have the potential to address various diseases. This research focuses on developing a new scaffold, oxazole-5(4H)-one derivatives, for the selective inhibition of human carbonic anhydrase VA (hCAVA). Two compounds show high binding affinity and inhibit the expression of CAVA and GLUT4 in adipocytes.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Medicinal
Rehab F. Ahmed, Walaa R. Mahmoud, Nagwa M. Abdelgawad, Marwa A. Fouad, Mona F. Said
Summary: This study designed a series of novel carbonic anhydrase inhibitors and evaluated their inhibitory activity and anticancer activity. Compounds 4b, 5b, 5d, 5e, 6b, 9b, 9e, and 11b showed significant inhibitory activity against both CA isoforms, while compound 6e exhibited significant cytostatic activity against multiple cancer cell lines, suggesting its potential as a promising anticancer drug.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Nader S. Abutaleb, Ahmed E. M. Elhassanny, Alessio Nocentini, Chad S. Hewitt, Ahmed Elkashif, Bruce R. Cooper, Claudiu T. Supuran, Mohamed N. Seleem, Daniel P. Flaherty
Summary: Ethoxzolamide exhibits potent anti-gonococcal activity and warrants further investigation as an effective agent against Neisseria gonorrhoeae.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
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
Biochemistry & Molecular Biology
Saeid Hadi Ali Janvand, Lucy Kate Ladefoged, Asta Zubriene, Andrius Sakalauskas, Gunna Christiansen, Virginija Dudutiene, Birgit Schiott, Daumantas Matulis, Vytautas Smirnovas, Daniel E. Otzen
Summary: Fluorinated sulfonamide compounds can inhibit the formation of amyloid fibrils, potentially providing therapeutic effects against amyloid-related disorders such as Parkinson's, Alzheimer's, and type 2 diabetes, possibly by maintaining insulin in its native monomeric state.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Biochemistry & Molecular Biology
Viviana De Luca, Simone Giovannuzzi, Claudiu T. Supuran, Clemente Capasso
Summary: Blocking bacterial carbonic anhydrases can reduce pathogen survival and fitness. The recombinant M. sciuri gamma-CA showed significant hydratase activity, with a sulfonamide inhibitory profile different from that of MscCA beta, suggesting the possibility of developing novel CA class-specific inhibitors.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Multidisciplinary
Giulia Degiacomi, Beatrice Gianibbi, Deborah Recchia, Giovanni Stelitano, Giuseppina Ivana Truglio, Paola Marra, Alessandro Stamilla, Vadim Makarov, Laurent Robert Chiarelli, Fabrizio Manetti, Maria Rosalia Pasca
Summary: To combat drug-resistant strains of Mycobacterium tuberculosis, new targets are needed to develop effective drugs. This study demonstrates a workflow for validating new targets and inhibitors using genetic, in silico, and enzymological approaches. The essential role of CanB in the survival of the pathogen was confirmed through conditional mutants, and three molecules were selected as inhibitors of CanB, showing bactericidal activity against wild-type and conditional mutants of M. tuberculosis.
Article
Biochemistry & Molecular Biology
Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Volodymyr Brovarets, Roman Vydzhak, Svitlana Panchishin, Athina Geronikaki, Claudiu T. Supuran
Summary: A series of novel benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with bulky moieties were synthesized and investigated for their inhibitory effects on various human carbonic anhydrase isoforms. Isoform-selective inhibitors were obtained, with a computational approach employed to explain the observed selectivity, potentially useful in drug design for developing inhibitors with pharmacological applications such as antiglaucoma, diuretic, antitumor, or anti-cerebral ischemia drugs.
Article
Biochemistry & Molecular Biology
Nora Astrain-Redin, Niccolo Paoletti, Daniel Plano, Alessandro Bonardi, Paola Gratteri, Andrea Angeli, Carmen Sanmartin, Claudiu T. Supuran
Summary: In the search for new cancer treatments, organoselenium compounds and carbonic anhydrase inhibitors have shown promise. Selenium-containing compounds, especially selenols, have demonstrated potent inhibition of tumor-associated CA isoforms. In this study, selenoesters combining NSAIDs and natural product fragments were evaluated as nonclassical inhibitors of tumor-associated CA isoforms.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Roman M. Vydzhak, Svitlana Y. Panchishin, Volodymyr Brovarets, Viviana De Luca, Clemente Capasso, Athina Geronikaki, Claudiu T. Supuran
Summary: A series of sulfanilamide derivatives containing heterocyclic carboxamide moieties were evaluated as CA inhibitors against several isoforms of human CA, with some showing selectivity towards hCA II and hCA XII. Molecular docking of some compounds on isoforms hCA II and XII was performed to understand their interaction with active site amino acid residues, rationalizing the reported inhibitory activity.
Article
Veterinary Sciences
Mary R. Telle, Nickolas Chen, Daniel Shinsako, Julie A. Kiland, Kazuya Oikawa, Ralph Moller Trane, Gillian J. McLellan
VETERINARY OPHTHALMOLOGY
(2019)
Article
Pathology
Billie Beckwith-Cohen, Allison Hoffman, Gillian J. McLellan, Richard R. Dubielzig
VETERINARY PATHOLOGY
(2019)
Article
Neurosciences
Billie Beckwith-Cohen, Lars C. Holzhausen, Tzu-Ming Wang, Rajit Rajappa, Richard H. Kramer
JOURNAL OF NEUROSCIENCE
(2019)
Article
Neurosciences
Michael Telias, Bristol Denlinger, Zachary Helft, Casey Thornton, Billie Beckwith-Cohen, Richard H. Kramer
Article
Veterinary Sciences
Harathi Krishnan, Scott Hetzel, Gillian J. McLellan, Ellison Bentley
VETERINARY OPHTHALMOLOGY
(2020)
Article
Genetics & Heredity
Andrew C. Lewin, Lyndon M. Coghill, Gillian J. McLellan, Ellison Bentley, Konstantin G. Kousoulas
Article
Ophthalmology
Kevin C. Snyder, Kazuya Oikawa, Jeremy Williams, Julie A. Kiland, Shaile Gehrke, Leandro B. C. Teixeira, Alex S. Huang, Gillian J. McLellan
TRANSLATIONAL VISION SCIENCE & TECHNOLOGY
(2019)
Article
Neurosciences
Kazuya Oikawa, James N. Ver Hoeve, Leandro B. C. Teixeira, Kevin C. Snyder, Julie A. Kiland, N. Matthew Ellinwood, Gillian J. McLellan
MOLECULAR NEUROBIOLOGY
(2020)
Article
Veterinary Sciences
Andrea L. Minella, Julie A. Kiland, Shawna Gloe, Gillian J. McLellan
Summary: The study compared the accuracy and precision of two types of tonometers in measuring intraocular pressure in ex vivo canine eyes. Results showed that the TONOVET Plus and TV01 were more accurate than the Tono-Pen VET and Tono-Pen AVIA Vet, especially at higher IOPs. Additionally, the precision was high for all devices, with the TONOVET Plus being the most precise in the lower range and the TV01 in the higher range of IOP.
VETERINARY OPHTHALMOLOGY
(2021)
Article
Ophthalmology
Kazuya Oikawa, Leandro B. C. Teixeira, Adib Keikhosravi, Kevin W. Eliceiri, Gillian J. McLellan
Summary: By studying the optic nerve head structure in domestic cats, researchers have found similarities with humans and non-human primates, including diverse cell types and a robust collagen structure, which could be crucial in enhancing the understanding of the pathological processes in glaucomatous optic neuropathy.
EXPERIMENTAL EYE RESEARCH
(2021)
Article
Veterinary Sciences
Caryn E. Plummer, Dineli Bras, Sinisa Grozdanic, Andras M. Komaromy, Gillian McLellan, Paul Miller, John S. Sapienza, Leandro Teixeira, Terah Webb
Summary: The survey of 199 veterinary ophthalmology clinicians found that a variety of topical anti-hypertensive drugs were used but dorzolamide, timolol, and combination products were the most common. Majority of clinicians did not use concurrent anti-inflammatory medications, with some opting for prednisolone acetate or dexamethasone. Only 40% used neuroprotectant agents, with amlodipine and Ocu-Glo being the most commonly prescribed. Recommendations for re-examination intervals varied, with most clinicians suggesting re-evaluations every 3 to 6 months.
VETERINARY OPHTHALMOLOGY
(2021)
Article
Veterinary Sciences
Mary Rebecca Telle, Kevin C. Snyder, Kazuya Oikawa, Jacob P. Nilles, Shaile Gehrke, Leandro B. C. Teixeira, Julie A. Kiland, Alex Huang, Gillian J. McLellan
Summary: In canine eyes with PACG, abnormalities in the post-trabecular aqueous outflow channels were identified through AA and OCT, while normal eyes showed normal outflow patterns.
VETERINARY OPHTHALMOLOGY
(2022)
Article
Ophthalmology
Kore Chan, Mrinalini Hoon, Bikash R. Pattnaik, James N. Ver Hoeve, Brad Wahlgren, Shawna Gloe, Jeremy Williams, Brenna Wetherbee, Julie A. Kiland, Kara R. Vogel, Erwin Jansen, Gajja Salomons, Dana Walters, Jean-Baptiste Roullet, K. Michael Gibson, Gillian J. McLellan
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE
(2020)
Article
Ophthalmology
Yasmin Bradfield, Thaisa Barbosa, Barbara Blodi, Stuart W. Tompson, Gillian J. McLellan, Michael Struck, Terri L. Young
OPHTHALMOLOGY GLAUCOMA
(2019)