Results 21 to 30 of about 109,847 (333)

Synthesis and biological evaluation of new 3-substituted coumarin derivatives as selective inhibitors of human carbonic anhydrase IX and XII

Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
The Carbonic anhydrase isoforms IX and XII play a significant role in regulating the intracellular and extracellular pH in hypoxic tumours abetting the metastasis of solid tumours.
Shaik Mahammad Ghouse, Kavyaraj Bahatam, Andrea Angeli, Gaurav Pawar, Krishna Kartheek Chinchilli, Venkata Madhavi Yaddanapudi, Arifuddin Mohammed, Claudiu T. Supuran, Srinivas Nanduri   +8 more
doaj   +1 more source

Carbonic Anhydrase Inhibitors and Epilepsy: State of the Art and Future Perspectives

Molecules, 2021
Carbonic anhydrases (CAs) are a group of ubiquitously expressed metalloenzymes that catalyze the reversible hydration/dehydration of CO2/HCO3. Thus, they are involved in those physiological and pathological processes in which cellular pH buffering plays ...
L. Ciccone, Chiara Cerri, S. Nencetti, E. Orlandini   +3 more
semanticscholar   +1 more source

Multivalent Carbonic Anhydrases Inhibitors [PDF]

International Journal of Molecular Sciences, 2019
Biomolecular recognition using a multivalent strategy has been successfully applied, this last decade on several biological targets, especially carbohydrate-processing enzymes, proteases, and phosphorylases. This strategy is based on the fact that multivalent interactions of several inhibitory binding units grafted on a presentation platform may ...
Fabrizio Carta, Pascal Dumy, Claudiu T. Supuran, Jean-Yves Winum   +3 more
openaire   +3 more sources

AlphaFold predicts the most complex protein knot and composite protein knots [PDF]

Protein Science. 2022; 31( 8):e4380, 2022
The computer artificial intelligence system AlphaFold has recently predicted previously unknown three-dimensional structures of thousands of proteins. Focusing on the subset with high-confidence scores, we algorithmically analyze these predictions for cases where the protein backbone exhibits rare topological complexity, i.e. knotting.
arxiv   +1 more source

Structure-Activity Relationship Studies of Acetazolamide-Based Carbonic Anhydrase Inhibitors with Activity against Neisseria gonorrhoeae.

ACS Infectious Diseases, 2021
Neisseria gonorrhoeae is an urgent threat to public health in the United States and around the world. Many of the current classes of antibiotics to treat N. gonorrhoeae infection are quickly becoming obsolete due to increased rates of resistance.
Chad S. Hewitt, Nader S. Abutaleb, Ahmed E. M. Elhassanny, A. Nocentini, Xufeng Cao, Devon P Amos, Molly S Youse, Katrina J Holly, A. K. Marapaka, Weiwei An, J. Kaur, Aaron D. Krabill, Ahmed Elkashif, Y. Elgammal, Amanda L. Graboski, C. Supuran, M. Seleem, D. Flaherty   +17 more
semanticscholar   +1 more source

Multitargeting approaches involving carbonic anhydrase inhibitors: hybrid drugs against a variety of disorders

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Carbonic anhydrases (CAs, EC 4.2.1.1) are enzymes involved in a multitude of diseases, and their inhibitors are in clinical use as drugs for the management of glaucoma, epilepsy, obesity, and tumours.
C. Supuran
semanticscholar   +1 more source

Topical carbonic anhydrase inhibitors and glaucoma in 2021: where do we stand?

British Journal of Ophthalmology, 2021
Carbonic anhydrase inhibitors (CAIs) have been used for many decades in the treatment of glaucoma. Systemic CAIs were an early treatment option to lower intraocular pressure by reducing aqueous humour production; however, frequent side effects including ...
Ari M Stoner, A. Harris, F. Oddone, Aditya V. Belamkar, A. V. Verticchio Vercellin, Joshua D Shin, I. Janulevičienė, B. Siesky   +7 more
semanticscholar   +1 more source

Structure‐guided identification of a selective sulfonamide‐based inhibitor targeting the human carbonic anhydrase VA isoform

Archiv der Pharmazie, Volume 356, Issue 1, January 2023., 2023
Combining ligand‐based and structure‐based methodologies, the applied virtual screening approach identified a collection of sulfonamides targeting the human carbonic anhydrase (hCA) VA isoform. 2‐(3,4‐Dihydro‐2H‐quinolin‐1‐yl)‐N‐(4‐sulfamoylphenyl)acetamide was identified as a potent and selective lead compound as a candidate for further exploitation ...
Laura De Luca, Andrea Angeli, Federico Ricci, Claudiu T. Supuran, Rosaria Gitto   +4 more
wiley   +1 more source

Synthesis of New 1H-1,2,3-Triazole Analogs in Aqueous Medium via “Click” Chemistry: A Novel Class of Potential Carbonic Anhydrase-II Inhibitors

Frontiers in Chemistry, 2021
A series of novel 1H-1,2,3-triazole analogs (9a–j) were synthesized via “Click” chemistry and Suzuki–Miyaura cross-coupling reaction in aqueous medium. The compounds were evaluated for their carbonic anhydrase-II enzyme inhibitory activity in vitro.
Satya Kumar Avula, Majid Khan, Majid Khan, Sobia Ahsan Halim, Ajmal Khan, Samia Ahmed Al-Riyami, Rene Csuk, Biswanath Das, Ahmed Al-Harrasi   +8 more
doaj   +1 more source

5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Hydrophilic derivatives of an earlier described series of carbonic anhydrase inhibitors have been designed, prepared and profiled against a panel of carbonic anhydrase isoforms, including the glaucoma-related hCA II.
Stanislav Kalinin, Alexander Kovalenko, Annika Valtari, Alessio Nocentini, Maxim Gureev, Arto Urtti, Mikhail Korsakov, Claudiu T. Supuran, Mikhail Krasavin   +8 more
doaj   +1 more source