| Literature DB >> 24307504 |
Jiří Brynda1, Pavel Mader, Václav Šícha, Milan Fábry, Kristýna Poncová, Mario Bakardiev, Bohumír Grüner, Petr Cígler, Pavlína Řezáčová.
Abstract
CA inhibitors: Human carbonic anhydrases (CAs) are diagnostic and therapeutic targets. Various carborane cages are shown to act as active-site-directed inhibitors, and substitution with a sulfamide group and other substituents leads to compounds with high selectivity towards the cancer-specific isozyme IX. Crystal structures of the carboranes in the active site provide information that can be applied to the structure-based design of specific inhibitors.Entities:
Keywords: carbonic anhydrases; carboranes; drug discovery; inhibitors; structure elucidation
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Year: 2013 PMID: 24307504 DOI: 10.1002/anie.201307583
Source DB: PubMed Journal: Angew Chem Int Ed Engl ISSN: 1433-7851 Impact factor: 15.336