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. 2024 Sep 30;15(10):1749-1755.
doi: 10.1021/acsmedchemlett.4c00341. eCollection 2024 Oct 10.

Lasamide, a Potent Human Carbonic Anhydrase Inhibitor from the Market: Inhibition Profiling and Crystallographic Studies

Chiara Baroni  1 , Ilaria D'Agostino  2   3   4 , Gioele Renzi  4 , Jaydeo T Kilbile  5 , Yasinalli Tamboli  6 , Marta Ferraroni  1 , Simone Carradori  3 , Clemente Capasso  7 , Fabrizio Carta  4 , Claudiu T Supuran  4
Affiliations

Lasamide, a Potent Human Carbonic Anhydrase Inhibitor from the Market: Inhibition Profiling and Crystallographic Studies

Chiara Baroni et al. ACS Med Chem Lett. .

Abstract

Lasamide is a synthetic precursor and a contaminant of the diuretic Furosemide manufacturing process and represents a highly valuable building block for fragment-based drug discovery approaches. We assessed the ability of Lasamide to inhibit in vitro the human-expressed Carbonic Anhydrases by means of the stopped-flow technique, and we assessed its binding modes within hCAs II and XII-mimic catalytic clefts by X-ray crystallography. Interestingly, an unprecedented crystal form for the hCA IX mimic H-tag is reported and discussed herein.

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Conflict of interest statement

The authors declare no competing financial interest.

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