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

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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Publication Details

Journal
ACS Medicinal Chemistry Letters
Published
2024-09-30
DOI
https://doi.org/10.1021/acsmedchemlett.4c00341
Citations
8
Primary Topic
Enzyme function and inhibition
Type
article
Field-Weighted Citation Impact
1.87

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article

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

Clemente Capasso, Yasinalli Tamboli, Jaydeo T. Kilbile, Marta Ferraroni et al.
8 citations
ACS Medicinal Chemistry Letters
Enzyme function and inhibition
1.87
article

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

Clemente Capasso, Yasinalli Tamboli, Jaydeo T. Kilbile, Marta Ferraroni, Claudiu T. Supuran, Simone Carradori, Fabrizio Carta, Ilaria D’Agostino, Gioele Renzi, Chiara Baroni
article en
8 citations

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.

ACS Medicinal Chemistry LettersVol. 15(10)
University of Pisa (IT), King Saud bin Abdulaziz University for Health Sciences (SA), University of Chieti-Pescara (IT), King Abdullah International Medical Research Center (SA), Institute of Biosciences and Bioresources (IT), National Research Council (IT), University of Florence (IT), National Guard Health Affairs (SA)
Università degli Studi di Firenze, Università degli Studi G. d'Annunzio Chieti - Pescara, Università di Pisa, King Abdullah International Medical Research Center
Openalex Percentile: Top 14%
Enzyme function and inhibition
1.87
DOIOpen Access PDFOpenAlex
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