Work

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

Year: 2024

Type: article

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.

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.4c00341

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

Institutions: University of Florence, University of Pisa, University of Chieti-Pescara, King Saud bin Abdulaziz University for Health Sciences, King Abdullah International Medical Research Center, National Guard Health Affairs, Institute of Biosciences and Bioresources, National Research Council

Language: English

Topic: Enzyme function and inhibition

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funders: Università degli Studi di Firenze, Università degli Studi G. d'Annunzio Chieti - Pescara, Università di Pisa, King Abdullah International Medical Research Center

Award: G348921432

OpenAlex ID: W4402977540

FWCI: 0.942

Cites: 37

Cited by: 8

Related to: 10