AI Article Synopsis
- - Lasamide, a synthetic byproduct of the diuretic Furosemide manufacturing, is highlighted as a valuable component for drug discovery techniques.
- - Researchers tested Lasamide's effectiveness in inhibiting human Carbonic Anhydrases (hCAs) using a stopped-flow method and examined its binding through X-ray crystallography.
- - The study introduces a new crystal form for a specific Carbonic Anhydrase mimic (hCA IX), which is discussed in detail.
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.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11472397 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.4c00341 | DOI Listing |
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