Work

Unsymmetrical Cysteine Disulfides as Carbonic Anhydrase Inhibitors

Year: 2021

Type: article

Abstract: A small library of unsymmetrical cysteine disulfides as four aliphatic, three aromatic and one heteroaromatic were evaluated for their inhibition of two important carbonic anhydrase (CA) enzymes, namely human carbonic anhydrase isoenzymes I (hCA I) and II (hCA II). IC50 values were recorded in the low nanomolar range (8.6–18.3 nM for hCA I and 42.9–99.9 nM for hCA II). The inhibition activities were significantly superior to those of the clinically available CA inhibitor acetazolamide for hCA I, while only marginally inferior for hCA II. These results highlight the relevance of screening small molecules as potential CA inhibitors (CAIs).

Source: Russian Journal of Bioorganic Chemistry

DOI: 10.1134/s1068162021050344

Authors: N. Stellenboom, R. Hunter, M. Caira, A. Oztekin, K. Zilbeyaz

Institution: University of Cape Town

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

OpenAlex ID: W3207131410

FWCI: 0.14

Cites: 48

Cited by: 4

Related to: 10