In Vitro Activity of APX2041, a New Gwt1 Inhibitor, and In Vivo Efficacy of the Prodrug APX2104 against Aspergillus fumigatus
| Autor: | John A. Allen, E. Keats Shwab, Yohannes G. Asfaw, Praveen R. Juvvadi, William J. Steinbach, Shareef Shaheen, D. Christopher Cole, Karen Joy Shaw, Mili Kapoor |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
0301 basic medicine
Antifungal medicine.drug_class 030106 microbiology Aspergillosis Microbiology Aspergillus fumigatus 03 medical and health sciences 0302 clinical medicine In vivo medicine Pharmacology (medical) Experimental Therapeutics 030212 general & internal medicine skin and connective tissue diseases Pharmacology biology business.industry Prodrug biology.organism_classification medicine.disease bacterial infections and mycoses In vitro Infectious Diseases Murine model business |
| Zdroj: | Antimicrob Agents Chemother |
| Popis: | Invasive aspergillosis (IA) due to Aspergillus fumigatus is a deadly infection for which new antifungal therapies are needed. Here, we demonstrate the efficacy of a Gwt1 inhibitor, APX2041, and its prodrug, APX2104, against A. fumigatus. The wild-type, azole-resistant, and echinocandin-resistant A. fumigatus strains were equally susceptible to APX2041 in vitro. APX2104 treatment in vivo significantly prolonged survival of neutropenic mice challenged with the wild-type and azole-resistant strains, revealing APX2104 as a potentially promising therapeutic against IA. |
| Databáze: | OpenAIRE |
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