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Nat Ecol Evol ; 6(10): 1501-1515, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-36050399

RESUMO

Antimicrobial resistance is an emerging threat for public health. The success of resistance mutations depends on the trade-off between the benefits and costs they incur. This trade-off is largely unknown and uncharacterized for antifungals. Here, we systematically measure the effect of all amino acid substitutions in the yeast cytosine deaminase Fcy1, the target of the antifungal 5-fluorocytosine (5-FC, flucytosine). We identify over 900 missense mutations granting resistance to 5-FC, a large fraction of which appear to act through destabilization of the protein. The relationship between 5-FC resistance and growth sustained by cytosine deamination is characterized by a sharp trade-off, such that small gains in resistance universally lead to large losses in canonical enzyme function. We show that this steep relationship can be explained by differences in the dose-response functions of 5-FC and cytosine. Finally, we observe the same trade-off shape for the orthologue of FCY1 in Cryptoccocus neoformans, a human pathogen. Our results provide a powerful resource and platform for interpreting drug target variants in fungal pathogens as well as unprecedented insights into resistance-function trade-offs.


Assuntos
Antifúngicos , Flucitosina , Antifúngicos/farmacologia , Citosina , Citosina Desaminase/genética , Citosina Desaminase/metabolismo , Citosina Desaminase/farmacologia , Flucitosina/farmacologia , Nutrientes , Saccharomyces cerevisiae/genética
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