| Literature DB >> 36050399 |
Philippe C Després1,2,3,4, Angel F Cisneros5,6,7,8, Emilie M M Alexander5,6,7,8, Ria Sonigara5,6,8,9, Cynthia Gagné-Thivierge5,6,7,8,9, Alexandre K Dubé5,6,7,8,9, Christian R Landry10,11,12,13,14.
Abstract
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.Entities:
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Year: 2022 PMID: 36050399 DOI: 10.1038/s41559-022-01846-4
Source DB: PubMed Journal: Nat Ecol Evol ISSN: 2397-334X Impact factor: 19.100