Caspofungin uptake is mediated by a high-affinity transporter in Candida albicans

Antimicrobial Agents and Chemotherapy
Padmaja PaderuDavid S Perlin

Abstract

The uptake of the echinocandin drug caspofungin acetate in Candida albicans was evaluated at drug levels at or near the MIC for the organism. Maximal uptake was achieved in 10 min and was energy independent. A saturable transport system, consistent with a facilitated-diffusion carrier, was observed with the unlabeled drug competing with the labeled drug for uptake and efflux. More than 90% of the transported drug was observed in a single kinetic compartment that was available for efflux, indicating that the drug was free in the cytoplasm following uptake. Efflux was also energy independent but was sensitive to the presence of a fully loaded carrier on both faces of the bilayer. Overall, the data presented are consistent with the presence of a high-affinity facilitated-diffusion transporter that mediates caspofungin uptake and could be a potential source of transport-related reduced susceptibility.

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Citations

Mar 7, 2013·Applied Microbiology and Biotechnology·Tamás EmriIstván Pócsi
Apr 11, 2007·Antimicrobial Agents and Chemotherapy·Padmaja PaderuDavid S Perlin
Jan 16, 2013·Antimicrobial Agents and Chemotherapy·Antigoni ElefantiJoseph Meletiadis
Jun 28, 2005·Antimicrobial Agents and Chemotherapy·Marybeth A Maligie, Claude P Selitrennikoff
Apr 2, 2005·Biological & Pharmaceutical Bulletin·Shinji EbaraMasataka Nakamura
Mar 25, 2008·Therapeutics and Clinical Risk Management·Gregory EschenauerPeggy L Carver
Sep 1, 2005·BioDrugs : Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy·Brian C Monk, David R K Harding
Dec 24, 2010·Drugs·Sharon C-A ChenTania C Sorrell
Apr 30, 2011·Future Microbiology·David S Perlin
Sep 16, 2015·Critical Reviews in Microbiology·Jessica C Song, David A Stevens
Oct 7, 2009·Expert Review of Anti-infective Therapy·Maria Teresa FeraAngelina De Sarro
Apr 13, 2007·Expert Opinion on Drug Metabolism & Toxicology·William W HopeThomas J Walsh
Jan 11, 2012·International Journal of Antimicrobial Agents·Fedja FarowskiCarsten Müller
May 24, 2006·Pharmacotherapy·Christopher D MillerDavid S Perlin
May 4, 2005·Yeast
May 27, 2020·Journal of the Royal Society, Interface·Olga A NevIvana Gudelj
Sep 16, 2005·Drugs·Paul L McCormack, Caroline M Perry
May 8, 2021·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·M Ángeles CurtoJuan C G Cortés
Dec 17, 2019·Journal of Medicinal Chemistry·Emily K DennisSylvie Garneau-Tsodikova

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