Specific interactions between the Candida albicans ABC transporter Cdr1p ectodomain and a d-octapeptide derivative inhibitor

• Published in: Molecular microbiology Vol. 85; no. 4; pp. 747 - 767
• Main Authors: Niimi, Kyoko, Harding, David R. K., Holmes, Ann R., Lamping, Erwin, Niimi, Masakazu, Tyndall, Joel D. A., Cannon, Richard D., Monk, Brian C.
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.08.2012; Blackwell
• Subjects: ABC transporters; Biological and medical sciences; Candida albicans; Candida albicans - enzymology; Drug Resistance, Fungal; Enzyme Inhibitors - metabolism; Fundamental and applied biological sciences. Psychology; Fungal Proteins - antagonists & inhibitors; Fungal Proteins - genetics; Fungal Proteins - metabolism; Fungi; Inhibitor drugs; Membrane Transport Proteins - genetics; Membrane Transport Proteins - metabolism; Microbial Sensitivity Tests; Microbiology; Miscellaneous; Models, Molecular; Mutation; Mycology; Oligopeptides - metabolism; Protein Binding; Protein Conformation; Saccharomyces cerevisiae; Suppression, Genetic; Yeast; Fungi; Candida albicans; Octapeptide; Yeast; Fungi Imperfecti; ABC transporter

Summary Overexpression of the Candida albicans ATP‐binding cassette transporter CaCdr1p causes clinically significant resistance to azole drugs including fluconazole (FLC). Screening of a ∼ 1.89 × 106 member d‐octapeptide combinatorial library that concentrates library members at the yeast cell surf...