1154411-50-3Relevant academic research and scientific papers
Cerulenin analogues as inhibitors of efflux pumps in drug-resistant candida albicans
Diwischek, Florian,Morschhae, Joachim,Holzgrabe, Ulrike
, p. 150 - 164 (2009)
Overexpression of the ABC transporters Cdrl and Cdr2 or the major facilitator Mdrl causes multidrug resistance in the human fungal pathogen Candida albicans. The fatty acid synthesis inhibitor cerulenin and the structurally unrelated Golgi transport inhibitor brefeldin A are substrates for both types of efflux pumps in Candida albicans. In an effort to overcome efflux pump-mediated drug resistance in Candida albicans, cerulenin analogues were generated using a variety of synthesis pathways. The so obtained cerulenin derivatives were tested on multidrug-resistant Candida albicans isolates which constitutively overexpress either Mdr1 or Cdr1 and Cdr2. Some of these compounds were found to decrease Mdr1-mediated resistance to brefeldin A up to eight-fold compared to the control. 2009 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
