Small-Molecule Scaffolds for CYP51 Inhibitors Identified by High-Throughput Screening and Defined by X-Ray Crystallography

Sterol 14α-demethylase (CYP51), a major checkpoint in membrane sterol biosynthesis, is a key target for fungal antibiotic therapy. We sought small organic molecules for lead candidate CYP51 inhibitors. The changes in CYP51 spectral properties following ligand binding make CYP51 a convenient target f...

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Autors principals: Podust, Larissa M., von Kries, Jens P., Eddine, Ali Nasser, Kim, Youngchang, Yermalitskaya, Liudmila V., Kuehne, Ronald, Ouellet, Hugues, Warrier, Thulasi, Alteköster, Markus, Lee, Jong-Seok, Rademann, Jörg, Oschkinat, Hartmut, Kaufmann, Stefan H. E., Waterman, Michael R.
Format: Artigo
Idioma:Inglês
Publicat: American Society for Microbiology (ASM) 2007
Matèries:
Chemistry; Biosynthesis
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC2151439/
https://ncbi.nlm.nih.gov/pubmed/17846131
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1128/AAC.00311-07
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