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- W2055257794 abstract "In order to discover novel probes that may help in the investigation and control of infectious diseases through a new mechanism of action, we have evaluated a library of phenol-based natural products (NPs) for enzyme inhibition against four recently characterized pathogen β-family carbonic anhydrases (CAs). These include CAs from Mycobacterium tuberculosis, Candida albicans, and Cryptococcus neoformans as well as α-family human CA I and CA II for comparison. Many of the NPs selectively inhibited the mycobacterial and fungal β-CAs, with the two best performing compounds displaying submicromolar inhibition with a preference for fungal over human CA inhibition of more than 2 orders of magnitude. These compounds provide the first example of non-sulfonamide inhibitors that display β over α CA enzyme selectivity. Structural characterization of the library compounds in complex with human CA II revealed a novel binding mode whereby a methyl ester interacts via a water molecule with the active site zinc." @default.
- W2055257794 created "2016-06-24" @default.
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- W2055257794 date "2011-02-18" @default.
- W2055257794 modified "2023-10-14" @default.
- W2055257794 title "Natural Product-Based Phenols as Novel Probes for Mycobacterial and Fungal Carbonic Anhydrases" @default.
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- W2055257794 doi "https://doi.org/10.1021/jm1013242" @default.
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