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  • Screening a natural product-based combinatorial library using FTICR mass spectrometry

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    Author(s)
    Poulsen, SA
    Davis, RA
    Keys, TG
    Griffith University Author(s)
    Poulsen, Sally-Ann
    Davis, Rohan A.
    Year published
    2006
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    Abstract
    This manuscript reports the use of Fourier transform ion cyclotron resonance mass spectrometry to screen a combinatorially generated natural product-based library for binding affinity to bovine carbonic anhydrase II (bCAII). The fungal natural product 3-chloro-4-hydroxyphenylacetamide was the library template, with 11 secondary amide analogues of this template constituting the combinatorial library. 2-(3-Chloro-4-hydroxyphenyl)-N-(4-sulfamoylphenethyl)acetamide (compound 11) of this library was identified as a tight binding inhibitor of bCAII, by detection of a noncovalent complex corresponding to [bCAII + 11] in the mass ...
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    This manuscript reports the use of Fourier transform ion cyclotron resonance mass spectrometry to screen a combinatorially generated natural product-based library for binding affinity to bovine carbonic anhydrase II (bCAII). The fungal natural product 3-chloro-4-hydroxyphenylacetamide was the library template, with 11 secondary amide analogues of this template constituting the combinatorial library. 2-(3-Chloro-4-hydroxyphenyl)-N-(4-sulfamoylphenethyl)acetamide (compound 11) of this library was identified as a tight binding inhibitor of bCAII, by detection of a noncovalent complex corresponding to [bCAII + 11] in the mass spectrum. A competitive bCAII enzyme binding assay validated the mass spectrometry screening result. The equilibrium dissociation constant (Ki) for 11 was measured as 77.4 nM. Preliminary structure-activity investigations of the bioactive natural product analogue are also reported.
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    Journal Title
    Bioorganic & Medicinal Chemistry
    Volume
    14
    Issue
    2
    Publisher URI
    http://www.sciencedirect.com/science/journal/09680896
    DOI
    https://doi.org/10.1016/j.bmc.2005.08.030
    Copyright Statement
    © 2006 Elsevier. Please refer to the journal's website for access to the definitive, published version. This is the author-manuscript version of this paper. Reproduced in accordance with the copyright policy of the publisher.
    Subject
    Medicinal and biomolecular chemistry
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Biochemistry and cell biology
    Publication URI
    http://hdl.handle.net/10072/13862
    Collection
    • Journal articles

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