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    The Rationale for Targeting the NAD/NADH Cofactor Binding Site of Parasitic S-Adenosyl-L-homocysteine Hydrolase for the Design of Anti-parasitic Drugs

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    Schowen_2009.pdf (928.7Kb)
    Issue Date
    2009-05
    Author
    Cai, Sumin
    Li, Qing-Shan
    Fang, Jianwen
    Borchardt, Ronald T.
    Kuczera, Krzysztof
    Middaugh, C. Russell
    Schowen, Richard L.
    Publisher
    Taylor & Francis
    Type
    Article
    Article Version
    Scholarly/refereed, author accepted manuscript
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    Abstract
    Trypanosomal S-adenoyl-L-homocysteine hydrolase (Tc-SAHH), considered as a target for treatment of Chagas disease, has the same catalytic mechanism as human SAHH (Hs-SAHH) and both enzymes have very similar X-ray structures. Efforts toward the design of selective inhibitors against Tc-SAHH targeting the substrate binding site have not to date shown any significant promise. Systematic kinetic and thermodynamic studies on association and dissociation of cofactor NAD/H for Tc-SAHH and Hs-SAHH provide a rationale for the design of anti-parasitic drugs directed toward cofactor-binding sites. Analogues of NAD and their reduced forms show significant selective inactivation of Tc-SAHH, confirming that this design approach is rational.
    Description
    This is an Accepted Manuscript of an article published by Taylor & Francis in Nucleosides, Nucleotides and Nucleic Acids in May 2009, available online: http://www.tandfonline.com/10.1080/15257770903051031.
    URI
    http://hdl.handle.net/1808/24659
    DOI
    https://doi.org/10.1080/15257770903051031
    Collections
    • Pharmaceutical Chemistry Scholarly Works [327]
    Citation
    Cai, S., Li, Q.-S., Fang, J., Borchardt, R. T., Kuczera, K., Middaugh, C. R., & Schowen, R. L. (2009). The Rationale for Targeting the NAD/NADH Cofactor Binding Site of Parasitic S-Adenosyl-L-homocysteine Hydrolase for the Design of Anti-parasitic Drugs. Nucleosides, Nucleotides & Nucleic Acids, 28(5), 485–503. http://doi.org/10.1080/15257770903051031

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    KU Libraries
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    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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