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From In Situ to In Vivo: An In Situ Click-Chemistry-Derived Carbonic Anhydrase II Imaging Agent for Positron Emission Tomography

Authors

  • Dr. Vani P. Mocharla,

    1. Siemens Molecular Imaging Biomarker Research, 6100 Bristol Parkway, Culver City, CA 90230 (USA)
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  • Dr. Joseph C. Walsh,

    1. Siemens Molecular Imaging Biomarker Research, 6100 Bristol Parkway, Culver City, CA 90230 (USA)
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  • Dr. Henry C. Padgett,

    1. Siemens Molecular Imaging Biomarker Research, 6100 Bristol Parkway, Culver City, CA 90230 (USA)
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  • Dr. Helen Su,

    1. Department of Molecular and Medical Pharmacology, University of California, Los Angeles, 650 Charles E. Young Dr. South, 23–120 Center for Health Sciences, Los Angeles, CA 90095 (USA)
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  • Dr. Barbara Fueger,

    1. Department of Molecular and Medical Pharmacology, University of California, Los Angeles, 650 Charles E. Young Dr. South, 23–120 Center for Health Sciences, Los Angeles, CA 90095 (USA)
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  • Prof. Dr. Wolfgang A. Weber,

    1. Department of Molecular and Medical Pharmacology, University of California, Los Angeles, 650 Charles E. Young Dr. South, 23–120 Center for Health Sciences, Los Angeles, CA 90095 (USA)
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  • Prof. Dr. Johannes Czernin,

    1. Department of Molecular and Medical Pharmacology, University of California, Los Angeles, 650 Charles E. Young Dr. South, 23–120 Center for Health Sciences, Los Angeles, CA 90095 (USA)
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  • Dr. Hartmuth C. Kolb

    Corresponding author
    1. Siemens Molecular Imaging Biomarker Research, 6100 Bristol Parkway, Culver City, CA 90230 (USA)
    • Siemens Molecular Imaging Biomarker Research, 6100 Bristol Parkway, Culver City, CA 90230 (USA)
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Abstract

original image

CA II makes a good PET: Discovering positron emission tomography (PET) probes with high target affinities is challenging. PET probe discovery using in situ click chemistry uses 19F-bearing fragments as 18F surrogates. This ensures that the lead hits and PET probes have equivalent chemical or biological characteristics, making PET probe discovery predictable and reliable.

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