A benzenesulfonamide derivative as a novel PET radioligand for CXCR4.
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ABSTRACT:
SUBMITTER: Oum YH
PROVIDER: S-EPMC6942325 | biostudies-literature | 2020 Jan
REPOSITORIES: biostudies-literature
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A benzenesulfonamide derivative as a novel PET radioligand for CXCR4.
Oum Yoon Hyeun YH Shetty Dinesh D Yoon Younghyoun Y Liang Zhongxing Z Voll Ronald J RJ Goodman Mark M MM Shim Hyunsuk H
Bioorganic & medicinal chemistry 20191130 2
CXCR4 is involved in various diseases such as inflammation, tumor growth, and cancer metastasis through the interaction with its natural endogenous ligand, chemokine CXCL12. In an effort to develop imaging probes for CXCR4, we developed a novel small molecule CXCR4-targeted PET agent (compound 5) by combining our established benzenesulfonamide scaffold with a labeling component by virtue of click chemistry. 5 shows nanomolar affinity (IC<sub>50</sub> = 6.9 nM) against a known CXCR4 antagonist (T ...[more]
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