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The most common mutation, F508del, leads to almost total absence of CFTR at the plasma membrane, a defect potentially corrected via drug\u2010based therapies. Herein, we report the first proof\u2010of\u2010principle study of a noninvasive imaging probe able to detect CFTR at the plasma membrane. We radiolabeled the CFTR inhibitor, CFTR<jats:sub>inh<\/jats:sub>\u2010172a, with technetium\u201099m via a pyrazolyl\u2010diamine chelating unit, yielding a novel <jats:sup>99m<\/jats:sup>Tc(CO)<jats:sub>3<\/jats:sub> complex. A non\u2010radioactive surrogate showed that the structural modifications introduced in the inhibitor did not affect its activity. The radioactive complex was able to detect plasma membrane CFTR, shown by its significantly higher uptake in wild\u2010type versus mutated cells. Furthermore, assessment of F508del CFTR pharmacological correction in human cells using the radioactive complex revealed differences in corrector versus control uptake, recapitulating the biochemical correction observed for the protein.<\/jats:p>","DOI":"10.1002\/cmdc.201800187","type":"journal-article","created":{"date-parts":[[2018,6,4]],"date-time":"2018-06-04T15:00:21Z","timestamp":1528124421000},"page":"1469-1478","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Targeting of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein with a Technetium\u201099m Imaging Probe"],"prefix":"10.1002","volume":"13","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-5644-3199","authenticated-orcid":false,"given":"Vera F. 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