Abstract:
:A number of Bruton's tyrosine kinase (BTK) inhibitors are currently in development, yet it has been difficult to visualize BTK expression and pharmacological inhibition in vivo in real time. We synthesized a fluorescent, irreversible BTK binder based on the drug Ibrutinib and characterized its behavior in cells and in vivo. We show a 200 nM affinity of the imaging agent, high selectivity, and irreversible binding to its target following initial washout, resulting in surprisingly high target-to-background ratios. In vivo, the imaging agent rapidly distributed to BTK expressing tumor cells, but also to BTK-positive tumor-associated host cells.
journal_name
Sci Repjournal_title
Scientific reportsauthors
Turetsky A,Kim E,Kohler RH,Miller MA,Weissleder Rdoi
10.1038/srep04782subject
Has Abstractpub_date
2014-04-24 00:00:00pages
4782issn
2045-2322pii
srep04782journal_volume
4pub_type
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