Journal article
A Bone-Seeking trans-Cyclooctene for Pretargeting and Bioorthogonal Chemistry: A Proof of Concept Study Using 99mTc- and 177Lu-Labeled Tetrazines
Abstract
A high yield synthesis of a novel, small molecule, bisphosphonate-modified trans-cyclooctene (TCO-BP, 2) that binds to regions of active bone metabolism and captures functionalized tetrazines in vivo, via the bioorthogonal inverse electron demand Diels-Alder (IEDDA) cycloaddition, was developed. A 99mTc-labeled derivative of 2 demonstrated selective localization to shoulder and knee joints in a biodistribution study in normal mice. Compound 2 …
Authors
Yazdani A; Bilton H; Vito A; Genady AR; Rathmann SM; Ahmad Z; Janzen N; Czorny S; Zeglis BM; Francesconi LC
Journal
Journal of Medicinal Chemistry, Vol. 59, No. 20, pp. 9381–9389
Publisher
American Chemical Society (ACS)
Publication Date
October 27, 2016
DOI
10.1021/acs.jmedchem.6b00938
ISSN
0022-2623