Thiol-Reactive Bifunctional Chelators for the Creation of Site-Selectively Modified Radioimmunoconjugates with Improved Stability.

ABSTRACT: Maleimide-bearing bifunctional chelators have been used extensively for the site-selective bioconjugation and radiolabeling of peptides and proteins. However, bioconjugates obtained using these constructs inevitably suffer from limited stability in vivo, a trait that translates into suboptimal activity concentrations in target tissues and higher uptake levels in healthy, nontarget tissues. To circumvent this issue, phenyloxadiazolyl methylsulfones have previously been reported as alternatives to maleimides for thiol-based ligations, but these constructs have scarcely been used in the field of radiochemistry. In this report, we describe the synthesis of two thiol-reactive bifunctional chelators for ⁸⁹Zr and ¹⁷⁷Lu based on a new, easy-to-make phenyloxadiazolyl methylsul

SUBMITTER: Adumeau P 

PROVIDER: S-EPMC6523022 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature