دانلود مقاله شیمی دارویی A Bone-Seeking Trans-Cyclooctene for Pretargeting

مقاله تخصصی شیمی دارویی با عنوان A Bone-Seeking Trans-Cyclooctene for Pretargeting که در ژورنال معتبر ACS در Sep 2016 چاپ شده است را به طور رایگان از سایت جم شیمی دانلود نمایید. این مقاله در 33 صفحه و فول تکست در اختیار شما کاربران گرامی قرار گرفته است.

چکیده مقاله تخصصی شیمی

: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 reacted rapidly
with a 177Lu-labeled tetrazine in vitro, and pretargeting experiments in mice, using 2 and the
177Lu-labeled tetrazine, yielded high activity concentrations in shoulder and knee joints, with
minimal uptake in other tissues. Pretargeting experiments with 2 and a novel 99mTc-labeled tetrazine also produced high activity concentrations in the knees and shoulders. Critically, both
radiolabeled tetrazines showed negligible uptake in the skeleton and joints, when administered in
the absence of 2. Compound 2 can be utilized to target functionalized tetrazines to bone and represents a convenient reagent to test novel tetrazines for use with in vivo bioorthogonal pretargeting strategies

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