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用于(68)Ga放射性药物的螯合剂设计和标记方法的最新进展。

Recent advances in chelator design and labelling methodology for (68) Ga radiopharmaceuticals.

作者信息

Burke Benjamin P, Clemente Gonçalo S, Archibald Stephen J

机构信息

Department of Chemistry, University of Hull, Hull, HU6 7RX, UK; Positron Emission Tomography Research Centre, University of Hull, Hull, HU6 7RX, UK.

出版信息

J Labelled Comp Radiopharm. 2014 Apr;57(4):239-43. doi: 10.1002/jlcr.3146. Epub 2014 Feb 4.

Abstract

Gallium-68 has the potential to become the technetium-99m of positron emission tomography with ideal decay characteristics and a long-lived parent isotope for generator production. The work in the area of (68) Ga is focused on two key areas: (1) synthesis of a library of bifunctional chelators, which can be quickly radiolabelled to form kinetically inert complexes under mild conditions compatible with biomolecules and (2) development of radiosynthetic methodologies for clinical use and to facilitate radiolabelling of a wide range of chelators under mild conditions. Recent advances in these areas, with particular focus on the past 3 years, are covered herein.

摘要

镓 - 68具有成为正电子发射断层扫描中锝 - 99m的潜力,它具有理想的衰变特性以及用于发生器生产的长寿命母体同位素。镓 - 68领域的工作集中在两个关键领域:(1)合成双功能螯合剂库,该库可在与生物分子兼容的温和条件下快速进行放射性标记以形成动力学惰性配合物;(2)开发用于临床应用的放射性合成方法,并促进在温和条件下对多种螯合剂进行放射性标记。本文涵盖了这些领域的最新进展,尤其重点关注过去3年的进展。

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