Conjugation of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetracetic acid (DOTA) and its derivatives to peptides:: Synthesis, applications and future prospects

Conjugation of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetracetic acid (DOTA) and its derivatives to peptides:: Synthesis, applications and future prospects
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DOI:
10.2174/157019307782411671
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发表时间:
2007-11-01
影响因子:
2.3
通讯作者:
De Leon-Rodriguez, L. M.
De Leon-Rodriguez, L. M.
中科院分区:
化学4区
文献类型:
--
作者:
Kovacs, Z.;De Leon-Rodriguez, L. M.

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通用螯合剂1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸(DOTA)及其双功能衍生物广泛用于生物医学应用中用各种金属离子标记肽。双功能 DOTA 衍生物及其与肽的缀合已成为构建目标特异性含金属试剂(包括靶向 MRI 造影剂以及诊断和治疗放射性药物)的既定策略。本综述涵盖了 DOTA-肽缀合物的合成、它们在生物医学中的潜在用途以及与其应用相关的问题。
The universal chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetracetic acid (DOTA) and its bifunctional derivatives are widely used to label peptides with various metal ions for biomedical applications. Bifunctional DOTA derivatives and their conjugation to peptides has become an established strategy for constructing target-specific metal containing agents including targeted MRI contrast agents and diagnostic and therapeutic radiopharmaceuticals. This review covers the synthesis of DOTA-peptide conjugates, their potential use in biomedicine and the problems related to their applications.