Structural modifications of amino acid sequences of radiolabeled peptides for targeted tumor imaging.,Bioorganic Chemistry

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Structural modifications of amino acid sequences of radiolabeled peptides for targeted tumor imaging.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-04-01 , DOI: 10.1016/j.bioorg.2020.103802
Fariba Maleki ₁ , Arezou Masteri Farahani ₁ , Farzaneh Rezazedeh ₁ , Nourollah Sadeghzadeh ₂

Affiliation

Molecular imaging techniques are increasingly being used in localization, staging and therapy control of cancer. Due to their unique target specificity for the endogenous receptors, radiopeptides have been used widely for the development of radiopharmaceuticals for targeted tumor imaging in nuclear oncology. It is necessary to modify radiolabeled peptides in order to achieve more effective agents. Structural modifications of amino acid chains have significant effect on the metabolic stability, biological activity and efficiency of peptide conjugates that are currently applied as imaging tracers. There are several ways to modify the peptide chain but the most common strategies include amino acid substitutions, cyclization and multimerization. In this review, we have focused on studies involving these kind of modifications on amino acid sequences of radiolabeled peptides and we have provided an overview of the effects of these chemical modifications on the in vitro and in vivo properties of these radioconjugates and their potential as SPECT (Single photon emission computed tomography) and PET (positron emission tomography) imaging agents.

中文翻译：

用于目标肿瘤成像的放射性标记肽氨基酸序列的结构修饰。

分子成像技术越来越多地用于癌症的定位，分期和治疗控制中。由于其对内源性受体的独特靶标特异性，放射性肽已广泛用于开发用于核肿瘤学中靶向肿瘤成像的放射性药物。为了获得更有效的试剂，必须修饰放射性标记的肽。氨基酸链的结构修饰对目前用作成像示踪剂的肽缀合物的代谢稳定性，生物学活性和效率具有重要影响。有几种方法可以修饰肽链，但最常见的策略包括氨基酸取代，环化和多聚化。在这篇评论中

更新日期：2020-04-21

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