Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.,ACS Medicinal Chemistry Letters

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Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-01-08 , DOI: 10.1021/acsmedchemlett.9b00569
Azzurra Stefanucci ₁ , Marilisa Pia Dimmito ₁ , Gabriela Molnar ₂ , John M Streicher ₂ , Ettore Novellino ₃ , Gokhan Zengin ₄ , Adriano Mollica ₁

Affiliation

The development of bioconjugates is of pivotal importance in medicinal chemistry due to their potential applications as therapeutic agents to improve the targeting of specific diseases, decrease toxicity, or control drug release. In this work we achieved the synthesis and characterization of three novel opioid peptides fluorescently labeled, analogues of cyclic biphalin derivatives, namely 1D, 1C, and 2C. Among them, compound 1D, containing a dansyl-maleimide motif, exhibited an excellent binding affinity and functional potency for the δ-opioid receptor (DOR). 1D also demonstrated a strong fluorescence emission spectrum ranging from 300 to 700 nm. These features could be highly desirable for medical and biological applications needed for targeting the DOR, including in vivo imaging, and as a lead for the design of fluorescent probes.

中文翻译：

发展环状阿片类似物：Biphalin的荧光标记生物缀合物。

生物共轭物的开发在药物化学中具有至关重要的意义，因为它们作为治疗剂的潜在应用可改善特定疾病的靶向性，降低毒性或控制药物释放。在这项工作中，我们实现了荧光标记的三种新型阿片样肽的合成和表征，它们是环状双phalin衍生物的类似物，即1D，1C和2C。其中，包含丹磺酰基马来酰亚胺基序的化合物1D对δ阿片受体（DOR）表现出优异的结合亲和力和功能性。1D还显示了300至700 nm的强荧光发射光谱。对于靶向DOR所需的医学和生物学应用（包括体内成像），以及作为荧光探针设计的先导，这些功能可能非常理想。

更新日期：2020-01-08

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