Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin
Küçük Resim Yok
Tarih
2020
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
American Chemical Society
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
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 ?-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. © 2020 American Chemical Society.
Açıklama
Anahtar Kelimeler
bioconjugates, Biphalin, fluorescent probes, GPCRs, opioids
Kaynak
ACS Medicinal Chemistry Letters
WoS Q Değeri
Q2
Scopus Q Değeri
Q1
