English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Plus monthly

Global: Zendy Tools annual

Global: Zendy Tools monthly

Global: Zendy Free Plan

The purpose of this study was to examine the effects of the -Arg-Pro-(RP) and -Gly-Gly-Nle- (GGNle) moieties on the melanoma targeting and clearance properties of 99m Tc-peptides. We synthesized four new peptides {Ac-GGNle-CCEHdFRWC-NH 2 , Ac-GGNle-CCEHdFRWCRP-NH 2 , Ac-CCEHdFRWC-NleGG-NH 2 and Ac-CCEHdFRWCRP-NleGG-NH 2 } and determined their melanocortin-1 (MC1) receptor binding affinities in B16/F1 melanoma cells. Then we further examined the biodistribution properties of 99m Tc-Ac-GGNle-CCEHdFRWCRP-NH 2 and 99m Tc-Ac-CCEHdFRWCRP-NleGG-NH 2 in B16/F1 melanoma-bearing C57 mice. Overall, the Arg-Pro motif was critical for retaining low nanomolar MC1 receptor binding affinity. The deletion of the -RP- moiety dramatically reduced the receptor binding affinities of the peptides. The N-terminus was a better position than C-terminus for the -GGNle- moiety in retaining the lower renal and liver uptake. High melanoma uptake coupled with fast urinary clearance of 99m Tc-Ac-GGNle-CCEHdFRWCRP-NH 2 provided a new insight into the design of new α-melanocyte stimulating hormone (α-MSH) peptides.

Effects of the Arg-Pro and Gly-Gly-Nle Moieties on Melanocortin-1 Receptor Binding Affinities of α-MSH Peptides