Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587551 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
Three new DOTA-conjugated GnRH peptides with various hydrocarbon linkers were synthesized to evaluate the influences of the linkers on their receptor binding affinities. The hydrocarbon linker displayed a profound impact on the receptor binding affinities of DOTA-conjugated GnRH peptides. The Aun linker was better than Gaba, Ahx and Aoc linkers in retaining strong receptor binding affinity of the GnRH peptide. DOTA-Aun-(d-Lys6-GnRH) displayed 22.8Â nM GnRH receptor binding affinity. 111In-DOTA-Aun-(d-Lys6-GnRH) exhibited fast tumor uptake and urinary clearance in MDA-MB-231 human breast cancer-xenografted nude mice. The cellular and biological results provided an insight into the design of new GnRH peptides in the future.
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Authors
Haixun Guo, Helen Hathaway, Melanie E. Royce, Eric R. Prossnitz, Yubin Miao,