Discovery of a Human Neuromedin U Receptor 1‑Selective Hexapeptide Agonist with Enhanced Serum Stability
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https://figshare.com/articles/dataset/Discovery_of_a_Human_Neuromedin_U_Receptor_1_Selective_Hexapeptide_Agonist_with_Enhanced_Serum_Stability/5071297
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资源简介：
Neuromedin
U (NMU) activates two NMU receptors (NMUR1 and NMUR2)
and is a useful antiobesity drug lead. We report discovery of a hexapeptide
agonist, 2-thienylacetyl-Trp1-Phe(4-F)2-Arg3-Pro4-Arg5-Asn6-NH2 (4). However, the NMUR1 selectivity and serum stability
of this agonist were unsatisfactory. Through a structure–activity
relationship study focused on residue 2 of agonist 4,
serum stability, and pharmacokinetic properties, we report here the
discovery of a novel NMUR1 selective hexapeptide agonist 7b that suppresses body weight gain in mice.
创建时间：
2017-06-02
