Synthetic routes to the Neuropeptide Y Y1 receptor antagonist 1229U91 and related analogues for SAR studies and cell-based imaging

被引：7

作者：

Mountford, Simon J. ^{[1
]}

Liu, Mengjie ^{[1
]}

Zhang, Lei ^{[2
]}

Groenen, Marleen ^{[3
]}

Herzog, Herbert ^{[2
]}

Holliday, Nicholas D. ^{[3
]}

Thompson, Philip E. ^{[1
]}

机构：

[1] Monash Inst Pharmaceut Sci, Parkville, Vic 3052, Australia

[2] St Vincents Hosp, Garvan Inst Med Res, Neurosci Res Program, Darlinghurst, NSW 2010, Australia

[3] Univ Nottingham, Queens Med Ctr, Sch Life Sci, Cell Signalling Res Grp, Nottingham NG7 2UH, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2014年 / 12卷 / 20期

关键词：

HIGH-AFFINITY; PHARMACOLOGICAL CHARACTERIZATION; GR231118; 1229U91; BREAST-CANCER; POTENT; PEPTIDES; AGONIST; RADIOLIGAND; SELECTIVITY; SYSTEM;

D O I：

10.1039/c4ob00176a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The potent Y-1 receptor antagonist, 1229U91 has an unusual cyclic dimer structure that makes syntheses of analogue series quite challenging. We have examined three new routes to the synthesis of such peptides that has given access to novel structural variants including heterodimeric compounds, ring size variants and labelled conjugates. These compounds, including a fluorescently labelled analogue VIII show potent antagonism that can be utilised in studying Y1 receptor pharmacology.

引用

页码：3271 / 3281

页数：11

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