Structure-activity relationships of the dimeric analogues of endomorphin-2 with different lengths of spacers

被引：0
|
作者：
Gao, Yan-Feng [1 ]
Zhai, Ming-Xia [1 ]
Liu, Wei-Xia [2 ]
Liu, Xin [2 ]
Yuan, Ye [2 ]
Qi, Yuan-Ming [1 ]
Wang, Rui [2 ]
机构：
[1] Zhengzhou Univ, Dept Bioengn, Zhengzhou 450001, Peoples R China
[2] Lanzhou Univ, Sch Life Sci, Inst Biochem & Mol Biol, Lanzhou 730000, Peoples R China
来源：
PROTEIN AND PEPTIDE LETTERS | 2008年 / 15卷 / 03期
关键词：
endomorphin-2; dimerization; analogue; structure-activity relationships; opioid receptor; balanced agonist;
D O I：
暂无
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
In the present study, seven novel dimeric analogues of endomorphin-2 with longer spacers were designed and synthesized. Through dimerization, their affinity for opioid receptor was mostly increased, especially the delta-opioid receptor preferred dimeric analogue, DEM12. The results were confirmed by the in vitro bioassay. The structure-activity relationships were also discussed.
引用
收藏
页码：275 / 279
页数：5
相关论文
共 50 条
  • [41] Studies on the quantitative structure-activity relationships of paclitaxel analogues
    Shi, BX
    Liang, SL
    Yuan, YJ
    Sun, M
    Miao, FM
    CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE, 2000, 21 (03): : 401 - 406
  • [42] Determining the structure-activity relationships of aminobiphenyl and benzidine analogues
    Chung, KT
    Claxton, LD
    TOXICOLOGY AND APPLIED PHARMACOLOGY, 2004, 197 (03) : 258 - 259
  • [43] Quantitative structure-activity relationships studies on oxytocin analogues
    Mei Hu
    Yang Li
    Shu Mao
    Liu Li
    Li Zhi-Liang
    CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE, 2007, 28 (05): : 964 - 967
  • [44] Structure-activity relationships of fluorinated lysophosphatidic acid analogues
    Xu, Y
    Aoki, J
    Shimizu, K
    Umezu-Goto, M
    Hama, K
    Takanezawa, Y
    Yu, SX
    Mills, GB
    Arai, H
    Qian, L
    Prestwich, GD
    JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (09) : 3319 - 3327
  • [45] Structure-activity relationships of NF449 analogues
    Braun, K
    Ullmann, H
    Kassack, M
    Nickel, P
    Lambrecht, G
    DRUG DEVELOPMENT RESEARCH, 2002, 56 (04) : 574 - 574
  • [46] Investigation of structure-activity relationships in a series of glibenclamide analogues
    Yuriev, E
    Kong, DCM
    Iskander, MN
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2004, 39 (10) : 835 - 847
  • [47] Quantitative structure-activity relationships studies on oxytocin analogues
    Mei, Hu
    Yang, Li
    Shu, Mao
    Liu, Li
    Li, Zhi-Liang
    Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities, 2007, 28 (05): : 964 - 967
  • [48] Synthesis of Mixed Opioid Affinity Cyclic Endomorphin-2 Analogues with Fluorinated Phenylalanines
    Piekielna, Justyna
    Perlikowska, Renata
    do-Rego, Jean Claude
    do-Rego, Jean-Luc
    Cerlesi, Maria Camilla
    Calo, Girolamo
    Kluczyk, Alicja
    Lapinski, Krzysztof
    Toemboely, Csaba
    Janecka, Anna
    ACS MEDICINAL CHEMISTRY LETTERS, 2015, 6 (05): : 579 - 583
  • [49] Novel endomorphin-2 analogs with μ-opioid receptor antagonist activity
    Kruszynski, R
    Fichna, J
    do-Rego, JC
    Chung, NN
    Schiller, PW
    Kosson, P
    Costentin, J
    Janecka, A
    JOURNAL OF PEPTIDE RESEARCH, 2005, 66 (03): : 125 - 131
  • [50] Synthesis and binding profiles of endomorphin-2 the analogues containing conformationally constrained moiety
    Tsuda, Y.
    Kawakami, T.
    Fujita, Y.
    Yamada, T.
    Isozaki, K.
    Shimohigashi, Y.
    Lazarus, L. H.
    JOURNAL OF PEPTIDE SCIENCE, 2006, 12 : 183 - 183
12345