Literature DB >> 15780619

Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.

Yanfeng Gao1, Xin Liu, Jie Wei, Beibei Zhu, Qiang Chen, Rui Wang.   

Abstract

Endomorphin-2 (Tyr-Pro-Phe-Phe-NH(2)) is a putative endogenous mu-opioid receptor ligand. To develop potent analgesics with less side effects related to it, we used the methods of dimerization and C-terminal modification. Through dimerization we got the 'balanced agonists' with potent analgesic activity and we have developed the structure-activity relationship between the selectivity and the distance of the two tyrosine pharmacophores. Modification at the C-terminal increased the selectivity of endomorphin-2 to mu-opioid receptor with binding affinity conserved.

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Year:  2005        PMID： 15780619     DOI： 10.1016/j.bmcl.2005.02.021

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.

Authors:  Tingyou Li; Kimitaka Shiotani; Anna Miyazaki; Yuko Tsuda; Akihiro Ambo; Yusuke Sasaki; Yunden Jinsmaa; Ewa Marczak; Sharon D Bryant; Lawrence H Lazarus; Yoshio Okada
Journal:  J Med Chem       Date:  2007-05-12       Impact factor: 7.446

2.  A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.

Authors:  Severo Salvadori; Claudio Trapella; Stella Fiorini; Lucia Negri; Roberta Lattanzi; Sharon D Bryant; Yunden Jinsmaa; Lawrence H Lazarus; Gianfranco Balboni
Journal:  Bioorg Med Chem       Date:  2007-08-29       Impact factor: 3.641

3.  The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues.

Authors:  Adriano Mollica; Francesco Pinnen; Azzurra Stefanucci; Federica Feliciani; Cristina Campestre; Luisa Mannina; Anatoly P Sobolev; Gino Lucente; Peg Davis; Josephine Lai; Shou-Wu Ma; Frank Porreca; Victor J Hruby
Journal:  J Med Chem       Date:  2012-03-22       Impact factor: 7.446

4.  Lipo-endomorphin-1 derivatives with systemic activity against neuropathic pain without producing constipation.

Authors:  Pegah Varamini; Friederike M Mansfeld; Joanne T Blanchfield; Bruce D Wyse; Maree T Smith; Istvan Toth
Journal:  PLoS One       Date:  2012-08-17       Impact factor: 3.240
  4 in total

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