Synthesis and Biological Activities of Cyclic Lanthionine Enkephalin Analogues: δ-Opioid Receptor Selective Ligands

2002 ◽  
Vol 45 (17) ◽  
pp. 3746-3754 ◽  
Author(s):  
Yosup Rew ◽  
Shelle Malkmus ◽  
Camilla Svensson ◽  
Tony L. Yaksh ◽  
Nga N. Chung ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Biological Activities ◽  
Enkephalin Analogues ◽  
Selective Ligands ◽  
Δ Opioid Receptor

scholarly journals Synthesis and Biological Activities of Cyclic Lanthionine Enkephalin Analogues:  δ-Opioid Receptor Selective Ligands.

2002 ◽  
Vol 45 (24) ◽  
pp. 5414-5414 ◽  
Author(s):  
Yosup Rew ◽  
Shelle Malkmus ◽  
Camilla Svensson ◽  
Tony L. Yaksh ◽  
Nga N. Chung ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Biological Activities ◽  
Enkephalin Analogues ◽  
Selective Ligands ◽  
Δ Opioid Receptor

De Novo Design, Synthesis, and Biological Activities of High-Affinity and Selective Non-Peptide Agonists of the δ-Opioid Receptor‖

1998 ◽  
Vol 41 (24) ◽  
pp. 4767-4776 ◽  
Author(s):  
Subo Liao ◽  
Josue Alfaro-Lopez ◽  
Mark D. Shenderovich ◽  
Keiko Hosohata ◽  
Jun Lin ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
De Novo ◽  
Biological Activities ◽  
De Novo Design ◽  
Design Synthesis ◽  
High Affinity ◽  
Δ Opioid Receptor

scholarly journals Involvement of Trp-284, Val-296, and Val-297 of the Human δ-Opioid Receptor in Binding of δ-Selective Ligands

1996 ◽  
Vol 271 (31) ◽  
pp. 18789-18796 ◽  
Author(s):  
Manon Valiquette ◽  
Huy K. Vu ◽  
Shi Yi Yue ◽  
Claes Wahlestedt ◽  
Philippe Walker
Keyword(s):  
Opioid Receptor ◽  
Selective Ligands ◽  
Δ Opioid Receptor

scholarly journals Structural requirements for ligands of the δ-opioid receptor

2009 ◽  
Vol 74 (11) ◽  
pp. 1207-1217 ◽  
Author(s):  
Vuk Micovic ◽  
Milovan Ivanovic ◽  
Ljiljana Dosen-Micovic
Keyword(s):  
Opioid Receptor ◽  
Binding Pocket ◽  
Hydroxyl Group ◽  
Opioid Ligands ◽  
Chiral Compounds ◽  
Alkyl Groups ◽  
Selective Ligands ◽  
Ligand Interactions ◽  
Automated Docking ◽  
Δ Opioid Receptor

The ?-opioid receptor is sensitive to ligand geometry. In order to assist the synthesis of new ?-selective opioid ligands, the structure elements of ?-selective opioid ligands necessary for their effective binding were investigated. The automated docking procedure with a flexible ligand was used to simulate the binding of 17 ?-selective ligands to the ?-receptor. It was found that voluminous N-alkyl groups reduce the binding potency of naltrindole derivatives by preventing the ligands from adopting the preferred conformation in the receptor. This was confirmed by enantiospecific binding of chiral compounds where only one enantiomer adopts the naltrindole-like preferred conformation in the binding pocket. Voluminous groups replacing the hydroxyl group in the 3-hydroxybenzyl fragment of naltrindole analogs reduce the binding potency due to unfavorable steric interactions with the receptor. The two diastereoisomers of the potent ?-opioid ligand SNC80 confirmed the preferred binding conformation and the major receptor-ligand interactions.

ENKEPHALIN-INDUCED DESENSITIZATION OF ADENYLATE CYCLASE IN RECOMBINANT CV CELLS EXPRESSING A MOUSE δ-OPIOID RECEPTOR

Analgesia ◽  
1995 ◽  
Vol 1 (4) ◽  
pp. 603-606
Author(s):  
Vincent Nappey ◽  
Jean-luc Butour ◽  
Christiane Moisand ◽  
Claire Gaveriaux-Ruff ◽  
Brigitte Kieffer ◽  
...  
Keyword(s):  
Adenylate Cyclase ◽  
Opioid Receptor ◽  
Δ Opioid Receptor
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