Probing the shape of a hydrophobic pocket in the active site of δ-opioid antagonists

Journal of Peptide Science

Volumn 7, Issue 7, 2001, Pages 374-385

  Santagada, Vincenzo ^a   Caliendo, Giuseppe ^b   Severino, Beatrice ^c   Perissutti, Elisa ^a   Ceccarelli, Francesca ^a   Giusti, Laura ^a   Mazzoni, Maria Rosaria ^a   Salvadori, Severo ^b   Temussi, Piero Andrea ^a  

^a UNIVERSITY OF NAPLES FEDERICO II   (Italy)

^b UNIVERSITY OF PISA   (Italy)

^c UNIVERSITY OF FERRARA   (Italy)

Author keywords

Antagonists; Dipeptides; Opioids

Indexed keywords

2',6' DIMETHYL TYROSINE; CARBOXYLIC ACID DERIVATIVE; DELTA OPIATE RECEPTOR ANTAGONIST; DIPEPTIDE; OPIATE PEPTIDE; OPIATE RECEPTOR; TETRAHYDROISOQUINOLINE 3 CARBOXYLIC ACID; TYROSINE; TYROSINE DERIVATIVE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ARTICLE; CONTROLLED STUDY; HYDROPHOBICITY; PEPTIDE ANALYSIS; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN STRUCTURE;

AMINO ACID SUBSTITUTION; ANIMALS; BINDING SITES; BINDING, COMPETITIVE; BRAIN; DIPEPTIDES; ISOQUINOLINES; MOLECULAR CONFORMATION; NALTREXONE; NARCOTIC ANTAGONISTS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, OPIOID, DELTA; TETRAHYDROISOQUINOLINES; THERMODYNAMICS; TYROSINE;

EID: 0034914627     PISSN: 10752617     EISSN: None     Source Type: Journal    
DOI: 10.1002/psc.331     Document Type: Article

References (25)

1. Differential stereochemical requirements of μ vs. δ opioid receptors for ligand binding and signal transduction. Development of a class of potent and highly δ-selective peptide antagonists
2. Selective opioid dipeptides
3. Conversion of enkephalin and dermorphin into δ-selective opioid antagonists by single residue substitution
4. Pharmacophore elements of the tipp class of δ-opioid receptor antagonists
5. Ultraselective δ-opioid-mimetic dipeptide antagonists
6. Conformational analysis of potent and very selective δ-opioid dipeptide antagonists
7. The role of concepts in structure-activity relationship studies of opioid ligands
8. 1 replacements in the cyclic δ-receptor selective tetrapeptide Tyr-C[D-Cys-Phe-D-Pen]OH (JOM-13)
9. 3 replacements in the cyclic δ-receptor selective tetrapeptide Tyr-C[D-Cys-Phe-D-Pen]OH (JOM-13)
10. Development of a model for the δ-opioid receptor pharmacophore: 3. Comparison of the cyclic tetrapeptide Tyr-C[D-Cys-Phe-D-Pen]OH with other conformationally constrained δ-receptor selective ligands
11. Steric hindrance in α-chymoptrypsin-catalyzed reactions
12. Carbodumide-mediated amide formation in a two-phase system. A high-yield and low-racemization procedure for peptide synthesis
13. 3H]-naltrindole binding to delta opioid receptors in mouse brain and mouse vas deferens: Evidence for delta opioid receptor heterogeneity
14. Protein measurement with Folin phenol reagent
15. 50) of an enzymatic reaction
16. AMBER, a computer program for applying molecular mechanics, normal mode analysis, molecular dynamics and free energy calculations to elucidate the structures and energies of molecules
17. An all-atom force-field for simulations of proteins and nucleic acids
18. Design of μ-selective opioid dipeptide antagonists
19. Application of the message-address concept in the design of highly potent and selective non-peptide δ-opioid receptor antagonists
20. Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone
21. The design of antagonists of regulatory peptides and comments on their specificity
22. Structure-function relations in gastrin-like peptides
23. Oxytocin analogs in the analysis of some phases of hormone action. Recent Prog
24. Allosteric proteins and cellular control systems
25. Models of antagonism. Design and solution structure of a partially rigid opioid antagonist lacking the basic center