Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: Exploring the 'address' recognition locus

Journal of Medicinal Chemistry

Volumn 44, Issue 6, 2001, Pages 857-862

  Metzger, T G ^a   Paterlini, M G ^a   Ferguson, D M ^a   Portoghese, P S ^a  

^a UNIVERSITY OF MINNESOTA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5' GUANIDINONALTRINDOLE; DELTA OPIATE RECEPTOR; DELTA OPIATE RECEPTOR ANTAGONIST; GUANIDINE DERIVATIVE; KAPPA OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR ANTAGONIST; MU OPIATE RECEPTOR; NALTREXONE; NALTRINDOLE; NORBINALTORPHIMINE; OPIATE RECEPTOR; OXYMORPHONE; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ARTICLE; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; HUMAN; HUMAN CELL; LIGAND BINDING; RECEPTOR AFFINITY; SITE DIRECTED MUTAGENESIS;

AMINO ACID SEQUENCE; BASE SEQUENCE; BINDING, COMPETITIVE; CELL LINE; HUMANS; LIGANDS; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; NALTREXONE; OXYMORPHONE; RECEPTORS, OPIOID; RECEPTORS, OPIOID, DELTA; RECEPTORS, OPIOID, KAPPA; RECEPTORS, OPIOID, MU;

EID: 0035866624     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000381r     Document Type: Article

References (25)

1. International Union of Pharmacology. XII. Classification of opioid receptors
2. Cloning of a delta opioid receptor by functional expression
3. The delta-opioid receptor: Isolation of a cDNA by expression cloning and pharmacological characterization
4. Cloning and functional comparison of kappa and delta opioid receptors from mouse brain
5. mu opiate receptor: cDNA cloning and expression
6. Molecular cloning and functional expression of a μ-opioid receptor from rat brain
7. Cloning and pharamcological characterization of a rat κ opioid receptor
8. Cloning and pharmacological characerization of a rat μ opioid receptor
9. ACTH: A short introductory review
10. Selective naltrexone-derived opioid receptor antagonists
11. Synthesis and κ opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for κ antagonist activity
12. Analysis of selective binding epitopes for the κ-opioid receptor antagonist nor-binaltorphimine
13. A chimeric study of the molecular basis of affinity and selectivity of the κ and δ opioid receptors
14. δ-opioid receptor: The third extracellular loop determines naltrindole selectivity
15. Mutational evidence for a common κ antagonist binding pocket in the wild-type κ and mutant μ[K303E] opioid receptors
16. Involvement of Trp-284, Val-296, and Val-297 of the human δ-opioid receptor in binding of δ-selective binding
17. Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: Molecular recognition loci for the pharmacophore and address components of kappa antagonists
18. Application of the message-address concept to the docking of naltrexone and selective naltrexone-derived opioid antagonists into opioid receptor models
19. On the role of the extracellular loops of opioid receptors in conferring ligand selectivity
20. A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists
21. Pyrrolomorphinans as delta selective opioid receptor antagonists- the role of steric hindrance in conferring selectivity
22. An a-carbon template for the transmembrane helices in the Rhodopsin family of G-protein coupled receptors
23. High efficiency transformation of mammalian cells by plasmid DNA
24. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
25. Relationship between the inhibition constant (k1) and the concentration of inhibitor which causes 50% inhibition (I50) of an enzymatic reaction