Proposal for the biologically active conformation of opiates and enkephalin.
A model for the opiate receptor has been defined by using a computer-based molecular display and x-ray crystallographic input data. The model can explain the stereochemical fashion in which the morphine, morphinan, and oripavine classes of compounds interact with the receptor. The minimal structural unit of the enkephalins demonstrated to be pharmacologically active. Tyr-Gly-Gly-Phe, was also fitted to this model by using a systematic search of conformational space.
D004723:Endorphins / Q000494:pharmacology; D004745:Enkephalins / Q000494:pharmacology; D008958:Models, Molecular; D008968:Molecular Conformation; D009292:Narcotic Antagonists / Q000494:pharmacology; D009294:Narcotics / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014961:X-Ray Diffraction
D004723:Endorphins; D004745:Enkephalins; D009292:Narcotic Antagonists; D009294:Narcotics
J Neurochem. 1977 Jan;28(1):13-20
188984
Proc Natl Acad Sci U S A. 1976 Sep;73(9):3165-7
1067610
Nature. 1976 Oct 14;263(5578):609-12
185523
J Pharm Pharmacol. 1976 Aug;28(8):660-1
11324
Proc Natl Acad Sci U S A. 1976 Nov;73(11):4215-9
186791
Science. 1976 Oct 15;194(4262):330-2
968485
J Pharmacol Exp Ther. 1975 Jul;194(1):205-19
239219
Annu Rev Pharmacol. 1971;11:241-70
4948499
Can Med Assoc J. 1973 Oct 6;109(7):615-9
4599599
Nat New Biol. 1973 Aug 8;244(136):186-7
4516455
J Med Chem. 1974 Aug;17(8):907-8
4845387
Proc Natl Acad Sci U S A. 1975 Feb;72(2):590-4
1054841
Neuropharmacology. 1975 Dec;14(12):941-9
768801
Annu Rev Pharmacol. 1975;15:29-47
238462
Proc Natl Acad Sci U S A. 1974 Sep;71(9):3474-7
4530316
Nature. 1976 Jul 22;262(5566):313-4
183126
Br J Pharmacol. 1972 Dec;46(4):764-6
4655272
Proc Natl Acad Sci U S A. 1976 Jun;73(6):2156-9
1064883
Nature. 1976 Aug 26;262(5571):782-3
958449
Biochem Biophys Res Commun. 1976 Jul 12;71(1):175-9
962911
Nature. 1976 Apr 29;260(5554):795-7
1264259
Nature. 1976 Jun 3;261(5559):423-5
934276
Nature. 1976 Mar 11;260(5547):165-6
1256559
Life Sci. 1975 Dec 1;17(11):1643-54
1207378
J Med Chem. 1975 Jul;18(7):656-62
1151985
J Am Chem Soc. 1967 Jun 7;89(12):2901-5
6043810
J Med Chem. 1965 Sep;8(5):609-16
5867942