Pharmacophore elements of the TIPP class of delta opioid receptor antagonists
dc.contributor.author | Mosberg, Henry I. | en_US |
dc.contributor.author | Omnaas, John R. | en_US |
dc.contributor.author | Sobczyk-Kojiro, Katarzyna | en_US |
dc.contributor.author | Dua, Rajesh K. | en_US |
dc.contributor.author | Ho, Jeffrey C. | en_US |
dc.contributor.author | Ma, Wenli | en_US |
dc.contributor.author | Bush, Paula | en_US |
dc.contributor.author | Mousigian, Carol A. | en_US |
dc.contributor.author | Lomize, Andrei L. | en_US |
dc.date.accessioned | 2006-09-08T21:08:52Z | |
dc.date.available | 2006-09-08T21:08:52Z | |
dc.date.issued | 1994-10 | en_US |
dc.identifier.citation | Mosberg, Henry I.; Omnaas, John R.; Sobczyk-Kojiro, Katarzyna; Dua, Raj; Ho, Jeffrey C.; Ma, Wenli; Bush, Paula; Mousigian, Carol; Lomize, Andrei; (1994). "Pharmacophore elements of the TIPP class of delta opioid receptor antagonists." Letters in Peptide Science 1(2): 69-72. <http://hdl.handle.net/2027.42/43172> | en_US |
dc.identifier.issn | 0929-5666 | en_US |
dc.identifier.issn | 1573-3904 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/43172 | |
dc.description.abstract | A series of tri-and tetrapeptides sharing the amino-terminal dipeptide unit Tyr-Tic, found in the high-affinity delta opioid receptor antagonist Tyr-Tic-Phe-Phe (TIPP), was prepared and evaluated in receptor binding assays to explore the role(s) of the phenylalanine residues in positions 3 and 4. It was found that aromaticity of residues 3 and 4 is not required for high affinity, a lipophilic side chain in either location being sufficient, as evidenced by the high delta receptor binding affinities observed for the tetrapeptide Tyr-Tic-Ala-Leu and the tripeptide Tyr-Tic-Leu. These results support the suggestion of Temussi et al. [Biochem. Biophys. Res. Commun., 198 (1994) 933] that the aromatic side chain of the Tic residue corresponds to the aromatic side chain found in residues 3 or 4 in other delta-selective peptide series. | en_US |
dc.format.extent | 298068 bytes | |
dc.format.extent | 3115 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Kluwer Academic Publishers; ESCOM Science Publishers B.V. ; Springer Science+Business Media | en_US |
dc.subject.other | Life Sciences | en_US |
dc.subject.other | Polymer Sciences | en_US |
dc.subject.other | Biochemistry, General | en_US |
dc.subject.other | Animal Anatomy / Morphology / Histology | en_US |
dc.subject.other | Opioid Peptides | en_US |
dc.subject.other | Pharmacophore | en_US |
dc.subject.other | Tetrahydroisoquinoline Carboxylic Acid | en_US |
dc.subject.other | TIPP | en_US |
dc.title | Pharmacophore elements of the TIPP class of delta opioid receptor antagonists | en_US |
dc.type | Article | en_US |
dc.subject.hlbsecondlevel | Chemistry | en_US |
dc.subject.hlbsecondlevel | Chemical Engineering | en_US |
dc.subject.hlbsecondlevel | Public Health | en_US |
dc.subject.hlbsecondlevel | Biological Chemistry | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.subject.hlbtoplevel | Engineering | en_US |
dc.subject.hlbtoplevel | Science | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, University of Michigan, 48109-1065, Ann Arbor, MI, U.S.A. | en_US |
dc.contributor.affiliationumcampus | Ann Arbor | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/43172/1/10989_2004_Article_BF00126275.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1007/BF00126275 | en_US |
dc.identifier.source | Letters in Peptide Science | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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