Related Content
Search Google Scholar for:
|
|
Science 23 December 1994:
Vol. 266. no. 5193, pp. 2019 - 2022
DOI: 10.1126/science.7801131
|
|
Articles
Science, Vol 266, Issue 5193, 2019-2022
Copyright © 1994 by American Association for the Advancement of Science
An all D-amino acid opioid peptide with central analgesic activity from a combinatorial library
CT Dooley,
NN Chung,
BC Wilkes,
PW Schiller,
JM Bidlack,
GW Pasternak,
and
RA Houghten
Torrey Pines Institute for Molecular Studies, San Diego, CA 92121.
A synthetic combinatorial library containing 52,128,400 D-amino acid hexapeptides was used to identify a ligand for the mu opioid receptor. The peptide, Ac-rfwink-NH2, bears no resemblance to any known opioid peptide. Simulations using molecular dynamics, however, showed that three amino acid moieties have the same spatial orientation as the corresponding pharmacophoric groups of the opioid peptide PLO17. Ac-rfwink-NH2 was shown to be a potent agonist at the mu receptor and induced long-lasting analgesia in mice. Analgesia produced by intraperitoneally administered Ac-rfwink-NH2 was blocked by intracerebroventricular administration of naloxone, demonstrating that this peptide may cross the blood-brain barrier.
THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
- Substrate Specificity of Platypus Venom L-to-D-Peptide Isomerase.
- P. S. Bansal, A. M. Torres, B. Crossett, K. K. Y. Wong, J. M. S. Koh, D. P. Geraghty, J. I. Vandenberg, and P. W. Kuchel (2008)
J. Biol. Chem.
283, 8969-8975
| Abstract »
| Full Text »
| PDF »
- Utilization of Combined Chemical Modifications to Enhance the Blood-Brain Barrier Permeability and Pharmacological Activity of Endomorphin-1.
- H.-M. Liu, X.-F. Liu, J.-L. Yao, C.-L. Wang, Y. Yu, and R. Wang (2006)
J. Pharmacol. Exp. Ther.
319, 308-316
| Abstract »
| Full Text »
| PDF »
- Discovery of active proteins directly from combinatorial randomized protein libraries without display, purification or sequencing: identification of novel zinc finger proteins.
- M. D. Hughes, Z.-R. Zhang, A. J. Sutherland, A. F. Santos, and A. V. Hine (2005)
Nucleic Acids Res.
33, e32
| Abstract »
| Full Text »
| PDF »
- Ligands for kappa -Opioid and ORL1 Receptors Identified from a Conformationally Constrained Peptide Combinatorial Library.
- J. A. J. Becker, A. Wallace, A. Garzon, P. Ingallinella, E. Bianchi, R. Cortese, F. Simonin, B. L. Kieffer, and A. Pessi (1999)
J. Biol. Chem.
274, 27513-27522
| Abstract »
| Full Text »
| PDF »
- A Linear Hexapeptide Somatostatin Antagonist Blocks Somatostatin Activity In Vitro and Influences Growth Hormone Release in Rats.
- W. R. Baumbach, T. A. Carrick, M. H. Pausch, B. Bingham, D. Carmignac, I. C. A. F. Robinson, R. Houghten, C. M. Eppler, L. A. Price, and J. R. Zysk (1998)
Mol. Pharmacol.
54, 864-873
| Abstract »
| Full Text »
- Selective Ligands for the µ, delta , and kappa Opioid Receptors Identified from a Single Mixture Based Tetrapeptide Positional Scanning Combinatorial Library.
- C. T. Dooley, P. Ny, J. M. Bidlack, and R. A. Houghten (1998)
J. Biol. Chem.
273, 18848-18856
| Abstract »
| Full Text »
| PDF »
- Band 3 Peptides Block the Adherence of Sickle Cells to Endothelial Cells In Vitro.
- B. J.-M. Thevenin, I. Crandall, S. K. Ballas, I. W. Sherman, and S. B. Shohet (1997)
Blood
90, 4172-4179
| Abstract »
| Full Text »
| PDF »
- Binding and In Vitro Activities of Peptides with High Affinity for the Nociceptin/Orphanin FQ Receptor, ORL1.
- C. T. Dooley, C. G. Spaeth, I. P. Berzetei-Gurske, K. Craymer, I. D. Adapa, S. R. Brandt, R. A. Houghten, and L. Toll (1997)
J. Pharmacol. Exp. Ther.
283, 735-741
| Abstract »
| Full Text »
- Phage Display Selection on Whole Cells Yields a Peptide Specific for Melanocortin Receptor 1.
- M. Szardenings, S. Tornroth, F. Mutulis, R. Muceniece, K. Keinanen, A. Kuusinen, and J. E. S. Wikberg (1997)
J. Biol. Chem.
272, 27943-27948
| Abstract »
| Full Text »
| PDF »
- A Region of Vitamin K-dependent Protein S That Binds to C4b Binding Protein (C4BP) Identified Using Bacteriophage Peptide Display Libraries.
- S. Linse, Y. Hardig, D. A. Schultz, and B. Dahlback (1997)
J. Biol. Chem.
272, 14658-14665
| Abstract »
| Full Text »
| PDF »
- All-D-Enantiomers of beta -Amyloid Exhibit Similar Biological Properties to All-L-beta -Amyloids.
- D. H. Cribbs, C. J. Pike, S. L. Weinstein, P. Velazquez, and C. W. Cotman (1997)
J. Biol. Chem.
272, 7431-7436
| Abstract »
| Full Text »
| PDF »
- Absorption and Excretion of Undegradable Peptides: Role of Lipid Solubility and Net Charge.
- J. R. Pappenheimer, M. L. Karnovsky, and J. E. Maggio (1997)
J. Pharmacol. Exp. Ther.
280, 292-300
| Abstract »
| Full Text »
- Identification of Inhibitors of Melittin Using Nonsupport-bound Combinatorial Libraries.
- S. E. Blondelle, R. A. Houghten, and E. Pérez-Payá (1996)
J. Biol. Chem.
271, 4093-4099
| Abstract »
| Full Text »
| PDF »
- Combinatorial approaches: A new tool to search for highly structured beta -hairpin peptides.
- M. T. Pastor, M. Lopez de la Paz, E. Lacroix, L. Serrano, and E. Perez-Paya (2002)
PNAS
99, 614-619
| Abstract »
| Full Text »
| PDF »
|
|
