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Bi- or multifunctional opioid peptide drugs
1Laboratory of Chemical Biology and Peptide Research, Clinical Research Institute of Montreal, 110 Pine Avenue West, Montreal, Quebec, Canada H2W 1R7. schillp@ircm.qc.ca
Life Sciences
|March 17, 2009
Summary
This review explores bifunctional drugs, distinguishing between single-target and dual-target interactions. It highlights strategies for developing novel opioid analgesics with improved properties and reduced side effects.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Drug Design
Background:
- Review of strategies for designing bi- or multifunctional drugs.
- Distinction between monovalent and bivalent drug interactions.
- Critique of current 'bivalent' ligand classifications.
Purpose of the Study:
- Illustrate development of multifunctional drugs using opioid analgesics.
- Review drug-like properties of Dmt(1)[DALDA] for triple action analgesia.
- Present rationales for mixed agonist/antagonist opioid peptides.
Main Methods:
- Analysis of bifunctional drug design strategies.
- Review of specific examples in opioid analgesic development.
- Discussion of drug-like properties and therapeutic potential.
Main Results:
- Critique of bivalent ligand binding assumptions.
- Highlighting Dmt(1)[DALDA] as a triple-action analgesic.
- Review of progress in mixed opioid agonist/antagonist development.
- Exploration of bifunctional peptides with combined opioid and other receptor antagonism.
Conclusions:
- Bifunctional drug design offers novel therapeutic avenues, particularly in pain management.
- Development of mixed opioid agonist/antagonist profiles can reduce side effects.
- Strategies for improving drug-like properties of peptide analgesics are crucial for clinical translation.
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