Biologically active metabolites in drug discovery
Shaoyi Sun1, Steven S Wesolowski1
1Xenon Pharmaceuticals Inc, 200-3650 Gilmore Way, Burnaby, BC V5G 4W8, Canada.
Bioorganic & Medicinal Chemistry Letters
|July 10, 2021
Summary
Biologically active metabolites are crucial for developing new drugs. This digest explores selected metabolites used as novel drug candidates or lead structures in drug design.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Pharmacology
Background:
- Biologically active metabolites represent a rich source for novel therapeutic agents.
- The identification and utilization of these compounds are key to advancing drug discovery.
- Metabolites offer unique chemical scaffolds with inherent biological activity.
Purpose of the Study:
- To highlight selected biologically active metabolites.
- To showcase their application as new chemical entities (NCEs) in drug development.
- To illustrate their role as lead structures for optimizing drug design.
Main Methods:
- Literature review and selection of relevant biologically active metabolites.
- Analysis of case studies where metabolites were developed into drug candidates.
- Examination of examples where metabolites served as starting points for lead optimization.
Main Results:
- Several biologically active metabolites have been successfully developed into drug candidates.
- Specific metabolites have demonstrated significant potential as lead structures in drug design.
- The diverse chemical structures of metabolites provide a broad scope for therapeutic innovation.
Conclusions:
- Biologically active metabolites are a vital and underutilized resource in drug discovery.
- Their unique properties facilitate the development of novel therapeutics and drug leads.
- Further exploration of metabolite-based drug design holds promise for future pharmaceutical advancements.
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