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Cytochrome P450 Enzyme Metabolites in Lead Discovery and Development.
Sylvie E Kandel1, Larry C Wienkers2, Jed N Lampe3
1XenoTech, LLC, 16825 W. 116 .St., Lenexa, KS 66219.
Annual Reports in Medicinal Chemistry
|March 24, 2015
Summary
Cytochrome P450 (CYP) enzymes are crucial for drug metabolism and natural product drug discovery. New technologies enable the use of CYPs for identifying novel drug leads and developing therapeutic compounds.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Drug Discovery
Background:
- Cytochrome P450 (CYP) enzymes are heme-containing monooxygenases primarily known for xenobiotic oxidation.
- CYPs play a significant role in natural product drug discovery due to their unique oxidative capabilities.
- They are essential for generating active metabolites with therapeutic potential.
Purpose of the Study:
- To review recent advancements in the analysis and production of CYP metabolites.
- To highlight drug leads identified from CYP metabolites.
- To explore the potential of CYPs as catalysts for future drug discovery.
Main Methods:
- Utilizing microscale analytical technologies for CYP metabolite analysis.
- Employing combinatorial biosynthesis for CYP metabolite production.
- Reviewing literature on drug leads derived from CYP metabolites.
Main Results:
- Identification of novel drug leads from CYP metabolites.
- Demonstration of CYPs as a viable platform for lead discovery and development.
- Showcasing the therapeutic potential of CYP-generated active metabolites.
Conclusions:
- CYP enzymes offer a promising avenue for natural product drug discovery.
- Advancements in analytical and biosynthetic tools enhance CYP applications in drug development.
- CYPs represent a powerful catalytic platform for generating future therapeutics.
Keywords:
14-hydroxyclarithromycin4-hydroxyatorvastatin6-hydroxybuspironecytochrome P450drug discoveryfexofenadinemetabolitesmetabolizer phenotypemicroscale microfluidicsnatural productsMore Related Videos
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