Cytochrome P450: Structure, Function, and Application in Drug Discovery and Development

2010 ◽  
pp. 55-107
Author(s):  
Ramesh B. Bambal ◽  
Stephen E. Clarke
Keyword(s):  
Cytochrome P450 ◽  
Drug Discovery ◽  
Structure Function ◽  
Drug Discovery And Development

Cytochrome P450 enzymes: a review on drug metabolizing enzyme inhibition studies in drug discovery and development

Bioanalysis ◽  
2021 ◽  
Vol 13 (17) ◽  
pp. 1355-1378
Author(s):  
Siva Nageswara Rao Gajula ◽  
Megha Sajakumar Pillai ◽  
Gananadhamu Samanthula ◽  
Rajesh Sonti
Keyword(s):  
Cytochrome P450 ◽  
Drug Discovery ◽  
Enzyme Inhibition ◽  
In Vitro Study ◽  
Cytochrome P450 Enzymes ◽  
Drug Discovery And Development ◽  
Drug Candidates ◽  
Cyp Enzymes ◽  
Cyp Inhibition

Assessment of drug candidate's potential to inhibit cytochrome P450 (CYP) enzymes remains crucial in pharmaceutical drug discovery and development. Both direct and time-dependent inhibition of drug metabolizing CYP enzymes by the concomitant administered drug is the leading cause of drug–drug interactions (DDIs), resulting in the increased toxicity of the victim drug. In this context, pharmaceutical companies have grown increasingly diligent in limiting CYP inhibition liabilities of drug candidates in the early stages and examining risk assessments throughout the drug development process. This review discusses different strategies and decision-making processes for assessing the drug–drug interaction risks by enzyme inhibition and lays particular emphasis on in vitro study designs and interpretation of CYP inhibition data in a stage-appropriate context.

Effects of protein flexibility and active site water molecules on the prediction of sites of metabolism for cytochrome P450 2C19 substrates

2016 ◽  
Vol 12 (3) ◽  
pp. 868-878 ◽  
Author(s):  
Junhao Li ◽  
Jinya Cai ◽  
Haixia Su ◽  
Hanwen Du ◽  
Juan Zhang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Discovery ◽  
Active Site ◽  
Protein Flexibility ◽  
Cytochrome P450s ◽  
Water Molecules ◽  
Drug Discovery And Development ◽  
Cytochrome P450 2C19 ◽  
Site Water

Structure-based prediction of sites of metabolism (SOMs) mediated by cytochrome P450s (CYPs) is of great interest in drug discovery and development.

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