Multi-parameter phenotypic profiling: using cellular effects to characterize small-molecule compounds.
Multi-parameter phenotypic profiling of small molecules provides important insights into their mechanisms of action, as well as a systems level understanding of biological pathways and their responses to small molecule treatments. It therefore deserves more attention at an early step in the drug discovery pipeline. Here, we summarize the technologies that are currently in use for phenotypic profiling--including mRNA-, protein- and imaging-based multi-parameter profiling--in the drug discovery context. We think that an earlier integration of phenotypic profiling technologies, combined with effective experimental and in silico target identification approaches, can improve success rates of lead selection and optimization in the drug discovery process.
Feng
Yan
Y
Developmental and Molecular Pathways, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, USA. yan.feng@novartis.com
Mitchison
Timothy J
TJ
Bender
Andreas
A
Young
Daniel W
DW
Tallarico
John A
JA
D000818:Animals; D055808:Drug Discovery; D005434:Flow Cytometry; D020869:Gene Expression Profiling; D006801:Humans; D008853:Microscopy; D010641:Phenotype; D010766:Phosphorylation; D040901:Proteomics; D013223:Statistics as Topic