TY - JOUR
T1 - Recent advances and method development for drug target identification
AU - Chan, Janet N.Y.
AU - Nislow, Corey
AU - Emili, Andrew
N1 - Funding Information:
This study was supported by operating grants from the Ontario Research Fund and the Province of Ontario. We thank Aaron Wheeler for expert advice and suggestions and members of the Emili laboratory for critical reading of the manuscript.
PY - 2010/2
Y1 - 2010/2
N2 - Although it is commonly recognized that most drugs cause inhibition or activation of function by physically binding to one or more gene products, the direct interactions of bioactive small molecules with specific gene products, or targets, is often not well characterized. From a therapeutic perspective, it is nevertheless essential to know a drug's binding partner(s) to understand the mechanism of action and anticipate possible side effects to avoid costly clinical failures. This knowledge is increasingly important as the prevalence of polypharmacy expands to include drugs that engage multiple targets. This review provides a succinct overview of several recent approaches that employ genetics, proteomics, expression profiling or bioinformatics procedures for the systematic characterization of the targets of bioactive compounds. The continuous improvement and advancement of existing technologies is critically discussed and we offer a perspective on the future of innovative emerging new generation technologies.
AB - Although it is commonly recognized that most drugs cause inhibition or activation of function by physically binding to one or more gene products, the direct interactions of bioactive small molecules with specific gene products, or targets, is often not well characterized. From a therapeutic perspective, it is nevertheless essential to know a drug's binding partner(s) to understand the mechanism of action and anticipate possible side effects to avoid costly clinical failures. This knowledge is increasingly important as the prevalence of polypharmacy expands to include drugs that engage multiple targets. This review provides a succinct overview of several recent approaches that employ genetics, proteomics, expression profiling or bioinformatics procedures for the systematic characterization of the targets of bioactive compounds. The continuous improvement and advancement of existing technologies is critically discussed and we offer a perspective on the future of innovative emerging new generation technologies.
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U2 - 10.1016/j.tips.2009.11.002
DO - 10.1016/j.tips.2009.11.002
M3 - Review article
C2 - 20004028
AN - SCOPUS:75149125686
SN - 0165-6147
VL - 31
SP - 82
EP - 88
JO - Trends in pharmacological sciences
JF - Trends in pharmacological sciences
IS - 2
ER -