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- W2160203886 endingPage "144" @default.
- W2160203886 startingPage "117" @default.
- W2160203886 abstract "G protein–coupled receptors (GPCRs) are an evolutionarily conserved family of signaling molecules comprising approximately 2% of the human genome; this receptor family remains a central focus in basic pharmacology studies and drug discovery efforts. Detailed studies of drug action at GPCRs over the past decade have revealed existing and novel ligands that exhibit polypharmacology—that is, drugs with activity at more than one receptor target for which they were designed. These “off-target” drug actions can be a liability that causes adverse side effects; however, in several cases, drugs with less selectivity demonstrate better clinical efficacy. Here we review physical screening and cheminformatic approaches that define drug activity at the GPCR receptorome. In many cases, such profiling has revealed unexpected targets that explain therapeutic actions as well as off-targets underlying drug side effects. Such drug-receptor profiling has also provided new insights into mechanisms of action of existing drugs and has suggested directions for future drug development." @default.
- W2160203886 created "2016-06-24" @default.
- W2160203886 creator A5007856961 @default.
- W2160203886 creator A5070959736 @default.
- W2160203886 date "2011-02-10" @default.
- W2160203886 modified "2023-10-08" @default.
- W2160203886 title "Strategies to Discover Unexpected Targets for Drugs Active at G Protein–Coupled Receptors" @default.
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