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Our model system of human GPCRs and the "downstream genes" was based on the classical GPCR signal pathways, which has been summarized in [ 15].
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Extended application of this system to human GPCRs, which comprise one of the most important types of drug targets that are being pursued today, would be a valuable technology.
Briefly, agonist stimulation of human GPCRs triggers expression of an artificial signal activator that amplifies signaling.
This novel approach will enhance the usefulness of yeast-based screening of agonistic ligands for a variety of human GPCRs.
Here we introduce a new highly sensitive detection method that provides robust agonist detection of human GPCRs.
Open image in new window Figure 1 Overview of human GPCRs.
The yeast Saccharomyces cerevisiae is an attractive host for the ligand screening of human GPCRs.
The MDS representation reveals a non-uniform distribution of human GPCRs.
With about 300 non-olfactory and 400 olfactory members, class A or rhodopsin-like GPCRs represent up to 90% of human GPCRs.
To interpret patterns in relation with evolution, we projected GPCR sequences from distant species onto the active space of human GPCRs.
66 clear orthologs of human GPCRs could be identified in Ciona based on phylogenetic analysis.
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