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- W2597671539 abstract "A collaborative project has been undertaken to explore marine cyanobacteria for lead compounds to treat comorbid pain and depression/anxiety. Serotonin (5-HT) signaling modulation has long been linked to antidepressant activity in humans and more recently, to chronic pain in a receptor-specific fashion. For these reasons extracts from marine cyanobacteria from Panama and Curacao were screened for their ability to bind to serotonergic G-protein coupled receptors (GCPRs) with known links to pain and depression/anxiety, as well as to monoamine transporter (MAT) that facilitates reuptake of serotonin. The secondary metabolites produced by marine cyanobacteria, particularly the peptide and peptide-containing compounds, share structural similarities and motifs with endogenous ligands of GPCRs and therefore could mimic binding to GPCRs. This made cyanobacterial extracts a logical target to screen for lead compounds to treat the disease states. Approximately 225 crude fractions and fractions were screened, using a radioligand competition-binding assay, for their ability to bind to 5-HT GPCRs and MAT. An additional 79 fractions are ready for screening. Eighty-nine of the fractions screened showed greater than 50% inhibition of binding of radioligand to 5-HT GPCRs (50) and MAT (39) – a 40% hit rate. Furthermore, in the high affinity binding assay eight fractions displayed selectivity to the 5-HT2c receptor and three fractions displayed selectivity to the 5-HT7 receptor, an overall 5% hit rate. These results are demonstrative of the usefulness of targeting marine cyanobacteria for GPCR ligands and will be discussed along with the ongoing research on the characterization of selective ligands of 5-HT2c and 5-HT7 GCPRs." @default.
- W2597671539 created "2017-04-07" @default.
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- W2597671539 date "2017-04-01" @default.
- W2597671539 modified "2023-09-27" @default.
- W2597671539 title "(163) Screening extracts of marine cyanobacteria for lead compounds to treat pain" @default.
- W2597671539 doi "https://doi.org/10.1016/j.jpain.2017.02.069" @default.
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