Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.1.3.16 (calcineurin)
17,112 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Hypofunction of the serotonin (5-HT) 5-HT_2C receptor (5-HT_2CR) has been implicated in a variety of disorders including substance use disorders. As such, approaches to enhance 5-HT_2CR signaling display therapeutic potential. In the present study, we show that disruption of the 5-HT_2CR interaction with the protein phosphatase and tensin homolog (PTEN) via peptidomimetics enhances 5-HT_2CR-mediating signaling in vitro and potentiates selective 5-HT_2CR agonists in behavioral rodent models. Overall, the present study provides further evidence that 5-HT_2CR activity can be modulated through an allosteric protein-protein interaction. This work provides the groundwork for the continued exploration of protein-protein interactions that can allosterically modulate this critical receptor and other important G protein-coupled receptors (GPCRs) for new therapeutic development through mechanisms that may display clinical utility.
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PMID:In Vivo and In Vitro Analyses of Novel Peptidomimetic Disruptors for the Serotonin 5-HT_2C Receptor Interaction With Phosphatase and Tensin Homolog. 3150 11

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