ArticleInternational journal for parasitology. Drugs and drug resistance2016
Kinetic profiling an abundantly expressed planarian serotonergic GPCR identifies bromocriptine as a perdurant antagonist.
Article in International journal for parasitology. Drugs and drug resistance, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 18 citations in OpenAlex.
- Article
- Identification of novel modulators of a schistosome transient receptor potential channel targeted by praziquantel.PLoS neglected tropical diseases · 2021Article
- The Journey to Discovering a Flatworm Target of Praziquantel: A Long TRP.Trends in parasitology · 2020Review
- Regenerative Adaptation to Electrochemical Perturbation in Planaria: A Molecular Analysis of Physiological Plasticity.iScience · 2019Article
- Neural control of body-plan axis in regenerating planaria.PLoS computational biology · 2019Article
- Planarian regeneration as a model of anatomical homeostasis: Recent progress in biophysical and computational approaches.Seminars in cell & developmental biology · 2019Review
- Structure-activity profiling of alkaloid natural product pharmacophores against a Schistosoma serotonin receptor.International journal for parasitology. Drugs and drug resistance · 2018Article
- Coalescing beneficial host and deleterious antiparasitic actions as an antischistosomal strategy.eLife · 2018Article
- Unique pharmacological properties of serotoninergic G-protein coupled receptors from cestodes.PLoS neglected tropical diseases · 2018Article
- Utilizing the planarian voltage-gated ion channel transcriptome to resolve a role for a CaBiochimica et biophysica acta. Molecular cell research · 2017Article
- Anthelmintics: From discovery to resistance II (San Diego, 2016).International journal for parasitology. Drugs and drug resistance · 2016Article
- Pharmacological profiling an abundantly expressed schistosome serotonergic GPCR identifies nuciferine as a potent antagonist.International journal for parasitology. Drugs and drug resistance · 2016Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The diversity and uniqueness of flatworm G protein coupled receptors (GPCRs) provides impetus for identifying ligands useful as tools for studying flatworm biology, or as therapeutics for treating diseases caused by parasitic flatworm infections. To catalyse this discovery process, technologies optimized for mammalian GPCR high throughput screening need be transposed for screening flatworm GPCRs. Here, we demonstrate the utility of a genetically encoded cAMP biosensor for resolving the properties of an abundantly expressed planarian serotonergic GPCR (S7.1R). Application of this methodology resolved the real time kinetics of GPCR modulation by ligands and demonstrated a marked difference in the kinetic action of antagonists at S7.1R. Notably, bromocriptine caused a protracted inhibition of S7.1R activity in vitro and a protracted paralysis of planarian movement, replicating the effect of S7.1R in vivo RNAi. The lengthy inhibition of function caused by bromocriptine at this abundantly expressed GPCR provides a useful tool to ablate serotonergic signaling in vivo, and is a noteworthy feature for exploitation as an anthelmintic vulnerability.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.