Metabotropic Receptors for Glutamate and GABA

Stewart, Gregory D.; Kniazeff, Julie; Prézeau, Laurent; Rondard, Philippe; Pin, Jean‐Philippe; Goudet, Cyril

doi:10.5772/32481

Cited by 2 publications

(2 citation statements)

References 210 publications

(153 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Class A GPCRs comprise a relatively short N-terminal extracellular domain, a 7-transmembrane domain (TMD), and a short C-terminal intracellular domain (Figure ). The orthosteric binding sites in class A GPCR are located in the transmembrane helical bundle. − …”

Section: Natural Receptorsmentioning

confidence: 99%

“…Class B GPCRs comprise a long N-terminal extracellular domain and a 7-TMD (Figure ). The orthosteric ligand binding sites are in the long N-terminal extracellular domains of class B GPCRs. , The complex of N-terminal domain and ligand is inserted in to the 7-TMD after the binding event, and then the receptor is activated. , The peptide hormone receptors, such as glucagon, glucagon-like peptides, parathyroid hormone (PTH), corticotropin-releasing factor, and secretin receptors, are involved in many human diseases, including diabetes, osteoporosis, neurodegeneration, cardiovascular disease, and cancer. Therefore, these receptors are considered very important drug targets.…”

Section: Natural Receptorsmentioning

confidence: 99%

See 1 more Smart Citation

Conducting Nanomaterial Sensor Using Natural Receptors

et al. 2018

View full text Add to dashboard Cite

One of the recently emerging topics in biotechnology is natural receptors including G protein-coupled receptors, ligand-gated ion channels, enzyme-linked receptors, and intracellular receptors, due to their molecular specificity. These receptors, other than intracellular receptors, which are membrane proteins expressed on the cell membrane, can detect extracellular stimuli. Many researchers have utilized cells with natural receptors embedded in the cellular membrane for human sense-mimicking platforms based on electrochemical impedance spectroscopy, quartz crystal microbalances, surface plasmon resonance, and surface acoustic waves. In addition, integration of conducting nanomaterials and natural receptors allows highly sensitive and selective responses toward target molecules, enabling, for example, nanobioelectronic noses for odorants, nanobioelectronic tongues for tastants, and G-protein-coupled receptor sensors for hormones, dopamine, cadaverine, geosmin, trimethylamine, etc. Moreover, as a part of nanobioelectronic sensors, natural receptors can be produced in various forms, such as peptides, proteins, nanovesicles, and nanodiscs, and each sensor can provide an ultralow limit of detection. In this Review, we discuss biosensors with natural receptors and then especially focus on natural receptor-conjugated conducting nanomaterial sensors. To provide a fundamental understanding, the sections encompass (1) the fabrication of conducting nanomaterials, (2) the production of natural receptors, (3) the characteristics of natural receptors, (4) the technology for immobilizing both components, and (5) their sensing applications. Finally, perspective is given on a new development in the use of natural receptors in a wide range of industries, such as food, cosmetics, and healthcare. In addition, artificial olfactory codes will be characterized by signal processing in the near future, leading to human olfactory standardization.

show abstract

Section: Natural Receptorsmentioning

confidence: 99%

Section: Natural Receptorsmentioning

confidence: 99%

Conducting Nanomaterial Sensor Using Natural Receptors

et al. 2018

View full text Add to dashboard Cite

show abstract

Recent Advances in the Drug Discovery and Development of Dualsteric/ Bitopic Activators of G Protein-Coupled Receptors

Reinecke

Wang

Zhang

2019

CTMC

View full text Add to dashboard Cite

G protein-coupled receptors (GPCRs) represent the largest family of proteins targeted by drug design and discovery efforts. Of these efforts, the development of GPCR agonists is highly desirable, due to their therapeutic robust utility in treating diseases caused by deficient receptor signaling. One of the challenges in designing potent and selective GPCR agonists lies in the inability to achieve combined high binding affinity and subtype selectivity, due to the high homology between orthosteric sites among GPCR subtypes. To combat this difficulty, researchers have begun to explore the utility of targeting topographically distinct and less conserved binding sites, namely “allosteric” sites. Pursuing these sites offers the benefit of achieving high subtype selectivity, however, it also can result in a decreased binding affinity and potency as compared to orthosteric agonists. Therefore, bitopic ligands comprised of an orthosteric agonist and an allosteric modulator connected by a spacer and allowing binding with both the orthosteric and allosteric sites within one receptor, have been developed. It may combine the high subtype selectivity of an allosteric modulator with the high binding affinity of an orthosteric agonist and provides desired advantages over orthosteric agonists or allosteric modulators alone. Herein, we review the recent advances in the development of bitopic agonists/activators for various GPCR targets and their novel therapeutic potentials.

show abstract

Metabotropic Receptors for Glutamate and GABA

Cited by 2 publications

References 210 publications

Conducting Nanomaterial Sensor Using Natural Receptors

Conducting Nanomaterial Sensor Using Natural Receptors

Recent Advances in the Drug Discovery and Development of Dualsteric/ Bitopic Activators of G Protein-Coupled Receptors

Contact Info

Product

Resources

About