<scp>GABA</scp>and Glutamate Receptor Ligands and their Therapeutic Potential in<scp>CNS</scp>Disorders

Madsen, Ulf; Bräuner‐Osborne, Hans; Greenwood, Jeremy R.; Johansen, Tommy N.; Krogsgaard‐Larsen, Povl; Liljefors, Tommy; Nielsen, Mogens; Frølund, Bente

doi:10.1002/9780470571224.pse019

Cited by 3 publications

(3 citation statements)

References 466 publications

(581 reference statements)

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“…Ser-186 in mGluR1, which corresponds to Ala-170 in hT1R1, is known to interact with the distal carboxylic acid moiety of l -Glu via a water molecule ( 13 , 30 ). Additionally, Gly-319 in mGluR1, which corresponds to Ala-302 in hT1R1, is also positioned near the carboxylate side chain of l -Glu ( 30 , 31 ). In mT1R1, mutating Ala to an acidic residue at this position is certainly expected to affect acidic amino acid binding due to the electrostatic repulsion between the negative charges of the carboxylic acid moieties.…”

Section: Discussionmentioning

confidence: 99%

Two Distinct Determinants of Ligand Specificity in T1R1/T1R3 (the Umami Taste Receptor)

Toda

Nakagita

Hayakawa

et al. 2013

Journal of Biological Chemistry

112

125

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Background: T1R1/T1R3 exhibits species-dependent differences in ligand specificity.Results: The ligand specificity is dependent on a combination of amino acid selectivity at the orthosteric site and receptor activity modulation at the non-orthosteric site.Conclusion: The molecular mechanism underlying the amino acid recognition of T1R1/T1R3 has been elucidated.Significance: This study provides new insights into the molecular mechanisms of the l-Glu-specific response in human T1R1/T1R3.

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Section: Discussionmentioning

confidence: 99%

Two Distinct Determinants of Ligand Specificity in T1R1/T1R3 (the Umami Taste Receptor)

Toda

Nakagita

Hayakawa

et al. 2013

Journal of Biological Chemistry

112

125

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“… a List of residues within 6 Å of l ‐Glu bound to mGlu 1 (Madsen et al. , 2005) based on previously published protein sequence alignments (Bräuner‐Osborne et al.…”

Section: Structure and Function Of Family C Gpcrsmentioning

confidence: 99%

Molecular basis for amino acid sensing by family C G‐protein‐coupled receptors

Wellendorph

Bräuner‐Osborne

2009

British J Pharmacology

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Family C of human G-protein-coupled receptors (GPCRs) is constituted by eight metabotropic glutamate receptors, two g-aminobutyric acid type B (GABAB1-2) subunits forming the heterodimeric GABAB receptor, the calcium-sensing receptor, three taste1 receptors (T1R1-3), a promiscuous L-a-amino acid receptor G-protein-coupled receptor family C, group 6, subtype A (GPRC6A) and seven orphan receptors. Aside from the orphan receptors, the family C GPCRs are dimeric receptors characterized by a large extracellular Venus flytrap domain which bind the endogenous agonists. Except from the GABAB1-2 and T1R2-3 receptor, all receptors are either activated or positively modulated by amino acids. In this review, we outline mutational, biophysical and structural studies which have elucidated the interaction of the amino acids with the Venus flytrap domains, molecular mechanisms of receptor selectivity and the initial steps in receptor activation.

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“…2. Ligand based drug designing method: Quantitative structure activity relationship (QSAR) method and pharmacophore modelling [7].…”

Section: Virtual Screeningmentioning

confidence: 99%

Review on Computational Bioinformatics and Molecular Modelling: Novel Tool for Drug Discovery

Jain¹

2018

IJTSRD

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Advancement in science and technology has brought a remarkable change in the field of drug discovery.Earlier it was very difficult to predict the target for receptor but nowadays, it is easy and robust task to dock the target protein with ligand and binding affinity is calculated. Docking helps in the virtual screening of drug along with its hit identification. There are two approaches through which docking can be carried out, shape complementary and stimulation approach. There are many procedures involved in carrying out docking and all require different software's and algorithms. Molecular docking serves as a good platform to screen a large number of ligands and is useful in Drug-DNA studies. This review mainly focuses on the general idea of molecular docking and discusses its major applications, different types of interaction involved and types of docking.

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GABAand Glutamate Receptor Ligands and their Therapeutic Potential inCNSDisorders

Cited by 3 publications

References 466 publications

Two Distinct Determinants of Ligand Specificity in T1R1/T1R3 (the Umami Taste Receptor)

Two Distinct Determinants of Ligand Specificity in T1R1/T1R3 (the Umami Taste Receptor)

Molecular basis for amino acid sensing by family C G‐protein‐coupled receptors

Review on Computational Bioinformatics and Molecular Modelling: Novel Tool for Drug Discovery

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