An overview on GPCRs and drug discovery: structure-based drug design and structural biology on GPCRs (Q34985885)

5 August 2017

2 references

22 August 2022

An overview on GPCRs and drug discovery: structure-based drug design and structural biology on GPCRs (English)

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G protein-coupled receptor

5 August 2017

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Kenneth Lundstrom

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PubMed ID

19513641

5 August 2017

language of work or name

English

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publication date

1 January 2009

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Methods in Molecular Biology

5 August 2017

2 references

5 August 2017

22 August 2022

552

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5 August 2017

51-66

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Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening

5 August 2017

1 reference

12 December 2020

Semliki Forest virus vectors for rapid and high-level expression of integral membrane proteins

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12 December 2020

A role for ghrelin in the central regulation of feeding

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12 December 2020

Beta-arrestin-dependent formation of beta2 adrenergic receptor-Src protein kinase complexes

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12 December 2020

Homogeneous Cell- and Bead-Based Assays for High Throughput Screening Using Fluorometric Microvolume Assay Technology

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12 December 2020

Effect of single point mutations of the human tachykinin NK1 receptor on antagonist affinity

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12 December 2020

Interaction of the anxiogenic agent, RS-30199, with 5-HT1A receptors: modulation of sexual activity in the male rat.

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12 December 2020

The receptors for mammalian sweet and umami taste

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12 December 2020

Lactococcus lactis as host for overproduction of functional membrane proteins

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12 December 2020

Is there a 'lock' for all agonist 'keys' in 7TM receptors?

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12 December 2020

Semliki Forest virus vectors for overexpression of 101 G protein-coupled receptors in mammalian host cells

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12 December 2020

Use of a disulfide cross-linking strategy to study muscarinic receptor structure and mechanisms of activation

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12 December 2020

Use of the hydrogen bond potential function in a comparative molecular field analysis (CoMFA) on a set of benzodiazepines.

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12 December 2020

Dimerization of G-protein-coupled receptors: implications for drug design and signaling

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12 December 2020

Strategies for designing GPCR-focused libraries and screening sets

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12 December 2020

Large-scale expression and purification of a G-protein-coupled receptor for structure determination -- an overview

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12 December 2020

G protein-coupled receptor dimerization: function and ligand pharmacology

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12 December 2020

G-protein-coupled receptor oligomerization and its potential for drug discovery

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12 December 2020

The human D1A dopamine receptor: heterologous expression in Saccharomyces cerevisiae and purification of the functional receptor

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12 December 2020

Human receptors for sweet and umami taste

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12 December 2020

Novel neurotransmitters as natural ligands of orphan G-protein-coupled receptors

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12 December 2020

Receptor screening and the search for new pharmaceuticals

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12 December 2020

Modeling the 3D structure of GPCRs from sequence

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12 December 2020

Signalling the fat controller

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12 December 2020

Benzimidazole derivatives. 3. 3D-QSAR/CoMFA model and computational simulation for the recognition of 5-HT(4) receptor antagonists

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12 December 2020

PREDICT modeling and in-silico screening for G-protein coupled receptors.

1 reference

12 December 2020

The conformation of neurotensin bound to its G protein-coupled receptor

1 reference

12 December 2020

Construction of a high affinity zinc switch in the kappa-opioid receptor.

1 reference

12 December 2020

Comparative molecular field analysis of selective A3 adenosine receptor agonists

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12 December 2020

QSAR modeling of GPCR ligands: methodologies and examples of applications

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12 December 2020

Protein-based virtual screening of chemical databases. II. Are homology models of G-Protein Coupled Receptors suitable targets?

1 reference

12 December 2020

Identification of nonpeptidic urotensin II receptor antagonists by virtual screening based on a pharmacophore model derived from structure-activity relationships and nuclear magnetic resonance studies on urotensin II.

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12 December 2020

Crystal structure of rhodopsin: A G protein-coupled receptor

1 reference

12 December 2020

Lead generation using pharmacophore mapping and three-dimensional database searching: application to muscarinic M(3) receptor antagonists

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12 December 2020

Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation

1 reference

12 December 2020

Recent advances in comparative molecular field analysis (CoMFA)

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12 December 2020

High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor

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12 December 2020

Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models

1 reference

12 December 2020

Interaction of substance P with the second and seventh transmembrane domains of the neurokinin-1 receptor

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12 December 2020

A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-releasing hormone receptor

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12 December 2020

GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function

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12 December 2020

Targeted disruption of the orphanin FQ/nociceptin gene increases stress susceptibility and impairs stress adaptation in mice

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12 December 2020

Model for the structure of bacteriorhodopsin based on high-resolution electron cryo-microscopy

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12 December 2020

Direct stimulation of Jak/STAT pathway by the angiotensin II AT1 receptor

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12 December 2020

The extracellular domain of the neurokinin-1 receptor is required for high-affinity binding of peptides

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12 December 2020

Design, synthesis, and evaluation of novel A2A adenosine receptor agonists

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12 December 2020

Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors

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12 December 2020

Comparative biochemical and pharmacological characterization of the mouse 5HT5A 5-hydroxytryptamine receptor and the human beta2-adrenergic receptor produced in the methylotrophic yeast Pichia pastoris

1 reference

12 December 2020

Probing the structure and function of the tachykinin neurokinin-2 receptor through biosynthetic incorporation of fluorescent amino acids at specific sites

1 reference

12 December 2020

Drug design strategies for targeting G-protein-coupled receptors

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12 December 2020

beta -Arrestin-mediated recruitment of the Src family kinase Yes mediates endothelin-1-stimulated glucose transport

1 reference

12 December 2020

GABA(B) receptors function as a heteromeric assembly of the subunits GABA(B)R1 and GABA(B)R2.

1 reference

12 December 2020

Synthesis and structure-activity relationships of a new model of arylpiperazines. 2. Three-dimensional quantitative structure-activity relationships of hydantoin-phenylpiperazine derivatives with affinity for 5-HT1A and alpha 1 receptors. A comparis

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12 December 2020

Connectivity and orientation of the seven helical bundle in the tachykinin NK-1 receptor probed by zinc site engineering

1 reference

12 December 2020

Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior

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12 December 2020

Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands

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12 December 2020

Use of constitutive G protein-coupled receptor activity for drug discovery.

1 reference

12 December 2020

Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.

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12 December 2020

Narcolepsy in orexin knockout mice: molecular genetics of sleep regulation

1 reference

12 December 2020

G protein-coupled receptor overexpression with the baculovirus-insect cell system: a tool for structural and functional studies.

1 reference

12 December 2020

Biophysical and genetic analysis of the ligand-binding site of the β-adrenoceptor

1 reference

12 December 2020

Modeling of G-protein-coupled receptors: application to dopamine, adrenaline, serotonin, acetylcholine, and mammalian opsin receptors

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12 December 2020

High level cell-free expression and specific labeling of integral membrane proteins

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12 December 2020

Structural genomics on membrane proteins: comparison of more than 100 GPCRs in 3 expression systems.

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12 December 2020

Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor

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12 December 2020

Molecular basis for the species selectivity of the substance P antagonist CP-96,345

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12 December 2020

Expression and purification of the Saccharomyces cerevisiae alpha-factor receptor (Ste2p), a 7-transmembrane-segment G protein-coupled receptor

1 reference

12 December 2020

Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists

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12 December 2020

Allosteric modulation of G protein-coupled receptors: perspectives and recent developments

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12 December 2020

X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease

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12 December 2020

Latest development in drug discovery on G protein-coupled receptors

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12 December 2020

Assessment of chemical libraries for their druggability

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12 December 2020

Different binding epitopes on the NK1 receptor for substance P and non-peptide antagonist.

1 reference

12 December 2020

Enhancing functional production of G protein-coupled receptors in Pichia pastoris to levels required for structural studies via a single expression screen

1 reference

12 December 2020

Structure-based analysis of GPCR function: evidence for a novel pentameric assembly between the dimeric leukotriene B4 receptor BLT1 and the G-protein

1 reference

12 December 2020

Endothelin antagonists: substituted mesitylcarboxamides with high potency and selectivity for ET(A) receptors

1 reference

12 December 2020

Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4. An unexpected effect of the chirality of Trp8 on NMR spectra in methanol

1 reference

12 December 2020

Allosteric binding sites on cell-surface receptors: novel targets for drug discovery

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12 December 2020

Structure and function in rhodopsin: high-level expression of rhodopsin with restricted and homogeneous N-glycosylation by a tetracycline-inducible N-acetylglucosaminyltransferase I-negative HEK293S stable mammalian cell line

1 reference

12 December 2020

Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand

1 reference

12 December 2020

Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines

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12 December 2020

In vitro folding of alpha-helical membrane proteins.

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12 December 2020

Structural features and light-dependent changes in the sequence 306-322 extending from helix VII to the palmitoylation sites in rhodopsin: a site-directed spin-labeling study

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12 December 2020

A continuous cell-free translation system capable of producing polypeptides in high yield

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12 December 2020

Purification and characterization of the human adenosine A(2a) receptor functionally expressed in Escherichia coli

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12 December 2020

Characterization of 16 human G protein-coupled receptors expressed in baculovirus-infected insect cells.

1 reference

12 December 2020

10.1007/978-1-60327-317-6_4

Identifiers

DOI

1 reference

5 August 2017

0 references

1 reference

PubMed ID

19513641