(Q38172457)

30 August 2017

title

Structure-based and fragment-based GPCR drug discovery (English)

1 reference

G protein-coupled receptor

30 August 2017

main subject

0 references

1 reference

Stephen P Andrews

1

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30 August 2017

Giles A Brown

series ordinal

2

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30 August 2017

John A Christopher

series ordinal

3

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30 August 2017

publication date

18 December 2013

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30 August 2017

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30 August 2017

volume

9

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30 August 2017

issue

2

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30 August 2017

page(s)

256-275

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Structural diversity of G protein-coupled receptors and significance for drug discovery

30 August 2017

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists

21 January 2018

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New 2-heterocyclyl-imidazo[2,1-i]purin-5-one derivatives as potent and selective human A3 adenosine receptor antagonists

21 January 2018

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21 January 2018

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Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain

21 January 2018

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Pyrazolo[1,5-c]quinazoline derivatives and their simplified analogues as adenosine receptor antagonists: synthesis, structure-affinity relationships and molecular modeling studies.

21 January 2018

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Exploring the directionality of 5-substitutions in a new series of 5-alkylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine as a strategy to design novel human a(3) adenosine receptor antagonists.

21 January 2018

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Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.

21 January 2018

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Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment

21 January 2018

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21 January 2018

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Design of a novel cyclotide-based CXCR4 antagonist with anti-human immunodeficiency virus (HIV)-1 activity

21 January 2018

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21 January 2018

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Structure-based ligand discovery for the protein-protein interface of chemokine receptor CXCR4

21 January 2018

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Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor

21 January 2018

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Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening

21 January 2018

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Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies

21 January 2018

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Introduction to fragment-based drug discovery

21 January 2018

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Recent developments in fragment-based drug discovery

21 January 2018

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Vemurafenib: the first drug approved for BRAF-mutant cancer

21 January 2018

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Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

21 January 2018

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An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes.

21 January 2018

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Fragment screening of GPCRs using biophysical methods: identification of ligands of the adenosine A(2A) receptor with novel biological activity

21 January 2018

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Complementarity between in silico and biophysical screening approaches in fragment-based lead discovery against the A(2A) adenosine receptor

21 January 2018

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Surface plasmon resonance spectroscopy for characterisation of membrane protein-ligand interactions and its potential for drug discovery

21 January 2018

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Screening for GPCR Ligands Using Surface Plasmon Resonance

21 January 2018

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Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.

21 January 2018

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Fragment screening using capillary electrophoresis (CEfrag) for hit identification of heat shock protein 90 ATPase inhibitors

21 January 2018

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Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay

21 January 2018

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Biased signalling and allosteric machines: new vistas and challenges for drug discovery

21 January 2018

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Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.

21 January 2018

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Biophysical mapping of the adenosine A2A receptor

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7 January 2021

Use of the X-ray structure of the Beta2-adrenergic receptor for drug discovery

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7 January 2021

Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines

1 reference

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7 January 2021

Design and characterization of optimized adenosine A₂A/A₁ receptor antagonists for the treatment of Parkinson's disease

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7 January 2021

Ligand-, structure- and pharmacophore-based molecular fingerprints: a case study on adenosine A1, A2A, A2B, and A3 receptor antagonists

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7 January 2021

Rational design of conformationally constrained cyclopentapeptide antagonists for C-x-C chemokine receptor 4 (CXCR4)

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7 January 2021

Identifiers

DOI

10.1002/CMDC.201300382

1 reference

30 August 2017

1 reference