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Impact of GPCR Structures on Drug Discovery

Cell, 2020-04, Vol.181 (1), p.81-91

2020

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Cryo-Electron Microscopy: Moving Beyond X-Ray Crystal Structures for Drug Receptors and Drug Development

Annual review of pharmacology and toxicology, 2020-01, Vol.60, p.51

2020

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Structure of the adenosine A2A receptor bound to an engineered G protein

Nature (London), 2016-08, Vol.536 (7614), p.104-107

2016

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Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

The Journal of biological chemistry, 2018-05, Vol.293 (19), p.7466-7473

2018

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Cryo-EM structure of the serotonin 5-HT1B receptor coupled to heterotrimeric Go

Nature (London), 2018-06, Vol.558 (7711), p.620-623

2018

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Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Nature (London), 2011-05, Vol.474 (7352), p.521-525

2011

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Active state structures of G protein-coupled receptors highlight the similarities and differences in the G protein and arrestin coupling interfaces

Current opinion in structural biology, 2017-08, Vol.45, p.124-132

2017

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Crystal Structures of a Stabilized β1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol

Structure (London), 2012-05, Vol.20 (5), p.841-849

2012

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Mini-G proteins: Novel tools for studying GPCRs in their active conformation

PloS one, 2017-04, Vol.12 (4), p.e0175642-e0175642

2017

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How Can Mutations Thermostabilize G-Protein-Coupled Receptors?

Trends in pharmacological sciences (Regular ed.), 2016-01, Vol.37 (1), p.37-46

2016

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Diverse activation pathways in class A GPCRs converge near the G-protein-coupling region

Nature (London), 2016-08, Vol.536 (7617), p.484-487

2016

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Structure of the agonist-bound neurotensin receptor

Nature (London), 2012-10, Vol.490 (7421), p.508-513

2012

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PtdIns(4,5)P2 stabilizes active states of GPCRs and enhances selectivity of G-protein coupling

Nature (London), 2018-07, Vol.559 (7714), p.423-427

2018

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Molecular basis for high-affinity agonist binding in GPCRs

Science (American Association for the Advancement of Science), 2019-05, Vol.364 (6442), p.775-778

2019

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The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

Nature (London), 2011-01, Vol.469 (7329), p.241-244

2011

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Overexpression of membrane proteins in mammalian cells for structural studies

Molecular membrane biology, 2013-02, Vol.30 (1), p.52-63

2013

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Structure of the class D GPCR Ste2 dimer coupled to two G proteins

Nature (London), 2021-01, Vol.589 (7840), p.148-153

2021

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Structure of a β1-adrenergic G-protein-coupled receptor

Nature (London), 2008-07, Vol.454 (7203), p.486-491

2008

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The 2.1 Å resolution structure of cyanopindolol-bound β1-adrenoceptor identifies an intramembrane Na+ ion that stabilises the ligand-free receptor

PloS one, 2014-03, Vol.9 (3), p.e92727-e92727

2014

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Thermostabilisation of an Agonist-Bound Conformation of the Human Adenosine A2A Receptor

Journal of molecular biology, 2011-06, Vol.409 (3), p.298-310

2011

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Insight into partial agonism by observing multiple equilibria for ligand-bound and Gs-mimetic nanobody-bound β1-adrenergic receptor

Nature communications, 2017-11, Vol.8 (1), p.1-12, Article 1795

2017

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Quality Control in Eukaryotic Membrane Protein Overproduction

Journal of molecular biology, 2014-12, Vol.426 (24), p.4139-4154

2014

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Conformational thermostabilization of the β1-adrenergic receptor in a detergent-resistant form

Proceedings of the National Academy of Sciences - PNAS, 2008-01, Vol.105 (3), p.877-882

2008

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A mutagenesis and screening strategy to generate optimally thermostabilized membrane proteins for structural studies

Nature protocols, 2016-08, Vol.11 (8), p.1554-1571

2016

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Biophysical Fragment Screening of the β1‑Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design

Journal of medicinal chemistry, 2013-05, Vol.56 (9), p.3446-3455

2013

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Impact of GPCR Structures on Drug Discovery

Cryo-Electron Microscopy: Moving Beyond X-Ray Crystal Structures for Drug Receptors and Drug Development

Structure of the adenosine A2A receptor bound to an engineered G protein

Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

Cryo-EM structure of the serotonin 5-HT1B receptor coupled to heterotrimeric Go

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Active state structures of G protein-coupled receptors highlight the similarities and differences in the G protein and arrestin coupling interfaces

Crystal Structures of a Stabilized β1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol

Mini-G proteins: Novel tools for studying GPCRs in their active conformation

How Can Mutations Thermostabilize G-Protein-Coupled Receptors?

Diverse activation pathways in class A GPCRs converge near the G-protein-coupling region

Structure of the agonist-bound neurotensin receptor

PtdIns(4,5)P2 stabilizes active states of GPCRs and enhances selectivity of G-protein coupling

Molecular basis for high-affinity agonist binding in GPCRs

The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

Overexpression of membrane proteins in mammalian cells for structural studies

Structure of the class D GPCR Ste2 dimer coupled to two G proteins

Structure of a β1-adrenergic G-protein-coupled receptor

The 2.1 Å resolution structure of cyanopindolol-bound β1-adrenoceptor identifies an intramembrane Na+ ion that stabilises the ligand-free receptor

Thermostabilisation of an Agonist-Bound Conformation of the Human Adenosine A2A Receptor

Insight into partial agonism by observing multiple equilibria for ligand-bound and Gs-mimetic nanobody-bound β1-adrenergic receptor

Quality Control in Eukaryotic Membrane Protein Overproduction

Conformational thermostabilization of the β1-adrenergic receptor in a detergent-resistant form

A mutagenesis and screening strategy to generate optimally thermostabilized membrane proteins for structural studies

Biophysical Fragment Screening of the β1‑Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design

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