Nature Search

Structural basis of ligand recognition and design of antihistamines targeting histamine H₄ receptor

The histamine H₄ receptor (H₄R) plays key roles in immune cell function. Here, the authors report structures of H₄R-Gi complex with various ligands bound, revealing distinct ligand binding modes and a basis for rational design of novel antihistamines targeting H₄R.

Ruixue Xia
Shuang Shi
Yuanzheng He
ResearchOpen Access20 Mar 2024
Nature Communications

Volume: 15, P: 1-13
Structural visualization of small molecule recognition by CXCR3 uncovers dual-agonism in the CXCR3-CXCR7 system

CXCR3 and CXCR7 are chemokine receptors involved in cellular migration in physiological and pathophysiological context. Here, the authors present cryo-EM structures of CXCR3 in complex with small molecule agonists and discover their dual-agonism at CXCR7.

Shirsha Saha
Fumiya K. Sano
Arun K. Shukla
ResearchOpen Access28 Mar 2025
Nature Communications

Volume: 16, P: 1-18
Linking agonist binding to histamine H₁ receptor activation

Aldo Jongejan
Martijn Bruysters
Rob Leurs
Research19 Jun 2005
Nature Chemical Biology

Volume: 1, P: 98-103
Opioids activate brain analgesic circuits through cytochrome P450/epoxygenase signaling

The authors generated a mutant mouse with neuron-specific reductions in brain cytochrome P450 activity. These mice have attenuated morphine antinociception, which suggests that neuronal P450 epoxygenase mediates the pain-relieving properties of morphine.

Jennie L Conroy
Cheng Fang
Lindsay B Hough
Research07 Feb 2010
Nature Neuroscience

Volume: 13, P: 284-286
The histamine H₃ receptor: from gene cloning to H₃ receptor drugs

Rob Leurs
Remko A. Bakker
Iwan J. P. de Esch
Reviews24 Jan 2005
Nature Reviews Drug Discovery

Volume: 4, P: 107-120
Role of H₃-Receptor-Mediated Signaling in Anxiety and Cognition in Wild-Type and Apoe^–/– Mice

Gerald Bongers
Rob Leurs
Jacob Raber
Research12 Nov 2003
Neuropsychopharmacology

Volume: 29, P: 441-449
Herpesvirus-encoded GPCRs: neglected players in inflammatory and proliferative diseases?

Herpesviruses can hijack the G protein-coupled receptor (GPCR)-mediated cellular signalling networks of their host, which subverts cellular signalling and contributes to viral pathogenesis. In this Review, the authors discuss how herpesvirus-encoded GPCRs could be promising targets in certain inflammatory and proliferative diseases.

Henry F. Vischer
Marco Siderius
Martine J. Smit
Reviews21 Jan 2014
Nature Reviews Drug Discovery

Volume: 13, P: 123-139
Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells

Leigh A. Stoddart
Andrea J. Vernall
Stephen J. Hill
ResearchOpen Access25 Jan 2018
Scientific Reports

Volume: 8, P: 1-19
Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor

Reggie Bosma
Leigh A. Stoddart
Rob Leurs
ResearchOpen Access27 May 2019
Scientific Reports

Volume: 9, P: 1-13
The constitutive activity of the virally encoded chemokine receptor US28 accelerates glioblastoma growth

Raimond Heukers
Tian Shu Fan
Martine J. Smit
ResearchOpen Access30 Apr 2018
Oncogene

Volume: 37, P: 4110-4121
Function-specific virtual screening for GPCR ligands using a combined scoring method

Albert J. Kooistra
Henry F. Vischer
Chris de Graaf
ResearchOpen Access24 Jun 2016
Scientific Reports

Volume: 6, P: 1-21

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Structural basis of ligand recognition and design of antihistamines targeting histamine H₄ receptor

Structural visualization of small molecule recognition by CXCR3 uncovers dual-agonism in the CXCR3-CXCR7 system

Linking agonist binding to histamine H₁ receptor activation

Opioids activate brain analgesic circuits through cytochrome P450/epoxygenase signaling

The histamine H₃ receptor: from gene cloning to H₃ receptor drugs

Role of H₃-Receptor-Mediated Signaling in Anxiety and Cognition in Wild-Type and Apoe^–/– Mice

Herpesvirus-encoded GPCRs: neglected players in inflammatory and proliferative diseases?

Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor

The constitutive activity of the virally encoded chemokine receptor US28 accelerates glioblastoma growth

Function-specific virtual screening for GPCR ligands using a combined scoring method

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