Structural insights into the human niacin receptor HCA2-Gi signalling complex

The niacin receptor HCAR2 modulates microglial response and limits disease progression in a mouse model of Alzheimer’s disease

(2022) Miguel Moutinho et al.   Science Translational Medicine

Role of HCA2 in Regulating Intestinal Homeostasis and Suppressing Colon Carcinogenesis

(2021) Zhuoyue Li et al.   Frontiers in Immunology

Structure, function and pharmacology of human itch GPCRs

(2021) Can Cao et al.   NATURE

Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-Gi Complex Structures

(2020) Tian Hua et al.   CELL

Hydroxycarboxylic Acid Receptor 2 Is a Zika Virus Restriction Factor That Can Be Induced by Zika Virus Infection Through the IRE1-XBP1 Pathway

(2020) Xiaocao Ma et al.   Frontiers in Cellular and Infection Microbiology

TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome

(2020) Reid H. J. Olsen et al.   Nature Chemical Biology

Author Correction: Structural insights into μ-opioid receptor activation

(2020) Weijiao Huang et al.   NATURE

Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor

(2020) Kuglae Kim et al.   CELL

Structure of a Signaling Cannabinoid Receptor 1-G Protein Complex

(2019) Kaavya Krishna Kumar et al.   CELL

Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes

(2019) Shoji Maeda et al.   SCIENCE

Molecular pharmacology of metabotropic receptors targeted by neuropsychiatric drugs

(2019) Bryan L. Roth   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Niacin Ameliorates Hepatic Steatosis by Inhibiting De Novo Lipogenesis Via a GPR109A-Mediated PKC–ERK1/2–AMPK Signaling Pathway in C57BL/6 Mice Fed a High-Fat Diet

(2019) Lingyan Ye et al.   JOURNAL OF NUTRITION

Common activation mechanism of class A GPCRs

(2019) Qingtong Zhou et al.   eLife

Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure–Functional Selectivity Relationships (SFSRs) and Therapeutic Potential

(2018) Liang Tan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein

(2018) Javier García-Nafría et al.   eLife

Dimethyl fumarate downregulates the immune response through the HCA 2 /GPR109A pathway: Implications for the treatment of multiple sclerosis

(2018) Felipe von Glehn et al.   Multiple Sclerosis and Related Disorders

Cryo-EM structure of human rhodopsin bound to an inhibitory G protein

(2018) Yanyong Kang et al.   NATURE

Structure of the adenosine-bound human adenosine A1 receptor–Gi complex

(2018) Christopher J. Draper-Joyce et al.   NATURE

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

(2018) Javier García-Nafría et al.   NATURE

Structure of the µ-opioid receptor–Gi protein complex

(2018) Antoine Koehl et al.   NATURE

A Bayesian approach to beam-induced motion correction in cryo-EM single-particle analysis

(2018) Jasenko Zivanov et al.   IUCrJ

Crystal structures of agonist-bound human cannabinoid receptor CB1

(2017) Tian Hua et al.   NATURE

MotionCor2: anisotropic correction of beam-induced motion for improved cryo-electron microscopy

(2017) Shawn Q Zheng et al.   NATURE METHODS

cryoSPARC: algorithms for rapid unsupervised cryo-EM structure determination

(2017) Ali Punjani et al.   NATURE METHODS

Hydroxy-Carboxylic Acid Receptor Actions in Metabolism

(2017) Stefan Offermanns   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Gctf: Real-time CTF determination and correction

(2016) Kai Zhang   JOURNAL OF STRUCTURAL BIOLOGY

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

(2016) Byron Carpenter et al.   NATURE

Dietary Fiber and Bacterial SCFA Enhance Oral Tolerance and Protect against Food Allergy through Diverse Cellular Pathways

(2016) Jian Tan et al.   Cell Reports

Discovery of 4-(phenyl)thio-1H-pyrazole derivatives as agonists of GPR109A, a high affinity niacin receptor

(2015) Hyeon Young Kim et al.   ARCHIVES OF PHARMACAL RESEARCH

Two disparate ligand-binding sites in the human P2Y1 receptor

(2015) Dandan Zhang et al.   NATURE

The Phyre2 web portal for protein modeling, prediction and analysis

(2015) Lawrence A Kelley et al.   Nature Protocols

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

(2015) Wesley K Kroeze et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

(2015) Wesley K Kroeze et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Activation of Gpr109a, Receptor for Niacin and the Commensal Metabolite Butyrate, Suppresses Colonic Inflammation and Carcinogenesis

(2014) Nagendra Singh et al.   IMMUNITY

Upregulation of GPR109A in Parkinson’s Disease

(2014) Chandramohan Wakade et al.   PLoS One

Free Fatty Acid (FFA) and Hydroxy Carboxylic Acid (HCA) Receptors

(2013) Stefan Offermanns   Annual Review of Pharmacology and Toxicology

Carboxylic Acid (Bio)Isosteres in Drug Design

(2013) Carlo Ballatore et al.   ChemMedChem

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

The Second Intracellular Loop of the Human Cannabinoid CB2 Receptor Governs G Protein Coupling in Coordination with the Carboxyl Terminal Domain

(2013) Congxia Zheng et al.   PLoS One

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

Exploiting structure similarity in refinement: automated NCS and target-structure restraints inBUSTER

(2012) Oliver S. Smart et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic Acid (MK-1903): A Potent GPR109a Agonist that Lowers Free Fatty Acids in Humans

(2012) P. Douglas Boatman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist

(2012) Kazuko Haga et al.   NATURE

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

(2012) Aashish Manglik et al.   NATURE

High-resolution crystal structure of human protease-activated receptor 1

(2012) Cheng Zhang et al.   NATURE

A crystal clear solution for determining G-protein-coupled receptor structures

(2012) Christopher G. Tate   TRENDS IN BIOCHEMICAL SCIENCES

Structure and function of an irreversible agonist-β2 adrenoceptor complex

(2011) Daniel M. Rosenbaum et al.   NATURE

International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B)

(2011) S. Offermanns et al.   PHARMACOLOGICAL REVIEWS

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Structural determinants in the second intracellular loop of the human cannabinoid CB1 receptor mediate selective coupling to Gs and Gi

(2010) XP Chen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Discovery of a Biaryl Cyclohexene Carboxylic Acid (MK-6892): A Potent and Selective High Affinity Niacin Receptor Full Agonist with Reduced Flushing Profiles in Animals as a Preclinical Candidate

(2010) Hong C. Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole–tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a

(2009) Jason E. Imbriglio et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

β-Arrestin1 mediates nicotinic acid–induced flushing, but not its antilipolytic effect, in mice

(2009) Robert W. Walters et al.   JOURNAL OF CLINICAL INVESTIGATION

Molecular modeling aided design of nicotinic acid receptor GPR109A agonists

(2008) Qiaolin Deng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans

(2008) Eseng Lai et al.   Journal of Clinical Lipidology

3-(1H-Tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): A Partial Agonist of the Nicotinic Acid Receptor, G-Protein Coupled Receptor 109a, with Antilipolytic but No Vasodilatory Activity in Mice

(2008) Graeme Semple et al.   JOURNAL OF MEDICINAL CHEMISTRY

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE