Trends in GPCR drug discovery: new agents, targets and indications

Commensal bacteria make GPCR ligands that mimic human signalling molecules

(2017) Louis J. Cohen et al.   NATURE

Opportunities for therapeutic antibodies directed at G-protein-coupled receptors

(2017) Catherine J. Hutchings et al.   NATURE REVIEWS DRUG DISCOVERY

2016 FDA drug approvals

(2017) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Angiotensin II for the Treatment of Vasodilatory Shock

(2017) Ashish Khanna et al.   NEW ENGLAND JOURNAL OF MEDICINE

Allosteric “beta-blocker” isolated from a DNA-encoded small molecule library

(2017) Seungkirl Ahn et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structurally Enabled Discovery of Adenosine A2A Receptor Antagonists

(2016) Ali Jazayeri et al.   CHEMICAL REVIEWS

Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

(2016) Denise Wootten et al.   CHEMICAL REVIEWS

Serotonin 5-HT6 Receptor Antagonists in Alzheimer’s Disease: Therapeutic Rationale and Current Development Status

(2016) Hilda Ferrero et al.   CNS DRUGS

Editorial overview: New technologies: GPCR drug design and function — exploiting the current (of) structures

(2016) Christofer S Tautermann et al.   CURRENT OPINION IN PHARMACOLOGY

Once-Daily Liraglutide Versus Lixisenatide as Add-on to Metformin in Type 2 Diabetes: A 26-Week Randomized Controlled Clinical Trial

(2016) Michael Nauck et al.   DIABETES CARE

Effect of Abaloparatide vs Placebo on New Vertebral Fractures in Postmenopausal Women With Osteoporosis

(2016) Paul D. Miller et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Targeting orphan G protein-coupled receptors for the treatment of diabetes and its complications: C-peptide and GPR146

(2016) G. R. Kolar et al.   JOURNAL OF INTERNAL MEDICINE

In vivo veritas, the next frontier for functionally selective GPCR ligands

(2016) Jean Martin Beaulieu   METHODS

Inside-out receptor inhibition

(2016) Thomas P. Sakmar et al.   NATURE

Can you teach old drugs new tricks?

(2016) Nicola Nosengo   NATURE

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

G protein-coupled receptors as targets for anti-diabetic therapeutics

(2016) Da Young Oh et al.   NATURE REVIEWS DRUG DISCOVERY

Cornerstones of CRISPR–Cas in drug discovery and therapy

(2016) Christof Fellmann et al.   NATURE REVIEWS DRUG DISCOVERY

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

Arbaclofen in Children and Adolescents with Autism Spectrum Disorder: A Randomized, Controlled, Phase 2 Trial

(2016) Jeremy Veenstra-VanderWeele et al.   NEUROPSYCHOPHARMACOLOGY

Open Targets: a platform for therapeutic target identification and validation

(2016) Gautier Koscielny et al.   NUCLEIC ACIDS RESEARCH

Alignment-free $d_2^*$ oligonucleotide frequency dissimilarity measure improves prediction of hosts from metagenomically-derived viral sequences

(2016) Nathan A. Ahlgren et al.   NUCLEIC ACIDS RESEARCH

A randomized, phase 2 study investigating TRV130, a biased ligand of the μ-opioid receptor, for the intravenous treatment of acute pain

(2016) Eugene R. Viscusi et al.   PAIN

Recent updates on GPCR biased agonism

(2016) André S. Pupo et al.   PHARMACOLOGICAL RESEARCH

Dopaminergic drugs in type 2 diabetes and glucose homeostasis

(2016) Felicitas Lopez Vicchi et al.   PHARMACOLOGICAL RESEARCH

Polypharmacology of dopamine receptor ligands

(2016) S. Butini et al.   PROGRESS IN NEUROBIOLOGY

New paradigms in GPCR drug discovery

(2015) Kenneth A. Jacobson   BIOCHEMICAL PHARMACOLOGY

Metabotropic glutamate receptors as drug targets: what's new?

(2015) Ferdinando Nicoletti et al.   CURRENT OPINION IN PHARMACOLOGY

Nanobodies and their Use in GPCR Drug Discovery

(2015) Karen Cromie et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

GPR40 agonists for the treatment of type 2 diabetes: life after ‘TAKing’ a hit

(2015) A. D. Mancini et al.   DIABETES OBESITY & METABOLISM

Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial

(2015) K. Kaku et al.   DIABETES OBESITY & METABOLISM

Structures of G protein-coupled receptors reveal new opportunities for drug discovery

(2015) Robert M. Cooke et al.   DRUG DISCOVERY TODAY

“Chemokine receptors as therapeutic targets: Why aren’t there more drugs?”

(2015) Roberto Solari et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Galanin receptors as a potential target for neurological disease

(2015) Krista Freimann et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Biased Agonism of the Angiotensin II Type I Receptor

(2015) Yuichi Ikeda et al.   International Heart Journal

Novel Therapeutic GPCRs for Psychiatric Disorders

(2015) Hidetoshi Komatsu   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Recognition of Bacterial Signal Peptides by Mammalian Formyl Peptide Receptors

(2015) Bernd Bufe et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

From G Protein-coupled Receptor Structure Resolution to Rational Drug Design

(2015) Ali Jazayeri et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Gut chemosensing mechanisms

(2015) Arianna Psichas et al.   JOURNAL OF CLINICAL INVESTIGATION

G Protein-Coupled Receptor 119 (GPR119) Agonists for the Treatment of Diabetes: Recent Progress and Prevailing Challenges

(2015) Kurt Ritter et al.   JOURNAL OF MEDICINAL CHEMISTRY

ASD v3.0: unraveling allosteric regulation with structural mechanisms and biological networks

(2015) Qiancheng Shen et al.   NUCLEIC ACIDS RESEARCH

The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands

(2015) Christopher Southan et al.   NUCLEIC ACIDS RESEARCH

GPCRdb: an information system for G protein-coupled receptors

(2015) Vignir Isberg et al.   NUCLEIC ACIDS RESEARCH

Insights into bombesin receptors and ligands: Highlighting recent advances

(2015) Irene Ramos-Álvarez et al.   PEPTIDES

Formyl peptide receptors at the interface of inflammation, angiogenesis and tumor growth

(2015) Nella Prevete et al.   PHARMACOLOGICAL RESEARCH

Tissue-based map of the human proteome

(2015) M. Uhlen et al.   SCIENCE

Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors

(2015) Ikuo Masuho et al.   Science Signaling

Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors

(2015) Ikuo Masuho et al.   Science Signaling

Evidence for the efficacy and effectiveness of THC-CBD oromucosal spray in symptom management of patients with spasticity due to multiple sclerosis

(2015) Uwe K. Zettl et al.   Therapeutic Advances in Neurological Disorders

Use of Antidiabetic Drugs in the U.S., 2003–2012

(2014) Christian Hampp et al.   DIABETES CARE

Targeting CB2-GPR55 Receptor Heteromers Modulates Cancer Cell Signaling

(2014) Estefanía Moreno et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Polypharmacology: Challenges and Opportunities in Drug Discovery

(2014) Andrew Anighoro et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biased ligands at G-protein-coupled receptors: promise and progress

(2014) Jonathan D. Violin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Allosteric and Biased G Protein-Coupled Receptor Signaling Regulation: Potentials for New Therapeutics

(2014) Etienne Khoury et al.   Frontiers in Endocrinology

The Druggable Genome: Evaluation of Drug Targets in Clinical Trials Suggests Major Shifts in Molecular Class and Indication

(2013) Mathias Rask-Andersen et al.   Annual Review of Pharmacology and Toxicology

The Dynamic Process of β2-Adrenergic Receptor Activation

(2013) Rie Nygaard et al.   CELL

Emerging paradigms in GPCR allostery: implications for drug discovery

(2013) Denise Wootten et al.   NATURE REVIEWS DRUG DISCOVERY

Development of allosteric modulators of GPCRs for treatment of CNS disorders

(2013) Hilary Highfield Nickols et al.   NEUROBIOLOGY OF DISEASE

DrugBank 4.0: shedding new light on drug metabolism

(2013) Vivian Law et al.   NUCLEIC ACIDS RESEARCH

Extrasensory perception: Odorant and taste receptors beyond the nose and mouth

(2013) Simon R. Foster et al.   PHARMACOLOGY & THERAPEUTICS

Tools for GPCR drug discovery

(2012) Ru Zhang et al.   ACTA PHARMACOLOGICA SINICA

G protein-coupled receptors as therapeutic targets for multiple sclerosis

(2012) Changsheng Du et al.   CELL RESEARCH

Trends in the exploitation of novel drug targets

(2011) Mathias Rask-Andersen et al.   NATURE REVIEWS DRUG DISCOVERY

The role of G protein-coupled receptors in the pathology of Alzheimer's disease

(2011) Amantha Thathiah et al.   NATURE REVIEWS NEUROSCIENCE

Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis

(2010) Volker Brinkmann et al.   NATURE REVIEWS DRUG DISCOVERY

Teaching old receptors new tricks: biasing seven-transmembrane receptors

(2010) Sudarshan Rajagopal et al.   NATURE REVIEWS DRUG DISCOVERY

G protein-coupled receptors: novel targets for drug discovery in cancer

(2010) Rosamaria Lappano et al.   NATURE REVIEWS DRUG DISCOVERY

The therapeutic potential of G-protein coupled receptors in Huntington's disease

(2010) Megan J. Dowie et al.   PHARMACOLOGY & THERAPEUTICS

Anatomical Profiling of G Protein-Coupled Receptor Expression

(2008) Jean B. Regard et al.   CELL

GPR119: “Double-Dipping” for Better Glycemic Control

(2008) L. Lauffer et al.   ENDOCRINOLOGY