Orphan GPR146: an alternative therapeutic pathway to achieve cholesterol homeostasis?

Constitutive G protein coupling profiles of understudied orphan GPCRs

(2021) Sumin Lu et al.   PLoS One

Low-density lipoproteins cause atherosclerotic cardiovascular disease: pathophysiological, genetic, and therapeutic insights: a consensus statement from the European Atherosclerosis Society Consensus Panel

(2020) Jan Borén et al.   EUROPEAN HEART JOURNAL

Hypercholesterolemia risk-associated GPR146 is an orphan G-protein coupled receptor that regulates blood cholesterol levels in humans and mice

(2020) Fangfang Han et al.   CELL RESEARCH

Is GPR146 really the receptor for proinsulin C-peptide?

(2020) Lina Lindfors et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Long-term safety and efficacy of lomitapide in patients with homozygous familial hypercholesterolemia: Five-year data from the Lomitapide Observational Worldwide Evaluation Registry (LOWER)

(2020) James A. Underberg et al.   Journal of Clinical Lipidology

NPY stimulates cholesterol synthesis acutely by activating the SREBP2-HMGCR pathway through the Y1 and Y5 receptors in murine hepatocytes

(2020) Fu Chen et al.   LIFE SCIENCES

GPCRdb in 2021: integrating GPCR sequence, structure and function

(2020) Albert J Kooistra et al.   NUCLEIC ACIDS RESEARCH

Constitutively active BRS3 is a genuinely orphan GPCR in placental mammals

(2019) Huihao Tang et al.   PLOS BIOLOGY

2019 ACC/AHA Guideline on the Primary Prevention of Cardiovascular Disease

(2019) Donna K. Arnett et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

GPR146 Deficiency Protects against Hypercholesterolemia and Atherosclerosis

(2019) Haojie Yu et al.   CELL

Novel approaches leading towards peptide GPCR de‐orphanisation

(2019) Alexander S. Hauser et al.   BRITISH JOURNAL OF PHARMACOLOGY

Mechanisms and regulation of cholesterol homeostasis

(2019) Jie Luo et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Massive mining of publicly available RNA-seq data from human and mouse

(2018) Alexander Lachmann et al.   Nature Communications

Mipomersen and its use in familial hypercholesterolemia

(2018) Johnathon Seth Parham et al.   EXPERT OPINION ON PHARMACOTHERAPY

2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA Guideline on the Management of Blood Cholesterol

(2018) Scott M. Grundy et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Single-cell transcriptomics of 20 mouse organs creates a Tabula Muris

(2018) et al.   NATURE

Genetics of blood lipids among ~300,000 multi-ethnic participants of the Million Veteran Program

(2018) Derek Klarin et al.   NATURE GENETICS

Exome-wide association study of plasma lipids in >300,000 individuals

(2017) Dajiang J Liu et al.   NATURE GENETICS

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

(2017) Alexander S. Hauser et al.   NATURE REVIEWS DRUG DISCOVERY

The mystery of membrane organization: composition, regulation and roles of lipid rafts

(2017) Erdinc Sezgin et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Familial hypercholesterolaemia

(2017) Joep C. Defesche et al.   Nature Reviews Disease Primers

Glucagon regulates hepatic lipid metabolism via cAMP and Insig-2 signaling: implication for the pathogenesis of hypertriglyceridemia and hepatic steatosis

(2016) Hai Wang et al.   Scientific Reports

Characterization of Autosomal Dominant Hypercholesterolemia Caused byPCSK9Gain of Function Mutations and Its Specific Treatment With Alirocumab, a PCSK9 Monoclonal AntibodyCLINICAL PERSPECTIVE

(2015) Paul N. Hopkins et al.   Circulation-Cardiovascular Genetics

Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65

(2015) Xi-Ping Huang et al.   NATURE

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

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

Tissue-based map of the human proteome

(2015) M. Uhlen et al.   SCIENCE

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

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

Characterization of Autosomal Dominant Hypercholesterolemia Caused byPCSK9Gain of Function Mutations and Its Specific Treatment With Alirocumab, a PCSK9 Monoclonal AntibodyCLINICAL PERSPECTIVE

(2015) Paul N. Hopkins et al.   Circulation-Cardiovascular Genetics

Rapid Knockout and Reporter Mouse Line Generation and Breeding Colony Establishment Using EUCOMM Conditional-Ready Embryonic Stem Cells: A Case Study

(2015) James L. J. Coleman et al.   Frontiers in Endocrinology

Liver histology during Mipomersen therapy for severe hypercholesterolemia

(2014) Nikroo Hashemi et al.   Journal of Clinical Lipidology

Validating Antibodies to the Cannabinoid CB2 Receptor

(2014) Yannick Marchalant et al.   JOURNAL OF HISTOCHEMISTRY & CYTOCHEMISTRY

Orexin/hypocretin receptor signalling cascades

(2013) J P Kukkonen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Familial hypercholesterolaemia is underdiagnosed and undertreated in the general population: guidance for clinicians to prevent coronary heart disease: Consensus Statement of the European Atherosclerosis Society

(2013) B. G. Nordestgaard et al.   EUROPEAN HEART JOURNAL

Evidence for an interaction between proinsulin C-peptide and GPR146

(2013) Gina L C Yosten et al.   JOURNAL OF ENDOCRINOLOGY

Discovery and refinement of loci associated with lipid levels

(2013) Cristen J Willer et al.   NATURE GENETICS

Intracellular Trafficking and Secretion of VLDL

(2012) Samata Tiwari et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

GLP-1 Receptor Activation Indirectly Reduces Hepatic Lipid Accumulation But Does Not Attenuate Development of Atherosclerosis in Diabetic MaleApoE−/−Mice

(2012) Naim Panjwani et al.   ENDOCRINOLOGY

Polyomic profiling reveals significant hepatic metabolic alterations in glucagon-receptor (GCGR) knockout mice: implications on anti-glucagon therapies for diabetes

(2011) Jianxin Yang et al.   BMC GENOMICS

The metabolic actions of glucagon revisited

(2010) Kirk M. Habegger et al.   Nature Reviews Endocrinology

Cellular cholesterol delivery, intracellular processing and utilization for biosynthesis of steroid hormones

(2010) Jie Hu et al.   Nutrition & Metabolism

How reliable are G-protein-coupled receptor antibodies?

(2009) Martin C. Michel et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

ERK phosphorylation: Spatial and temporal regulation by G protein-coupled receptors

(2008) Lauren T. May et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Molecular basis for LDL receptor recognition by PCSK9

(2008) H. J. Kwon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Specific Cholesterol Binding Site Is Established by the 2.8 Å Structure of the Human β2-Adrenergic Receptor

(2008) Michael A. Hanson et al.   STRUCTURE

Heterotrimeric G protein activation by G-protein-coupled receptors

(2007) William M. Oldham et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY