4.1 Article

Cholesterol in GPCR Structures: Prevalence and Relevance

Related references

Note: Only part of the references are listed.
Review Biochemistry & Molecular Biology

Allosteric Modulation of GPCRs of Class A by Cholesterol

Jan Jakubik et al.

Summary: G-protein coupled receptors (GPCRs) are membrane proteins that transmit extracellular signals to cells, and membrane cholesterol plays a significant role in regulating their function through direct binding and membrane property changes. Cholesterol affects ligand binding and activation of GPCRs, as well as altering their oligomerization state. Manipulating membrane cholesterol levels or modulating cholesterol binding sites on GPCRs may have potential for the development of new therapies.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

Article Biochemistry & Molecular Biology

Membrane cholesterol regulates endocytosis and trafficking of the serotonin1A receptor: Insights from acute cholesterol depletion

G. Aditya Kumar et al.

Summary: The role of membrane cholesterol in regulating GPCR endocytosis is explored in this study, showing how acute cholesterol depletion affects the internalization and intracellular trafficking of the serotonin1A receptor. Cholesterol depletion leads to altered endocytic pathway and lysosomal degradation of the receptor, indicating a novel cholesterol-dependent role in GPCR trafficking.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS (2021)

Article Multidisciplinary Sciences

Structural insights into the lipid and ligand regulation of serotonin receptors

Peiyu Xu et al.

Summary: This study investigates the structural and regulatory mechanisms of serotonin receptors, revealing the roles of phosphatidylinositol 4-phosphate and cholesterol molecules in modulating receptor activity and drug binding, while also uncovering how serotonin acts as a pan-agonist.

NATURE (2021)

Article Biochemistry & Molecular Biology

Predictable cholesterol binding sites in GPCRs lack consensus motifs

Geoffrey J. Taghon et al.

Summary: Research has shown that cholesterol binds in a similar manner in cryo-EM and X-ray structures of GPCRs, with 92% of cholesterol molecules residing in predictable locations lacking discernable cholesterol-binding motifs.

STRUCTURE (2021)

Article Biochemistry & Molecular Biology

Structural dynamics bridge the gap between the genetic and functional levels of GPCRs

Mariona Torrens-Fontanals et al.

Summary: G protein-coupled receptors are crucial in human physiological processes and are affected by genetic encoding and sequence diversity. Understanding the link between protein sequence, structure, and function is essential for interpreting the physiological response of GPCRs.

CURRENT OPINION IN STRUCTURAL BIOLOGY (2021)

Article Biochemical Research Methods

Conformational plasticity and dynamic interactions of the N-terminal domain of the chemokine receptor CXCR1

Shalmali Kharche et al.

Summary: This study investigates the interaction between CXCR1 and IL8, showing that ligand binding restricts the conformational plasticity of the apo-receptor N-terminal domain, leading to an open C-shaped conformation. These findings suggest a new strategy for understanding intrinsically disordered regions in GPCRs.

PLOS COMPUTATIONAL BIOLOGY (2021)

Article Multidisciplinary Sciences

A molecular sensor for cholesterol in the human serotonin1A receptor

G. Aditya Kumar et al.

Summary: Several G protein-coupled receptors (GPCRs) exhibit cholesterol sensitivity, attributed to specific sequences and structural features like the CRAC motif. This study explored the molecular basis of cholesterol sensitivity in the serotonin(1A) receptor and found a crucial lysine residue for sensing altered membrane cholesterol levels. Insights from molecular dynamics simulations revealed that cholesterol-sensitive functional states in the receptor are associated with reduced conformational dynamics of extracellular loops.

SCIENCE ADVANCES (2021)

Review Biochemistry & Molecular Biology

G protein-coupled receptors: structure- and function-based drug discovery

Dehua Yang et al.

Summary: Recent progress in understanding the structure-function relationships of G protein-coupled receptors has accelerated drug development significantly. This article aims to provide a comprehensive overview of this important field to a broader readership interested in drug discovery.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)

Article Biochemistry & Molecular Biology

Statin-Induced Chronic Cholesterol Depletion Switches GPCR Endocytosis and Trafficking: Insights from the Serotonin1A Receptor

G. Aditya Kumar et al.

ACS CHEMICAL NEUROSCIENCE (2020)

Review Medicine, Research & Experimental

Cholesterol interaction motifs in G protein-coupled receptors: Slippery hot spots?

Parijat Sarkar et al.

WILEY INTERDISCIPLINARY REVIEWS-SYSTEMS BIOLOGY AND MEDICINE (2020)

Editorial Material Multidisciplinary Sciences

The quest for high-resolution G protein-coupled receptor-G protein structures

Reinhard Grisshammer

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2020)

Review Cell Biology

Conformational Basis of G Protein-Coupled Receptor Signaling Versatility

Laura M. Wingler et al.

TRENDS IN CELL BIOLOGY (2020)

Review Biochemistry & Molecular Biology

How Do Molecular Dynamics Data Complement Static Structural Data of GPCRs

Mariona Torrens-Fontanals et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

Article Biophysics

Interfacial Binding Sites for Cholesterol on G Protein-Coupled Receptors

Anthony G. Lee

BIOPHYSICAL JOURNAL (2019)

Article Biochemistry & Molecular Biology

Molecular switches in GPCRs

Slawomir Filipek

CURRENT OPINION IN STRUCTURAL BIOLOGY (2019)

Review Pharmacology & Pharmacy

GPCRomics: An Approach to Discover GPCR Drug Targets

Paul A. Insel et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2019)

Review Biochemistry & Molecular Biology

Extramembranous Regions in G Protein-Coupled Receptors: Cinderella in Receptor Biology?

Sreetama Pal et al.

JOURNAL OF MEMBRANE BIOLOGY (2019)

Article Chemistry, Physical

Cholesteryl Hemisuccinate Is Not a Good Replacement for Cholesterol in Lipid Nanodiscs

Bozena Augustyn et al.

JOURNAL OF PHYSICAL CHEMISTRY B (2019)

Review Biotechnology & Applied Microbiology

GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

Ichio Shimada et al.

NATURE REVIEWS DRUG DISCOVERY (2019)

Review Biochemistry & Molecular Biology

New Binding Sites, New Opportunities for GPCR Drug Discovery

H. C. Stephen Chan et al.

TRENDS IN BIOCHEMICAL SCIENCES (2019)

Article Chemistry, Physical

Exploring GPCR-Lipid Interactions by Molecular Dynamics Simulations: Excitements, Challenges, and the Way Forward

Durba Sengupta et al.

JOURNAL OF PHYSICAL CHEMISTRY B (2018)

Editorial Material Cell Biology

Illuminating GPCR Signaling by Cryo-EM

Haaris Ahsan Safdari et al.

TRENDS IN CELL BIOLOGY (2018)

Review Biochemistry & Molecular Biology

The Molecular Basis of G Protein-Coupled Receptor Activation

William I. Weis et al.

ANNUAL REVIEW OF BIOCHEMISTRY, VOL 87 (2018)

Review Chemistry, Multidisciplinary

GPCR Dynamics: Structures in Motion

Naomi R. Latorraca et al.

CHEMICAL REVIEWS (2017)

Article Biochemistry & Molecular Biology

Interaction of G protein coupled receptors and cholesterol

Gerald Gimpl

CHEMISTRY AND PHYSICS OF LIPIDS (2016)

Review Spectroscopy

Cholesterol: An evergreen molecule in biology

G. Aditya Kumar et al.

BIOMEDICAL SPECTROSCOPY AND IMAGING (2016)

Article Biochemistry & Molecular Biology

Experimental determination and computational interpretation of biophysical properties of lipid bilayers enriched by cholesteryl hemisuccinate

Waldemar Kulig et al.

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES (2015)

Review Biochemistry & Molecular Biology

Molecular dynamics simulations of GPCR-cholesterol interaction: An emerging paradigm

Durba Sengupta et al.

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES (2015)

Review Cell Biology

Methodological advances: the unsung heroes of the GPCR structural revolution

Eshan Ghosh et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2015)

Article Biochemical Research Methods

A comprehensive review of the lipid cubic phase or in meso method for crystallizing membrane and soluble proteins and complexes

Martin Caffrey

ACTA CRYSTALLOGRAPHICA SECTION F-STRUCTURAL BIOLOGY COMMUNICATIONS (2015)

Article Biochemistry & Molecular Biology

How well does cholesteryl hemisuccinate mimic cholesterol in saturated phospholipid bilayers?

Waldemar Kulig et al.

JOURNAL OF MOLECULAR MODELING (2014)

Article Biochemistry & Molecular Biology

Membrane Lipids in the Function of Serotonin and Adrenergic Receptors

Md. Jafurulla et al.

CURRENT MEDICINAL CHEMISTRY (2013)

Editorial Material Biology

Regulation of G protein-coupled receptors by palmitoylation and cholesterol

Alan D. Goddard et al.

BMC BIOLOGY (2012)

Article Chemistry, Physical

Identification of Cholesterol Binding Sites in the Serotonin1A Receptor

Durba Sengupta et al.

JOURNAL OF PHYSICAL CHEMISTRY B (2012)

Article Chemistry, Multidisciplinary

Why GPCRs behave differently in cubic and lamellar lipidic mesophases

George Khelashvili et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2012)

Article Multidisciplinary Sciences

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

Wei Liu et al.

SCIENCE (2012)

Review Pharmacology & Pharmacy

Diversity and modularity of G protein-coupled receptor structures

Vsevolod Katritch et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2012)

Article Biochemistry & Molecular Biology

Identification of cholesterol recognition amino acid consensus (CRAC) motif in G-protein coupled receptors

Md. Jafurulla et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2011)

Article Biochemistry & Molecular Biology

Uncovering the intimate relationship between lipids, cholesterol and GPCR activation

Joanne Oates et al.

CURRENT OPINION IN STRUCTURAL BIOLOGY (2011)

Article Biochemistry & Molecular Biology

Functional characterization of putative cholesterol binding sequence (CRAC) in human type-1 cannabinoid receptor

Sergio Oddi et al.

JOURNAL OF NEUROCHEMISTRY (2011)

Review Biochemistry & Molecular Biology

Are specific nonannular cholesterol binding sites present in G-protein coupled receptors?

Yamuna Devi Paila et al.

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES (2009)

Review Multidisciplinary Sciences

The structure and function of G-protein-coupled receptors

Daniel M. Rosenbaum et al.

NATURE (2009)

Article Multidisciplinary Sciences

GPCR engineering yields high-resolution structural insights into β2-adrenergic receptor function

Daniel M. Rosenbaum et al.

SCIENCE (2007)

Article Biochemical Research Methods

A monoclonal antibody for G protein-coupled receptor crystallography

Peter W. Day et al.

NATURE METHODS (2007)

Review Biochemistry & Molecular Biology

Role of cholesterol in the function and organization of G-protein coupled receptors

Thomas J. Pucadyil et al.

PROGRESS IN LIPID RESEARCH (2006)

Review Biochemistry & Molecular Biology

Cholesterol and the interaction of proteins with membrane domains

Richard M. Epand

PROGRESS IN LIPID RESEARCH (2006)

Review Biochemical Research Methods

Structure modeling of all identified G protein-coupled receptors in the human genome

Yang Zhang et al.

PLOS COMPUTATIONAL BIOLOGY (2006)

Article Biochemistry & Molecular Biology

What's so special about cholesterol?

OG Mouritsen et al.

LIPIDS (2004)

Review Cell Biology

Seven-transmembrane receptors

KL Pierce et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2002)