Regulation of membrane protein structure and function by their lipid nano-environment

I Levental, E Lyman - Nature Reviews Molecular Cell Biology, 2023 - nature.com
Transmembrane proteins comprise~ 30% of the mammalian proteome, mediating
metabolism, signalling, transport and many other functions required for cellular life. The …

International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update

AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - ASPET
Our previous International Union of Basic and Clinical Pharmacology report on the
nomenclature and classification of adenosine receptors (2011) contained a number of …

Martini 3: a general purpose force field for coarse-grained molecular dynamics

PCT Souza, R Alessandri, J Barnoud, S Thallmair… - Nature …, 2021 - nature.com
The coarse-grained Martini force field is widely used in biomolecular simulations. Here we
present the refined model, Martini 3 (http://cgmartini. nl), with an improved interaction …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

Structure-based design of bitopic ligands for the µ-opioid receptor

A Faouzi, H Wang, SA Zaidi, JF DiBerto, T Che, Q Qu… - Nature, 2023 - nature.com
Mu-opioid receptor (µOR) agonists such as fentanyl have long been used for pain
management, but are considered a major public health concern owing to their adverse side …

[PDF][PDF] How ligands illuminate GPCR molecular pharmacology

D Wacker, RC Stevens, BL Roth - Cell, 2017 - cell.com
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …

Emerging diversity in lipid–protein interactions

V Corradi, BI Sejdiu, H Mesa-Galloso… - Chemical …, 2019 - ACS Publications
Membrane lipids interact with proteins in a variety of ways, ranging from providing a stable
membrane environment for proteins to being embedded in to detailed roles in complicated …

GPCR dynamics: structures in motion

NR Latorraca, AJ Venkatakrishnan, RO Dror - Chemical reviews, 2017 - ACS Publications
The function of G protein-coupled receptors (GPCRs) which represent the largest class of
both human membrane proteins and drug targets depends critically on their ability to …

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

CJ Draper-Joyce, M Khoshouei, DM Thal, YL Liang… - Nature, 2018 - nature.com
The class A adenosine A1 receptor (A1R) is a G-protein-coupled receptor that preferentially
couples to inhibitory Gi/o heterotrimeric G proteins, has been implicated in numerous …

Structural insights into µ-opioid receptor activation

W Huang, A Manglik, AJ Venkatakrishnan… - Nature, 2015 - nature.com
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …