☆ 4.8 Article

Functional screening and rational design of compounds targeting GPR132 to treat diabetes

NATURE METABOLISM (2023)

相关参考文献

注意：仅列出部分参考文献，下载原文获取全部文献信息。

Review Immunology

Macrophage function in adipose tissue homeostasis and metabolic inflammation

Triantafyllos Chavakis et al.

Summary: This review focuses on adipose tissue myeloid cells and their role in controlling and responding to inflammation and pathology. Obesity-related metabolic organ inflammation is a contributing factor to cardiometabolic disorders. Immune responses in adipose tissue, including expansion of immune cell populations and changes in their function, are triggered by alterations in lipid fluxes and storage in obese individuals. Recent studies suggest that adipose tissue macrophages (ATMs), a type of immune cell, also play important roles in lipid homeostasis. The review discusses the complex function of ATMs in adipose tissue homeostasis and metabolic inflammation. It also proposes that trained immunity, which involves long-term functional adaptations of myeloid cells, may be responsible for chronic systemic inflammation triggered by metabolic perturbations.

NATURE IMMUNOLOGY (2023)

添加到收藏夹

Review Gastroenterology & Hepatology

Nonalcoholic steatohepatitis-related hepatocellular carcinoma: pathogenesis and treatment

Josep M. Llovet et al.

Summary: Nonalcoholic fatty liver disease (NAFLD), including its more severe manifestation, nonalcoholic steatohepatitis (NASH), has a global prevalence of 20-25% and is a major public health problem. NASH-HCC, influenced by factors such as the immune microenvironment, PNPLA3 mutations, and the microbiome, has unique characteristics compared to other types of HCC and affects both men and women equally. The management of NASH-HCC involves surgery, locoregional therapies, and systemic therapies, with the future focus being on improving surveillance, developing targeted combination therapies, and identifying biomarkers for treatment responders.

NATURE REVIEWS GASTROENTEROLOGY & HEPATOLOGY (2023)

添加到收藏夹

Review Gastroenterology & Hepatology

Hepatic inflammatory responses in liver fibrosis

Linda Hammerich et al.

Summary: This Review provides an extensive overview of the mechanisms of inflammation and fibrosis in the liver, particularly in NAFLD or NASH, and discusses the current advances and therapeutic implications. Chronic liver diseases characterized by persistent inflammation and subsequent liver fibrosis have significant impact on long-term morbidity and mortality. Inflammatory responses involve hepatic cell types and signals related to intrahepatic injury pathways, gut-liver axis, and circulation.

NATURE REVIEWS GASTROENTEROLOGY & HEPATOLOGY (2023)

添加到收藏夹

Article Physiology

IL10 trains macrophage profibrotic function after lung injury

Aritra Bhattacharyya et al.

Summary: This study reveals the involvement of CX3CR1+ monocyte-derived macrophages (moMacs) in bleomycin-induced lung fibrosis through the production of Pdgfa. Analysis at the single-cell level shows high expression of the receptor IL10-RA in moMacs from human fibrotic lungs. Furthermore, a novel IL10-dependent mechanism of macrophage polarization is identified.

AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY (2022)

添加到收藏夹

Article Cell Biology

Autonomous sensing of the insulin peptide by an olfactory G protein-coupled receptor modulates glucose metabolism

Jie Cheng et al.

Summary: This study reveals that pancreatic beta cells use olfactory receptor Olfr109 to autonomously detect self-secreted insulin peptides, which inhibits insulin secretion and interacts with macrophages, leading to intra-islet inflammation.

CELL METABOLISM (2022)

添加到收藏夹

Article Multidisciplinary Sciences

Structure-based discovery of nonhallucinogenic psychedelic analogs

Dongmei Cao et al.

Summary: This study provides structural insights into the binding of drugs to 5-HT2AR and offers a foundation for the design of safe and effective nonhallucinogenic psychedelic analogs for the treatment of neuropsychiatric diseases.

SCIENCE (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Endogenous Lipid-GPR120 Signaling Modulates Pancreatic Islet Homeostasis to Different Extents

Ya-Qin Du et al.

Summary: This study reveals the existence of endogenous LCFA-GPR120 circuits in pancreatic islets that modulate islet homeostasis. Oleic acid (OA) and linoleic acid (LA) were identified as GPR120 agonists within the islets, promoting insulin secretion by inhibiting somatostatin secretion. LA exerted higher potency compared to OA, depending on beta-arrestin2 function. Impaired GPR120 signaling in diabetic models could be improved by replenishing OA and LA, and LA administration improved glucose metabolism in db/db mice.

DIABETES (2022)

添加到收藏夹

Article Multidisciplinary Sciences

Tethered peptide activation mechanism of the adhesion GPCRs ADGRG2 and ADGRG4

Peng Xiao et al.

Summary: In this study, three cryo-electron microscopy structures of aGPCRs coupled to the G(s) heterotrimer are presented, revealing the structural and biochemical insights into the tethered activation mechanism of aGPCRs. The structures of ADGRG2-beta-G(s) and ADGRG4-beta-G(s) complexes, as well as the ADGRG2(FL)-IP15-G(s) complex, provide valuable information about the binding and activation of aGPCRs by the Stachel sequences. Additionally, rational design of peptidic agonists and generation of peptidic antagonists for aGPCRs based on the aGPCR-beta structures are demonstrated.

NATURE (2022)

添加到收藏夹

Article Cell Biology

Mouse placenta fetal macrophages arise from endothelial cells outside the placenta

Xiaowen Chen et al.

Summary: Placental fetal macrophages in mice are found to originate from yolk sac endothelium, rather than from placental endothelial cells. Depletion of placental fMacs can be achieved by administering specific antibodies during early pregnancy. These findings provide insights into the origin and function of mouse placental fMacs.

DEVELOPMENTAL CELL (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease

Alastair J. H. Brown et al.

Summary: The study aims to design a well-tolerated M1 agonist with the potential to alleviate cognitive loss by translating from atomic structure to clinical trials, providing a strategy for targeting difficult GPCR targets effectively.

CELL (2021)

添加到收藏夹

Article Multidisciplinary Sciences

Structures of the glucocorticoid-bound adhesion receptor GPR97-Go complex

Yu-Qi Ping et al.

Summary: This study reveals how glucocorticoid stress hormones activate adhesion GPCR G3 and how glucocorticoids bind to its transmembrane domain, triggering receptor activation. The research also found that GPR97's cytoplasmic side has an open cavity where interactions with the Go protein contribute to its high basal activity.

NATURE (2021)

添加到收藏夹

Article Multidisciplinary Sciences

Restoring metabolism of myeloid cells reverses cognitive decline in ageing

Paras S. Minhas et al.

Summary: Ageing is characterized by chronic pro-inflammatory responses that affect various aspects of health, including the brain. The study shows that in ageing mice, myeloid cell bioenergetics are suppressed in response to increased signalling by the lipid messenger prostaglandin E-2 (PGE(2)), leading to maladaptive pro-inflammatory responses. By inhibiting myeloid EP2 signalling, it is possible to reverse cognitive ageing and restore youthful immune functions.

NATURE (2021)

添加到收藏夹

Article Cardiac & Cardiovascular Systems

MicroRNA-21-Dependent Macrophage-to-Fibroblast Signaling Determines the Cardiac Response to Pressure Overload

Deepak Ramanujam et al.

Summary: Recent research has shown that miR-21 is the most highly expressed microRNA in cardiac macrophages, playing a critical role in fibrosis and cardiac dysfunction. Furthermore, miR-21 regulates the polarization of macrophages towards an M1-like phenotype and promotes communication between macrophages and cardiac fibroblasts, leading to fibrotic remodeling.

CIRCULATION (2021)

添加到收藏夹

Article Multidisciplinary Sciences

Structure, function and pharmacology of human itch receptor complexes

Fan Yang et al.

Summary: MRGPRX2 is a key receptor involved in sensing basic secretagogues and eliciting itch signals and pseudoallergic reactions. The structures of its complex with G(i1) revealed shallow ligand-binding pockets and unique activation processes, providing a structural basis for designing therapies to prevent unwanted pseudoallergic reactions.

NATURE (2021)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Engineering islets from stem cells for advanced therapies of diabetes

Johanna Siehler et al.

Summary: Diabetes is a significant global health concern affecting millions of people, and advanced therapies utilizing stem cell differentiation and islet engineering may offer potential breakthroughs in treatment. Research in these areas could lead to improved understanding of pancreatic function and provide new insights into diabetes mechanisms.

NATURE REVIEWS DRUG DISCOVERY (2021)

添加到收藏夹

Review Gastroenterology & Hepatology

New insights into IL-6 family cytokines in metabolism, hepatology and gastroenterology

Maria D. Giraldez et al.

Summary: IL-6 family cytokines play crucial roles in metabolism, liver disease, and gastrointestinal disease, with potential as therapeutic targets. Therapies modulating gp130 signaling have shown promise in various clinical settings, including obesity, cancer, and inflammatory bowel disease.

NATURE REVIEWS GASTROENTEROLOGY & HEPATOLOGY (2021)

添加到收藏夹

Article Multidisciplinary Sciences

Virtual discovery of melatonin receptor ligands to modulate circadian rhythms

Reed M. Stein et al.

NATURE (2020)

添加到收藏夹

Review Endocrinology & Metabolism

The role of macrophages in obesity-associated islet inflammation and β-cell abnormalities

Wei Ying et al.

NATURE REVIEWS ENDOCRINOLOGY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

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

Reid H. J. Olsen et al.

NATURE CHEMICAL BIOLOGY (2020)

添加到收藏夹

Article Endocrinology & Metabolism

International consensus on the diagnosis and management of dumping syndrome

Emidio Scarpellini et al.

NATURE REVIEWS ENDOCRINOLOGY (2020)

添加到收藏夹

Article Multidisciplinary Sciences

Structural basis of GPBAR activation and bile acid recognition

Fan Yang et al.

NATURE (2020)

添加到收藏夹

Article Multidisciplinary Sciences

Ultra-large library docking for discovering new chemotypes

Jiankun Lyu et al.

NATURE (2019)

添加到收藏夹

Editorial Material Endocrinology & Metabolism

Understanding the mechanisms of reversal of type 2 diabetes

Roy Taylor et al.

LANCET DIABETES & ENDOCRINOLOGY (2019)

添加到收藏夹

Article Cell Biology

Expansion of Islet-Resident Macrophages Leads to Inflammation Affecting β Cell Proliferation and Function in Obesity

Wei Ying et al.

CELL METABOLISM (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Crystal structure of the endogenous agonist-bound prostanoid receptor EP3

Kazushi Morimoto et al.

NATURE CHEMICAL BIOLOGY (2019)

添加到收藏夹

Article Biology

Gq activity- and β-arrestin-1 scaffolding mediated ADGRG2/CFTR coupling are required for male fertility

Dao-Lai Zhang et al.

ELIFE (2018)

添加到收藏夹

Article Multidisciplinary Sciences

Specific oxylipins enhance vertebrate hematopoiesis via the receptor GPR132

Jamie L. Lahvic et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2018)

添加到收藏夹

Article Endocrinology & Metabolism

Mouse pancreatic islet macrophages use locally released ATP to monitor beta cell activity

Jonathan R. Weitz et al.

DIABETOLOGIA (2018)

添加到收藏夹

Review Chemistry, Multidisciplinary

GPCR Dynamics: Structures in Motion

Naomi R. Latorraca et al.

CHEMICAL REVIEWS (2017)

添加到收藏夹

Article Medicine, Research & Experimental

A cullin 4B-RING E3 ligase complex fine-tunes pancreatic δ cell paracrine interactions

Qing Li et al.

JOURNAL OF CLINICAL INVESTIGATION (2017)

添加到收藏夹

Article Immunology

The islet-resident macrophage is in an inflammatory state and senses microbial products in blood

Stephen T. Ferris et al.

JOURNAL OF EXPERIMENTAL MEDICINE (2017)

添加到收藏夹

Article Multidisciplinary Sciences

Crystal structures of agonist-bound human cannabinoid receptor CB1

Tian Hua et al.

NATURE (2017)

添加到收藏夹

Letter Biochemical Research Methods

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

Shawn Q. Zheng et al.

NATURE METHODS (2017)

添加到收藏夹

Article Multidisciplinary Sciences

D4 dopamine receptor high-resolution structures enable the discovery of selective agonists

Sheng Wang et al.

SCIENCE (2017)

添加到收藏夹

Article Multidisciplinary Sciences

Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling

Chun-Hua Liu et al.

NATURE COMMUNICATIONS (2017)

添加到收藏夹

Article Immunology

Promoter specificity and efficacy in Conditional and Inducible Transgenic targeting of Lung Macrophages

Alexandra L. McCubbrey et al.

FRONTIERS IN IMMUNOLOGY (2017)

添加到收藏夹

Article Chemistry, Physical

OPLS3: A Force Field Providing Broad Coverage of Drug-like Small Molecules and Proteins

Edward Harder et al.

JOURNAL OF CHEMICAL THEORY AND COMPUTATION (2016)

添加到收藏夹

Article Multidisciplinary Sciences

Structure-based discovery of opioid analgesics with reduced side effects

Aashish Manglik et al.

NATURE (2016)

添加到收藏夹

Article Chemistry, Physical

ff14SB: Improving the Accuracy of Protein Side Chain and Backbone Parameters from ff99SB

James A. Maier et al.

JOURNAL OF CHEMICAL THEORY AND COMPUTATION (2015)

添加到收藏夹

Article Medicine, Research & Experimental

Macrophages and β-cells are responsible for CXCR2-mediated neutrophil infiltration of the pancreas during autoimmune diabetes

Julien Diana et al.

EMBO MOLECULAR MEDICINE (2014)

添加到收藏夹

Article Chemistry, Physical

Lipid14: The Amber Lipid Force Field

Callum J. Dickson et al.

JOURNAL OF CHEMICAL THEORY AND COMPUTATION (2014)

添加到收藏夹

Article Biochemical Research Methods

Quantifying the local resolution of cryo-EMEM density maps

Alp Kucukelbir et al.

NATURE METHODS (2014)

添加到收藏夹

Article Biochemical Research Methods

Full-length RNA-seq from single cells using Smart-seq2

Simone Picelli et al.

NATURE PROTOCOLS (2014)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Targeting inflammation in the treatment of type 2 diabetes: time to start

Marc Y. Donath

NATURE REVIEWS DRUG DISCOVERY (2014)

添加到收藏夹

Article Computer Science, Interdisciplinary Applications

SPFP: Speed without compromise-A mixed precision model for GPU accelerated molecular dynamics simulations

Scott Le Grand et al.

COMPUTER PHYSICS COMMUNICATIONS (2013)

添加到收藏夹

Article Chemistry, Physical

PTRAJ and CPPTRAJ: Software for Processing and Analysis of Molecular Dynamics Trajectory Data

Daniel R. Roe et al.

JOURNAL OF CHEMICAL THEORY AND COMPUTATION (2013)

添加到收藏夹

Article Medicine, General & Internal

Interleukin-1 antagonism in type 1 diabetes of recent onset: two multicentre, randomised, double-blind, placebo-controlled trials

Antoinette Moran et al.

LANCET (2013)

添加到收藏夹

Article Biochemistry & Molecular Biology

Pancreatic β Cell Dedifferentiation as a Mechanism of Diabetic β Cell Failure

Chutima Talchai et al.

CELL (2012)

添加到收藏夹

Article Multidisciplinary Sciences

Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human

Atsuhiko Ichimura et al.

NATURE (2012)

添加到收藏夹

Article Chemistry, Medicinal

Assessing the Performance of the MM/PBSA and MM/GBSA Methods. 1. The Accuracy of Binding Free Energy Calculations Based on Molecular Dynamics Simulations

Tingjun Hou et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2011)

添加到收藏夹

Review Immunology

Type 2 diabetes as an inflammatory disease

Marc Y. Donath et al.

NATURE REVIEWS IMMUNOLOGY (2011)

添加到收藏夹

Article Biochemical Research Methods

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

Paul D. Adams et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2010)

添加到收藏夹

Article Multidisciplinary Sciences

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor

Michael P. Bokoch et al.

NATURE (2010)

添加到收藏夹

Article Chemistry, Medicinal

Identifying and Characterizing Binding Sites and Assessing Druggability

Thomas A. Halgren

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2009)

添加到收藏夹

Article Chemistry, Multidisciplinary

Software news and updates - CHARNIM-GUI: A web-based grraphical user interface for CHARMM

Sunhwan Jo et al.

JOURNAL OF COMPUTATIONAL CHEMISTRY (2008)

添加到收藏夹

Article Biochemistry & Molecular Biology

Epik:: a software program for pK a prediction and protonation state generation for drug-like molecules

John C. Shelley et al.

JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN (2007)

添加到收藏夹

Article Biochemistry & Molecular Biology

Identification of 9-hydroxyoctadecadienoic acid and other oxidized free fatty acids as ligands of the G protein-coupled receptor G2A

H Obinata et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2005)

添加到收藏夹

Article Biochemistry & Molecular Biology

Therapeutic effects of lysophosphatidylcholine in experimental sepsis

JJ Yan et al.

NATURE MEDICINE (2004)

添加到收藏夹

Article Chemistry, Multidisciplinary

Development and testing of a general amber force field

JM Wang et al.

JOURNAL OF COMPUTATIONAL CHEMISTRY (2004)

添加到收藏夹

Article Biochemical Research Methods

Coot:: model-building tools for molecular graphics

P Emsley et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2004)

添加到收藏夹

Article Chemistry, Multidisciplinary

UCSF chimera - A visualization system for exploratory research and analysis

EF Pettersen et al.

JOURNAL OF COMPUTATIONAL CHEMISTRY (2004)

添加到收藏夹

Article Biochemistry & Molecular Biology

Accurate determination of local defocus and specimen tilt in electron microscopy

JA Mindell et al.

JOURNAL OF STRUCTURAL BIOLOGY (2003)

添加到收藏夹

Article Biochemistry & Molecular Biology

The lysophospholipid receptor G2A activates a specific combination of G proteins and promotes apoptosis

P Lin et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2003)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.