Complex pharmacology of free fatty acid receptors

G Milligan, B Shimpukade, T Ulven… - Chemical …, 2017 - ACS Publications
G protein-coupled receptors (GPCRs) are historically the most successful family of drug
targets. In recent times it has become clear that the pharmacology of these receptors is far …

Targeting lipid GPCRs to treat type 2 diabetes mellitus—Progress and challenges

J Ghislain, V Poitout - Nature Reviews Endocrinology, 2021 - nature.com
Therapeutic approaches to the treatment of type 2 diabetes mellitus that are designed to
increase insulin secretion either directly target β-cells or indirectly target gastrointestinal …

[HTML][HTML] Single-cell transcriptome profiling of human pancreatic islets in health and type 2 diabetes

Å Segerstolpe, A Palasantza, P Eliasson… - Cell metabolism, 2016 - cell.com
Hormone-secreting cells within pancreatic islets of Langerhans play important roles in
metabolic homeostasis and disease. However, their transcriptional characterization is still …

[HTML][HTML] Systematic single-cell analysis provides new insights into heterogeneity and plasticity of the pancreas

S Tritschler, FJ Theis, H Lickert, A Böttcher - Molecular Metabolism, 2017 - Elsevier
Background Diabetes mellitus is characterized by loss or dysfunction of insulin-producing β-
cells in the pancreas, resulting in failure of blood glucose regulation and devastating …

Eicosapentaenoic acid potentiates brown thermogenesis through FFAR4-dependent up-regulation of miR-30b and miR-378

J Kim, M Okla, A Erickson, T Carr, SK Natarajan… - Journal of biological …, 2016 - ASBMB
Emerging evidence suggests that n-3 polyunsaturated fatty acids (PUFA) promote brown
adipose tissue thermogenesis. However, the underlying mechanisms remain elusive. Here …

Fatty acid-stimulated insulin secretion vs. lipotoxicity

P Ježek, M Jabůrek, B Holendová, L Plecitá-Hlavatá - Molecules, 2018 - mdpi.com
Fatty acid (FA)-stimulated insulin secretion (FASIS) is reviewed here in contrast to type 2
diabetes etiology, resulting from FA overload, oxidative stress, intermediate …

Functions of omega-3 fatty acids and FFA4 (GPR120) in macrophages

DS Im - European Journal of pharmacology, 2016 - Elsevier
Omega-3 polyunsaturated fatty acids (n-3 PUFAs), which are plentiful in fish oil, have been
known for decades to be beneficial functional nutrients in different disease states. GPR120 …

Platelet‐derived lipids promote insulin secretion of pancreatic β cells

T Karwen, K Kolczynska‐Matysiak, C Gross… - EMBO Molecular …, 2023 - embopress.org
Hyperreactive platelets are commonly observed in diabetic patients indicating a potential
link between glucose homeostasis and platelet reactivity. This raises the possibility that …

Mechanistic insights into cardiovascular protection for omega-3 fatty acids and their bioactive lipid metabolites

TD O'Connell, RP Mason, MJ Budoff… - European Heart …, 2020 - academic.oup.com
Patients with well-controlled low-density lipoprotein cholesterol levels, but persistent high
triglycerides, remain at increased risk for cardiovascular events as evidenced by multiple …

Free fatty acid receptors as new potential therapeutic target in inflammatory bowel diseases

A Bartoszek, E Von Moo, A Binienda, A Fabisiak… - Pharmacological …, 2020 - Elsevier
Abstract Family of Free Fatty Acid Receptors (FFARs), specific G protein-coupled receptors
comprises of four members: FFAR1-4, where each responds to different chain length of fatty …