Small molecules for fat combustion: targeting obesity
| Autor: | Yitao Wang, Jingxin Liu, Ligen Lin |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
SNS
sympathetic nervous system C/EBPα CCAAT/enhancer binding protein α PDEs phosphodiesterases OXPHOS oxidative phosphorylation FGF21 fibroblast growth factor 21 Review Type 2 diabetes Brown adipose tissue Bioinformatics Energy homeostasis CRABP-II cellular RA binding protein type II 0302 clinical medicine HFD high fat diet Weight loss RA retinoic acid RARE RA response element BMP8b bone morphogenetic protein 8b General Pharmacology Toxicology and Pharmaceutics media_common 0303 health sciences SIRT1 silent mating type information regulation 2 homolog 1 PXR pregnane X receptor TFAM mitochondrial transcription factor A WAT white adipose tissue Thermogenesis PPREs peroxisome proliferator response elements FAS fatty acid synthase Thermogenin cAMP cyclic adenosine monophosphate PTP1B protein-tyrosine phosphatase 1B medicine.anatomical_structure BA bile acids 030220 oncology & carcinogenesis VDR vitamin D receptor CRE cAMP response element medicine.symptom PET-CT positron emission tomography combined with computed tomography PRDM16 PR domain containing 16 ATP adenosine triphosphate RXR retinoid X receptor media_common.quotation_subject VDRE VDR response elements AKT protein kinase B 03 medical and health sciences TMEM26 transmembrane protein 26 CLA cis-12 conjugated linoleic acid ERE estrogen response element UCP1 uncoupling protein 1 medicine PGC-1α peroxisome proliferator-activated receptor γ coactivator 1-α Obesity β3-AR β3-adrenergic receptor 030304 developmental biology ERs estrogen receptors LXR liver X receptors PPARs peroxisome proliferator-activated receptors business.industry lcsh:RM1-950 Cidea cell death-inducing DNA fragmentation factor α-like effector A Uncoupling protein 1 Appetite RMR resting metabolic rate medicine.disease Dio2 iodothyronine deiodinase type 2 Beige cells ALDH9 aldehyde dehydrogenase 9 BAT brown adipose tissue AMPK AMP-activated protein kinase lcsh:Therapeutics. Pharmacology RAR RA receptor cGMP cyclic guanosine monophosphate PKA protein kinase A GPCRs G protein-coupled receptors TRPs transient receptor potential cation channels business MAPK mitogen-activated protein kinase |
| Zdroj: | Acta Pharmaceutica Sinica. B Acta Pharmaceutica Sinica B, Vol 9, Iss 2, Pp 220-236 (2019) |
| ISSN: | 2211-3835 |
| DOI: | 10.1016/j.apsb.2018.09.007 |
| Popis: | Obesity is increasing in an alarming rate worldwide, which causes higher risks of some diseases, such as type 2 diabetes, cardiovascular diseases, and cancer. Current therapeutic approaches, either pancreatic lipase inhibitors or appetite suppressors, are generally of limited effectiveness. Brown adipose tissue (BAT) and beige cells dissipate fatty acids as heat to maintain body temperature, termed non-shivering thermogenesis; the activity and mass of BAT and beige cells are negatively correlated with overweight and obesity. The existence of BAT and beige cells in human adults provides an effective weight reduction therapy, a process likely to be amenable to pharmacological intervention. Herein, we combed through the physiology of thermogenesis and the role of BAT and beige cells in combating with obesity. We summarized the thermogenic regulators identified in the past decades, targeting G protein-coupled receptors, transient receptor potential channels, nuclear receptors and miscellaneous pathways. Advances in clinical trials were also presented. The main purpose of this review is to provide a comprehensive and up-to-date knowledge from the biological importance of thermogenesis in energy homeostasis to the representative thermogenic regulators for treating obesity. Thermogenic regulators might have a large potential for further investigations to be developed as lead compounds in fighting obesity. Graphical abstract Brown adipose tissue (BAT) and beige cells dissipates fatty acids as heat, termed non-shivering thermogenesis, which has emerged as a potential therapeutically way to treat obesity. The current review provides a comprehensive and up-to-date of knowledge from the biological importance of thermogenesis to the representative thermogenic regulators for treating obesity.fx1 |
| Databáze: | OpenAIRE |
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