A step ahead of PPARγ full agonists to PPARγ partial agonists: therapeutic perspectives in the management of diabetic insulin resistance

European Journal of Pharmacology
Sridevi ChigurupatiPitchai Balakumar

Abstract

Described since long as a member of the nuclear receptor superfamily, peroxisome proliferator-activated receptors (PPARs) regulate the gene expression of proteins involved in glucose and lipid metabolism. PPARs indeed regulate several physiologic processes, including lipid homeostasis, adipogenesis, inflammation, and wound healing. PPARs bind natural or synthetic PPAR ligands can function as cellular sensors to regulate the gene transcription. Dyslipidemia, and type 2 diabetes mellitus (T2DM) with insulin resistance are treated using agonists of PPARα and PPARγ, respectively. The PPARγ is a key regulator of insulin sensitization and glucose metabolism, and therefore is considered as an imperative pharmacological target to combat diabetic metabolic disease and insulin resistance. Of note, currently available PPARγ full agonists like rosiglitazone display serious adverse effects such as fluid retention/oedema, weight gain, and increased incidence of cardiovascular events. On the other hand, PPARγ partial agonists are being suggested to devoid or having less incidence of these undesirable events, and are under developmental stages. Current research is on the way for the development of novel PPARγ partial agonists with enhanced the...Continue Reading

References

Oct 24, 2006·Diabetes Research and Clinical Practice·Helen D BerlieLinda A Jaber
Sep 13, 2007·JAMA : the Journal of the American Medical Association·Sonal SinghCurt D Furberg
Apr 30, 2008·Archives of Internal Medicine·Christian MeierChristoph R Meier
Aug 4, 2009·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Pitchai BalakumarManjeet Singh
Aug 20, 2009·BMJ : British Medical Journal·David N JuurlinkMuhammad M Mamdani
Jun 26, 2010·Pharmacotherapy·Daniel M Riche, S Travis King
Oct 28, 2010·Diabetes, Obesity & Metabolism·G Schernthaner, R J Chilton
Jul 28, 2011·British Journal of Pharmacology·Pitchai Balakumar, Nanjaian Mahadevan
Apr 10, 2012·European Journal of Pharmacology·Sumit ChaudharyChandrashekhar Devidas Upasani
Jun 27, 2012·Nature Reviews. Urology·Melanie Clyne
Aug 11, 2012·Journal of the National Cancer Institute·Ronac MamtaniJames D Lewis
Sep 5, 2012·Diabetologia·H M ColhounUNKNOWN Scottish Diabetes Research Network Epidemiology Group
Jan 5, 2013·Journal of Medicinal Chemistry·Jens C de GrootKonrad Büssow
Jan 9, 2013·Bioorganic & Medicinal Chemistry·Joshua P TaygerlyMotonao Nakamura
Feb 26, 2013·Journal of Chemical Information and Modeling·Irene KouskoumvekakiKarsten Kristiansen
Jul 3, 2013·Biochimica Et Biophysica Acta·Atanas G AtanasovElke H Heiss
Oct 5, 2013·Tumour Biology : the Journal of the International Society for Oncodevelopmental Biology and Medicine·Shiyao HeYe Zhang
Aug 2, 2014·Biochemical Pharmacology·Limei WangAtanas G Atanasov

❮ Previous
Next ❯

Citations

Jan 15, 2019·Current Molecular Pharmacology·Pitchai BalakumarRamanathan Sambathkumar
Dec 7, 2018·Chemical & Pharmaceutical Bulletin·Ko MorishitaHiroaki Shirahase
Feb 8, 2020·Journal of Cellular and Molecular Medicine·Liwei WuJianye Wu
Jun 9, 2020·Expert Opinion on Pharmacotherapy·Sabina Antonela AntoniuIleana Antohe
Aug 11, 2015·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Fan XieFujiang Guo
Feb 10, 2016·Alcoholism, Clinical and Experimental Research·Yuri A BlednovR Adron Harris
Oct 30, 2020·Diabetes, Metabolic Syndrome and Obesity : Targets and Therapy·Muluken Altaye AyzaDerbew Fikadu Berhe
Aug 4, 2021·Brain, Behavior, and Immunity·Lindsay R MeredithLara A Ray
Aug 30, 2021·European Journal of Medicinal Chemistry·Zheng LiLuyong Zhang

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cardiovascular Disease Pathophysiology

Cardiovascular disease involves several different processes that contribute to the pathological mechanism, including hyperglycemia, inflammation, atherosclerosis, hypertension and more. Vasculature stability plays a critical role in the development of the disease. Discover the latest research on cardiovascular disease pathophysiology here.

Asprosin

Asprosin is a fasting-induced hormone produced in the white adipose tissue to stimulate the hepatic release of glucose into the bloodstream. Discover the latest research on this protein hormone here.

CV Disorders & Type 2 Diabetes

This feed focuses on the association of cardiovascular diseases in patients with type 2 diabetes.

Biomarkers for Type 2 Diabetes

Biomarkers can help understand chronic diseases and assist in risk prediction for prevention and early detection of diseases. Here is the latest research on biomarkers in type 2 diabetes, a disease in which the body is unable to produce or properly use insulin.

Cardiovascular Inflammation

Inflammation plays a significant role in the development of cardiovascular diseases, an understanding of these endogenous processes is critical for evaluating the risks and potential treatment strategies. Discover the latest research on cardiovascular inflammation here.

Cardiovascular Diseases: Risk Factors

Cardiovascular disease is a significant health concern. Risk factors include hypertension, obesity, dyslipidemia and smoking. Women who are postmenopausal are at an increased risk of heart disease. Here is the latest research for risk factors of cardiovascular disease.

Cardiovascular Disorder in Diabetes

Diabetes is associated with an increased risk of cardiovascular disorders and heart failure. Discover the latest research here.

Cardiomegaly

Cardiomegaly, known as an enlarged heart, is a multifactorial disease with different pathophysiological mechanisms. Hypertension, pregnancy, exercise-induced and idiopathic causes are some mechanisms of cardiomegaly. Discover the latest research of cardiomegaly here.