PMID- 25748601
OWN - NLM
STAT- MEDLINE
DCOM- 20160209
LR  - 20150410
IS  - 1879-0712 (Electronic)
IS  - 0014-2999 (Linking)
VI  - 755
DP  - 2015 May 15
TI  - A step ahead of PPARgamma full agonists to PPARgamma partial agonists: therapeutic 
      perspectives in the management of diabetic insulin resistance.
PG  - 50-7
LID - S0014-2999(15)00162-4 [pii]
LID - 10.1016/j.ejphar.2015.02.043 [doi]
AB  - 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 
      PPARalpha and PPARgamma, respectively. The PPARgamma 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 PPARgamma 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, 
      PPARgamma 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 PPARgamma partial agonists with enhanced 
      therapeutic efficacy and reduced adverse effects. This review sheds lights on the 
      current status of development of PPARgamma partial agonists, for the management of 
      T2DM, having comparatively less or no adverse effects to that of PPARgamma full 
      agonists.
CI  - Copyright (c) 2015 Elsevier B.V. All rights reserved.
FAU - Chigurupati, Sridevi
AU  - Chigurupati S
AD  - Pharmaceutical Chemistry Unit, Faculty of Pharmacy, AIMST University, Semeling, 
      08100 Bedong, Malaysia.
FAU - Dhanaraj, Sokkalingam A
AU  - Dhanaraj SA
AD  - Pharmaceutical Technology Unit, Faculty of Pharmacy, AIMST University, Semeling, 
      08100 Bedong, Malaysia.
FAU - Balakumar, Pitchai
AU  - Balakumar P
AD  - Pharmacology Unit, Faculty of Pharmacy, AIMST University, Semeling, 08100 Bedong, 
      Kedah Darul Aman, Malaysia. Electronic address: pbala2006@gmail.com.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20150305
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (PPAR gamma)
SB  - IM
MH  - Animals
MH  - Diabetes Mellitus, Type 2/*drug therapy
MH  - Humans
MH  - Hypoglycemic Agents/*therapeutic use
MH  - *Insulin Resistance
MH  - PPAR gamma/*agonists
OTO - NOTNLM
OT  - Adverse effects
OT  - Cardiovascular events
OT  - Diabetes mellitus
OT  - PPARgamma full agonists
OT  - PPARgamma partial agonists
EDAT- 2015/03/10 06:00
MHDA- 2016/02/10 06:00
CRDT- 2015/03/10 06:00
PHST- 2014/12/19 00:00 [received]
PHST- 2015/02/25 00:00 [revised]
PHST- 2015/02/25 00:00 [accepted]
PHST- 2015/03/10 06:00 [entrez]
PHST- 2015/03/10 06:00 [pubmed]
PHST- 2016/02/10 06:00 [medline]
AID - S0014-2999(15)00162-4 [pii]
AID - 10.1016/j.ejphar.2015.02.043 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 2015 May 15;755:50-7. doi: 10.1016/j.ejphar.2015.02.043. Epub 
      2015 Mar 5.