PMID- 23627940
OWN - NLM
STAT- MEDLINE
DCOM- 20140501
LR  - 20190823
IS  - 1875-533X (Electronic)
IS  - 0929-8673 (Linking)
VI  - 20
IP  - 21
DP  - 2013
TI  - Pharmacological inhibition of protein tyrosine phosphatase 1B: a promising 
      strategy for the treatment of obesity and type 2 diabetes mellitus.
PG  - 2609-25
AB  - Obesity and metabolic syndrome represent major public health problems, and are 
      the biggest preventable causes of death worldwide. Obesity is the leading risk 
      factor for type 2 diabetes mellitus (T2DM), cardiovascular diseases and 
      non-alcoholic fatty liver disease. Obesity-associated insulin resistance, which 
      is characterized by reduced uptake and utilization of glucose in muscle, adipose 
      and liver tissues, is a key predictor of metabolic syndrome and T2DM. With 
      increasing prevalence of obesity in adults and children, the need to identify and 
      characterize potential targets for treating metabolic syndrome is imminent. 
      Emerging evidence from animal models, clinical studies and cell lines studies 
      suggest that protein tyrosine phosphatase 1B (PTP1B), an enzyme that negatively 
      regulates insulin signaling, is likely to be involved in the pathways leading to 
      insulin resistance. PTP1B is tethered to the cytosolic surface of endoplasmic 
      reticulum (ER), an organelle that is responsible for folding, modification, and 
      trafficking of proteins. Recent evidence links the disruption of ER homeostasis, 
      referred to as ER stress, to the pathogenesis of obesity and T2DM. PTP1B has been 
      recognized as an important player linking ER stress and insulin resistance in 
      obese subjects. This review highlights recent advances in the research related to 
      the role of PTP1B in signal transduction processes implicated in pathophysiology 
      of obesity and type 2 diabetes, and focuses on the potential therapeutic 
      exploitation of PTP1B inhibitors for the management of these conditions.
FAU - Panzhinskiy, E
AU  - Panzhinskiy E
AD  - Division of Pharmaceutical Sciences, College of Health Sciences & the Center for 
      Cardiovascular Research and Alternative Medicine, University of Wyoming College 
      of Health Sciences, Laramie, WY 82071, USA.
FAU - Ren, J
AU  - Ren J
FAU - Nair, S
AU  - Nair S
LA  - eng
GR  - 5P20RR016474-12/RR/NCRR NIH HHS/United States
GR  - 8 P20 GM103432-12/GM/NIGMS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Review
PL  - United Arab Emirates
TA  - Curr Med Chem
JT  - Current medicinal chemistry
JID - 9440157
RN  - 0 (Anti-Obesity Agents)
RN  - 0 (Antihypertensive Agents)
RN  - 0 (Enzyme Inhibitors)
RN  - EC 3.1.3.48 (Protein Tyrosine Phosphatase, Non-Receptor Type 1)
SB  - IM
MH  - Animals
MH  - Anti-Obesity Agents/chemistry/*pharmacology
MH  - Antihypertensive Agents/chemistry/*pharmacology
MH  - Diabetes Mellitus, Type 2/*drug therapy/enzymology
MH  - Dose-Response Relationship, Drug
MH  - Enzyme Inhibitors/chemistry/*pharmacology
MH  - Humans
MH  - Obesity/*drug therapy/enzymology
MH  - Protein Tyrosine Phosphatase, Non-Receptor Type 1/*antagonists & 
      inhibitors/metabolism
MH  - Structure-Activity Relationship
EDAT- 2013/05/01 06:00
MHDA- 2014/05/03 06:00
CRDT- 2013/05/01 06:00
PHST- 2012/12/31 00:00 [received]
PHST- 2013/02/27 00:00 [revised]
PHST- 2013/04/08 00:00 [accepted]
PHST- 2013/05/01 06:00 [entrez]
PHST- 2013/05/01 06:00 [pubmed]
PHST- 2014/05/03 06:00 [medline]
AID - CMC-EPUB-20130418-7 [pii]
AID - 10.2174/0929867311320210001 [doi]
PST - ppublish
SO  - Curr Med Chem. 2013;20(21):2609-25. doi: 10.2174/0929867311320210001.