PMID- 18054739
OWN - NLM
STAT- MEDLINE
DCOM- 20080226
LR  - 20240109
IS  - 1521-690X (Print)
IS  - 1521-690X (Linking)
VI  - 21
IP  - 4
DP  - 2007 Dec
TI  - Inhibition of the protein tyrosine phosphatase PTP1B: potential therapy for 
      obesity, insulin resistance and type-2 diabetes mellitus.
PG  - 621-40
AB  - The global epidemic of obesity and type-2 diabetes mellitus (T2DM) has 
      highlighted the need for new therapeutic approaches. The association of insulin 
      resistance with these disorders and the knowledge that insulin receptor signaling 
      is mediated by tyrosine (Tyr) phosphorylation have generated great interest in 
      the regulation of the balance between Tyr phosphorylation and dephosphorylation. 
      Several protein Tyr phosphatases (PTPs) have been implicated in the regulation of 
      insulin action, with the most convincing data for PTP1B. Murine models targeting 
      PTP1B, PTP1B(-/-)mice, demonstrate enhanced insulin sensitivity without the 
      weight gain seen with other insulin sensitizers such as peroxisome 
      proliferator-activated receptor gamma (PPARgamma) agonists, probably due to a 
      second action of PTP1B as a negative regulator of leptin signaling. Despite 
      intensive efforts and recent progress, a safe, selective and efficacious PTP1B 
      inhibitor has yet to be identified.
FAU - Koren, Shlomit
AU  - Koren S
AD  - Department of Medicine and The Banting and Best Diabetes Centre, Toronto General 
      Research Institute, University Health Network, University of Toronto, Toronto, 
      Ontario, Canada.
FAU - Fantus, I George
AU  - Fantus IG
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
PL  - Netherlands
TA  - Best Pract Res Clin Endocrinol Metab
JT  - Best practice & research. Clinical endocrinology & metabolism
JID - 101120682
RN  - 0 (Insulin)
RN  - 0 (Leptin)
RN  - EC 2.7.10.1 (Receptor, Insulin)
RN  - EC 3.1.3.48 (Protein Tyrosine Phosphatase, Non-Receptor Type 1)
RN  - EC 3.1.3.48 (Protein Tyrosine Phosphatase, Non-Receptor Type 11)
RN  - EC 3.1.3.48 (Protein Tyrosine Phosphatase, Non-Receptor Type 2)
RN  - EC 3.1.3.48 (Receptor-Like Protein Tyrosine Phosphatases, Class 2)
SB  - IM
MH  - Animals
MH  - Diabetes Mellitus, Type 2/*drug therapy/genetics
MH  - Drug Design
MH  - Humans
MH  - Insulin/*physiology
MH  - *Insulin Resistance/genetics
MH  - Leptin/physiology
MH  - Obesity/*drug therapy/genetics
MH  - Protein Tyrosine Phosphatase, Non-Receptor Type 1/*antagonists & inhibitors
MH  - Protein Tyrosine Phosphatase, Non-Receptor Type 11/physiology
MH  - Protein Tyrosine Phosphatase, Non-Receptor Type 2/physiology
MH  - Receptor, Insulin/drug effects
MH  - Receptor-Like Protein Tyrosine Phosphatases, Class 2/physiology
MH  - Signal Transduction/drug effects
MH  - Structure-Activity Relationship
MH  - Substrate Specificity
RF  - 107
EDAT- 2007/12/07 09:00
MHDA- 2008/02/27 09:00
CRDT- 2007/12/07 09:00
PHST- 2007/12/07 09:00 [pubmed]
PHST- 2008/02/27 09:00 [medline]
PHST- 2007/12/07 09:00 [entrez]
AID - S1521-690X(07)00081-4 [pii]
AID - 10.1016/j.beem.2007.08.004 [doi]
PST - ppublish
SO  - Best Pract Res Clin Endocrinol Metab. 2007 Dec;21(4):621-40. doi: 
      10.1016/j.beem.2007.08.004.