PTP1B inhibitors for type 2 diabetes treatment: a patent review (2011 – 2014)

Tamrakar, Akhilesh K.; Maurya, Chandan Kumar; Amit, K.

doi:10.1517/13543776.2014.947268

Cited by 111 publications

(58 citation statements)

References 98 publications

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“…Considering that PTP1B directly dephosphorylates insulin receptors and the receptor substrate, thereby negatively regulating the insulin signaling pathway, it may also have a direct effect on its downstream pathways by affecting the activity or expression of insulin signal transduction molecules to inhibit insulin signal transduction, leading to insulin resistance [36,37]. We expected CPOP to be useful in the treatment of type II diabetes [38].…”

Section: Resultsmentioning

confidence: 99%

Anti-Diabetic Effect of Portulaca oleracea L. Polysaccharideandits Mechanism in Diabetic Rats

Bai

Zang²,

et al. 2016

IJMS

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Diabetes mellitus (DM) is a metabolic syndrome caused by multiple genetic and environmental factors. Traditional Chinese medicine preparations have shown a comprehensive and function-regulating characteristic. Purslane (Portulaca oleracea L.) is an annual succulent herb. Currently, there have been some related reports on the treatment of diabetes with purslane. The current study was designed to separate and purify the polysaccharide, a systematic study of its physical and chemical properties, antioxidant activity, and anti-diabetic mechanism, in order to provide a theoretical basis for the development of drugs of purslane. A crude water soluble polysaccharide extracted from purslane was named CPOP (crude Portulaca oleracea L. polysaccharide). Effects of CPOP on bodyweight, glucose tolerance test (GTT), fasting blood glucose (FBG), fasting serum insulin (FINS), insulin sensitivity index (ISI), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), methane dicarboxylic aldehyde (MDA), and superoxygen dehydrogenises (SOD) were investigated. The results indicate that the oral administration of CPOP could significantly increase the body weight and significantly improve the glucose tolerance in diabetic rats. Meanwhile, CPOP could significantly reduce the FBG level, and elevate the FINS level and ISI value in diabetic rats. In addition, CPOP could significantly reduce TNF-α and IL-6 levels in diabetic rats; CPOP could also reduce MDA and SOD activities in the liver tissue of diabetic rats. These results suggest that the anti-diabetic effect of CPOP may be associated with its antioxidant and anti-inflammatory effects.

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Section: Resultsmentioning

confidence: 99%

Anti-Diabetic Effect of Portulaca oleracea L. Polysaccharideandits Mechanism in Diabetic Rats

Bai

Zang²,

et al. 2016

IJMS

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“…5 For this reason, PTP1B has received attention over the last few years as a novel therapeutic target for the treatment of diabetes and obesity, and as such there are numerous inhibitors against PTP1B at various stages of development. 6 …”

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confidence: 99%

Inhibition of PTP1B disrupts cell–cell adhesion and induces anoikis in breast epithelial cells

et al. 2017

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Protein tyrosine phosphatase 1B (PTP1B) is a well-known inhibitor of insulin signaling pathways and inhibitors against PTP1B are being developed as promising drug candidates for treatment of obesity. PTP1B has also been linked to breast cancer both as a tumor suppressor and as an oncogene. Furthermore, PTP1B has been shown to be a regulator of cell adhesion and migration in normal and cancer cells. In this study, we analyzed the PTP1B expression in normal breast tissue, primary breast cells and the breast epithelial cell line D492. In normal breast tissue and primary breast cells, PTP1B is widely expressed in both epithelial and stromal cells, with highest expression in myoepithelial cells and fibroblasts. PTP1B is widely expressed in branching structures generated by D492 when cultured in 3D reconstituted basement membrane (3D rBM). Inhibition of PTP1B in D492 and another mammary epithelial cell line HMLE resulted in reduced cell proliferation and induction of anoikis. These changes were seen when cells were cultured both in monolayer and in 3D rBM. PTP1B inhibition affected cell attachment, expression of cell adhesion proteins and actin polymerization. Moreover, epithelial to mesenchymal transition (EMT) sensitized cells to PTP1B inhibition. A mesenchymal sublines of D492 and HMLE (D492M and HMLEmes) were more sensitive to PTP1B inhibition than D492 and HMLE. Reversion of D492M to an epithelial state using miR-200c-141 restored resistance to detachment induced by PTP1B inhibition. In conclusion, we have shown that PTP1B is widely expressed in the human breast gland with highest expression in myoepithelial cells and fibroblasts. Inhibition of PTP1B in D492 and HMLE affects cell–cell adhesion and induces anoikis-like effects. Finally, cells with an EMT phenotype are more sensitive to PTP1B inhibitors making PTP1B a potential candidate for further studies as a target for drug development in cancer involving the EMT phenotype.

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“…effects (Tamrakar et al, 2014). The representative compound is MSI-1436 (Trodusquemine) which can suppress appetite and causes fat-specific weight loss in diet-induced obese mice and it is in phase I trial (Scott et al, 2010).…”

Section: Discussionmentioning

confidence: 99%

Structure and biosynthesis of fumosorinone, a new protein tyrosine phosphatase 1B inhibitor firstly isolated from the entomogenous fungus Isaria fumosorosea

Liu

Zhang

Chen

et al. 2015

Fungal Genetics and Biology

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PTP1B inhibitors for type 2 diabetes treatment: a patent review (2011 – 2014)

Cited by 111 publications

References 98 publications

Anti-Diabetic Effect of Portulaca oleracea L. Polysaccharideandits Mechanism in Diabetic Rats

Anti-Diabetic Effect of Portulaca oleracea L. Polysaccharideandits Mechanism in Diabetic Rats

Inhibition of PTP1B disrupts cell–cell adhesion and induces anoikis in breast epithelial cells

Structure and biosynthesis of fumosorinone, a new protein tyrosine phosphatase 1B inhibitor firstly isolated from the entomogenous fungus Isaria fumosorosea

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