PTEN targeting: the search for novel insulin sensitisers provides new insight into obesity research

Béguinot, Francesco

doi:10.1007/s00125-006-0547-2

Cited by 4 publications

(3 citation statements)

References 18 publications

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“…Such compounds include inhibitors of protein tyrosine phosphatases (PTPs), such as PTP‐1B, and inhibitors of signaling intermediates such as the protein kinase C (PKC) isoform PKC‐theta, which normally exerts a negative feedback by phosphorylating serine residues on the insulin receptor beta‐subunit and on IRS‐1 . An antisense oligonucleotide that inhibits the phosphatase PTEN and increases signaling downstream of PIP3 has improved insulin sensitivity and glycemic control in insulin‐resistant animal models …”

Section: Future Diabetes Therapiesmentioning

confidence: 99%

“…38,40 An antisense oligonucleotide that inhibits the phos-phatase PTEN and increases signaling downstream of PIP3 has improved insulin sensitivity and glycemic control in insulinresistant animal models. 41 Agents that potentiate postreceptor signaling steps have shown promise to increase insulin action but have not proceeded in development. For example, an analog of chiro-inositol (pinitol) enhances signaling of phosphoinositide-3-kinase (PI3K) and improves muscle glucose uptake and reduces hyperglycemia in diabetic animal models and T2DM patients.…”

Section: Increasing Insulin Actionmentioning

confidence: 99%

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The Current Drug Treatment Landscape for Diabetes and Perspectives for the Future

Bailey

2015

Clin Pharma and Therapeutics

106

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The escalating global epidemic of type 2 diabetes mellitus has focused attention on the devastating consequences of protracted hyperglycemia. Early and effective intervention to control blood glucose is a fundamental principle of treatment guidelines, requiring assiduous use of current therapies. However, many patients do not achieve or maintain glycemic targets, emphasizing the need for further therapies. This narrative review assesses the available medicinal options to address hyperglycemia and the opportunities to develop novel agents.

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Section: Future Diabetes Therapiesmentioning

confidence: 99%

Section: Increasing Insulin Actionmentioning

confidence: 99%

The Current Drug Treatment Landscape for Diabetes and Perspectives for the Future

Bailey

2015

Clin Pharma and Therapeutics

106

View full text Add to dashboard Cite

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“…63 However, there is concern that substantial disruption of PTEN could lead to tumour formation. 64 SH2-inositol phosphatases (SHIP-1 and SHIP-2) dephosphorylate PIP3 in the 5' position to form phosphatidylinositol 3,4-bisphosphate. Partial disruption of the SHIP-2 gene in mice improves insulin sensitivity, 65 making this a further putative target to enhance the effectiveness of PI3K.…”

Section: Protein Phosphatase Pten and Inositol Phosphatasesmentioning

confidence: 99%

Treating insulin resistance: future prospects

Bailey

2007

Diabetes and Vascular Disease Research

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Insulin resistance typically reflects multiple defects of insulin receptor and post-receptor signalling that impair a diverse range of metabolic and vascular actions. Many potential intervention targets and compounds with therapeutic activity have been described. Proof of principle for a non-peptide insulin mimetic has been demonstrated by specific activation of the intracellular B-subunit of the insulin receptor. Potentiation of insulin action has been achieved with agents that enhance phosphorylation and prolong the tyrosine kinase activity of the insulin receptor and its protein substrates after activation by insulin. These include inhibitors of phosphatases and serine kinases that normally prevent or terminate tyrosine kinase signalling. Additional approaches involve increasing the activity of phosphatidylinositol 3-kinase and other downstream components of the insulin signalling pathways. Experimental interventions to remove signalling defects caused by cytokines, certain adipocyte hormones, excess fatty acids, glucotoxicity and negative feedback by distal signalling steps have also indicated therapeutic possibilities. Several hormones, metabolic enzymes, minerals, co-factors and transcription co-activators have shown insulin-sensitising potential. Since insulin resistance affects many metabolic and cardiovascular diseases, it provides an opportunity for simultaneous therapeutic attack on a broad front.

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New drugs for the treatment of diabetes mellitus

Bailey

2015

International Textbook of Diabetes Mellitus

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PTEN targeting: the search for novel insulin sensitisers provides new insight into obesity research

Cited by 4 publications

References 18 publications

The Current Drug Treatment Landscape for Diabetes and Perspectives for the Future

The Current Drug Treatment Landscape for Diabetes and Perspectives for the Future

Treating insulin resistance: future prospects

New drugs for the treatment of diabetes mellitus

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