Protein Tyrosine Phosphatase 1B Inhibitors For Diabetes

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A novel role for protein tyrosine phosphatase 1B as a

mation, diabetes, and cancer, are regulated by a delicate balance between protein tyrosine kinases and phosphatases. Protein tyrosine phosphatase 1B (PTP1B, also known as PTPN1) is a major negative regulator of the insulin and leptin signaling pathways [3 5]. Studies from mice with the PTP1B gene deletion have demonstrated that PTP1B

Protein tyrosine phosphatase 1B inhibitors isolated from

Protein tyrosine phosphatase 1B (PTP1B), is an intracellular non-receptor type PTP, which is considered to be a well-validated therapeutic target for many diseases including diabetes. Extensive biochemical and genetic investigations have shown that PTP1B is involved in the negative control of insulin- and leptin-receptor4 6.

Modes of inhibition of human protein-tyrosine phosphatase 1b

Insulin resistance is the main feature of Type 2 diabetes, due to attenuated or diminished signaling from insulin receptors, resulting in hyperglicemia. Inhibition of protein tyrosine phosphatase 1B (PTP1B) has been suggested as an attractive target to improve insulin sensitivity in different cell types.

In vitro effects of cinnamic acid derivatives on protein

Protein Tyrosine Phosphatase 1B (PTP1B) is a major negative regulator of insulin signaling pathways. Finding selective PTP1B inhibitors from natural sources has been widely recognized as a potential drug target for the treatment of diabetes mellitus and obesity. In the present study, we evaluated the inhibitory activity of cinnamic acid derivatives

Protein Tyrosine Phosphatase 1B Inhibition and Glucose Uptake

Protein tyrosine phosphatase 1B and -glucosidase inhibitory activity of the compounds isolated from M. alba. Compounds Protein Tyrosine Phosphatase 1B -Glucosidase IC 50( M) a Inhibition Type b Ki ( M) c IC ( M) a Inhibition Type b Ki ( M) c 1 0.57 0.04 Mixed type 0.70 1.67 0.02 Mixed type 1.2 2 0.80 0.02 Mixed type 1.02 1.31c 0.01 Mixed type 0

TheRoleoftheC-terminalDomainofProteinTyrosine Phosphatase

Protein tyrosine phosphatase 1B (PTP-1B) has been impli- the world have been searching for selective inhibitors for PTP-1B, and most of them target inhibitors to

In Silico Structure-Based Design of a Potent and Selective

Jun 08, 2005 protein tyrosine phosphatases such as PTP-LAR, Calcineurin, and the highly homologous T-Cell Protein Tyrosine Phosphatase (TCPTP). Thus the designed tetrapeptide is a suitable lead compound for the development of new drugs against type 2 diabetes and obesity. Introduction Protein Tyrosine Phosphatase 1B (PTP1B) has recently been receiving consider-

Protein Tyrosine Phosphatase 1B Reduction - Diabetes

Protein tyrosine phosphatase 1B (PTP1B) has been implicated as a negative regulator of insulin action. Overexpression of PTP1B protein has been observed in insulin-resistant states associated with obesity. Mice lacking a functional PTP1B gene exhibit increased insu-lin sensitivity and are resistant to weight gain. To

JOURNALOF NUTRITIONAL SCIENCE - Cambridge

regulator of insulin signalling is protein tyrosine phosphatase 1B (PTP1B) that causes dephosphorylation of activated insulin receptor and induction of insulin resistance. Based on the overwhelming evidence, PTP1B inhibitors are anticipated to become potential therapeutic agents to control T2DM(6,7).

of Type 2 Diabetes Mellitus - MDPI

Mar 02, 2020 tyrosine phosphatase 1B (PTP1B). These natural inhibitors include several classes of compounds such as bromophenols, phlorotannins, sterols, terpenes, stilbenoids, flavonoids, furans, catechols, and fungal metabolites, among others. The structures of some of the natural compounds mentioned across this review are represented in Figure1.

PTP1B Inhibitors for Type 2 Diabetes Treatment

insulin no longer sufficiently triggers sugar removal from the blood. Protein tyrosine phosphatase- 1B (PTP1B) affects regulation of blood sugar, because it dephosphorylates the insulin receptor and reduces its activity. Studying PTP1B can help us understand whether inhibitors of this phosphatase could slow

Structure-based Design of a Low Molecular Weight

Nonpeptide, and Highly Selective Inhibitor of Protein-tyrosine Phosphatase 1B* (Received for publication, November 10, 1999, and in revised form, December 21, 1999) Lars Fogh Iversen,a,b,c Henrik Sune Andersen,b,d Sven Branner,a Steen B. Mortensen,a Gu¨nther H. Peters,e,i Kjeld Norris,f Ole Hvilsted Olsen,g Claus Bekker Jeppesen,h

Decrease of microRNA-122 Causes Hepatic Insulin Resistance by

Protein tyrosine phosphatase (PTP) constitutes a family of phosphatases including PTP1B, SHP1, SHP2, and LAR.3,4 As a negative regulator of insulin signaling cascade, PTP1B functions as a key phospha-tase and reverses tyrosine kinase action.5 A deficiency of PTP1B improved glycemic control by enhancing

Natural PTP1B Inhibitors From Polygonum cuspidatum and Their

strate in the presence and absence of the inhibitors (Figures 2 Figure 2. Lineweaver-Burk plots for the inhibition of compounds (2, 3, 6, and 9) on the protein tyrosine phosphatase 1B-catalyzed hydrolysis

Potent protein tyrosine phosphatase 1B (PTP1B) inhibiting

Protein tyrosine phosphatase 1B (PTP1B) is a key negative regulator of insulin signaling, and mounting evidence has linked PTP1B to insulin resistance, obesity, and type 2 diabetes mellitus (T2DM) (Panzhinskiy et al., 2013). In the insulin-signaling pathway, PTP1B dephosphorylates the insu-lin receptor and the insulin receptor substrate IRS-1

Louise Grant, Kirsty D. Shearer, Alicja Czopek - Diabetes

Diabetes 2014;63:456 470 DOI: 10.2337/db13-0885 Protein tyrosine phosphatase-1B (PTP1B) is a non-receptor tyrosine phosphatase, identified as an attractive drug target for conditions associated with metabolic Institute of Medical Sciences, University of Aberdeen, College of Life Sciences

Journal of Proteomics & Bioinformatics Open Access

Protein Tyrosine Phosphatase 1B (PTP-1B) is one of the important targets in the treatment of diabetes and obesity. They play a very important role in cellular signaling within and between cells. The best pharmacophore hypothesis (Hypo 1), consisting of four features, namely, one hydro-gen-bond acceptor (HBA), one hydrophobic point (HY),

Natural products possessing protein tyrosine phosphatase 1B

Potential pharmaceutical applications of several PTP1B inhibitors were presented. Keywords: natural products; phytochemistry; protein tyrosine phosphatase 1B (PTP1B); inhibitor; structure-activity relationship (SAR); type 2 diabetes; obesity Acta Pharmacologica Sinica (2012) 33: 1217 1245; doi: 10.1038/aps.2012.90; published online 3 Sep 2012

NPC Natural Product Communications Vol. 13 No. 2 A New Tannin

Keywords: Torreya nucifera, Diabetes, Obesity, PTP1B. Protein tyrosine phosphatase 1B (PTP1B), a member of protein tyrosine phosphatases (PTPs), is an enzyme that catalyzes protein tyrosine dephosphorylation. It has been considered as a negative regulator of insulin signaling. Although several PTPs such as PTP-

Evaluation of inhibition of protein tyrosine phosphatase 1B

Protein tyrosine phosphatase 1B (PTP1B) is known to be implicated in insulin resistance, and inhibitors of PTP1B were supposed to be useful to regulate insulin and leptin signalling pathways. In this report, calix[4]arene mono- and bis-α-ketophosphonic acids were tested in vitro as potential inhibitors of PTP1B. New calix[4]arene-based

THE DEVELOPMENT OF THE FIRST GENERATION OF EXO- AFFINITY

Type II Diabetes (T2DB) is one of the worldwide problems characterized by ineffective insulin signal transduction as a result of insulin resistance and impaired glucose homeostasis. Protein Tyrosine Phosphatase 1B (PTP1B), an enzyme in phosphatase family

Leptin resistance following over-expression of protein

increased expression of protein tyrosine phosphatase 1B (PTP1B) in peripheral tissues and whether over-expression of this phosphatase, specifically in liver, could alter the leptin-mediated effects on feeding and glucose metabolism. Obesity was induced in mice through a high-fat diet that resulted in hyperglycemia, hyperinsulinemia and

A novel protein tyrosine phosphatase 1B inhibitor with

Protein tyrosine phosphatase 1B (PTP1B), a member of the protein tyrosine phosphatases (PTPs) family, catalyses the dephosphorylation of the insulin receptor (InsR) that controls insulin signalling activity (Koren and Fantus, 2007). PTP1B knockout mice exhibit increased sensitivity to insulin and resistance to diet-induced T2DM (Elcheblyet al.,

Protein Tyrosine Phosphatase 1B and alpha-Glucosidase

diabetes and associated cardiovascular complications.6) Modulating postprandial hyperglycemia may therefore play a crucial role in the treatment and prevention of approaches have been proposed such as -glucosidase inhibitors to delay the digestion and absorption of carbohydrates,7) and protein tyrosine phosphatase 1B phorylation.

PTP1B Inhibitors as Potential Target for Type II Diabetes

and promotes insulin signaling. Protein tyrosine phosphatase 1B (PTP1B) is a negative regulator of IR signaling and is responsible for dephosphorylating the tyrosine phosphorylated IR. Inhibition of PTP1B could thus promote glucose uptake [1]. Early PTP1B inhibitors, such as charged active site-directed analogs, showed poor cell membrane

Protein tyrosine phosphatase 1B inhibitors from natural sources

from tyrosine phosphorylated proteins. These enzymes play an important role in cell growth regulation, prolifer-ation, and transformation. Among the PTPs family, Pro-tein-tyrosine phosphatase 1B (PTP1B) is a classical enzyme, also called protein tyrosine phosphatase non-re-ceptor type 1 (Barrett et al. 1999). It is widely expressed in

Journal of Chemical and Pharmaceutical Research, 2017, 9(11):46

and SHP-2. Among these, PTP1B has been most intensively studied as a target for the development of inhibitors aiming at the treatment of type 2 diabetes and obesity. Protein tyrosine Phosphatase 1B (PTP1B) is a negative regulator of insulin signal transduction by dephosphorylation of tyrosine residue in regulatory domain of β-subunit

The Role of Protein Tyrosine Phosphatase (PTP)-1B in

and diabetes. Several studies identified protein tyrosine phosphatase (PTP)-1B, a member of the PTP superfamily, as a major negative regulator for insulin receptor signaling and a novel molecular player in endothelial dysfunction and cardiovascular disease. Unlike other anti-diabetic approaches,

Protein tyrosine phosphatase-1B contributes to LPS-induced

Feb 24, 2014 Leptin signaling pathways are largely regulated by protein tyrosine phosphatases (PTP) via dephosphorylation of the phosphotyrosine residues on LepRb or other downstream sig-naling molecules (46). Tyrosine phosphatase-1B (PTP1B) binds to and dephosphorylates JAK-2 (25, 33, 52). Several reports demonstrated a crucial role of this protein in the

Type 2 diabetes mellitus and protein-tyrosine phosphatase 1b

Citation: Sun J, Qu C, Wang Y, et al. Type 2 diabetes mellitus and protein-tyrosine phosphatase 1b. J Diabetes Metab Disord Control. 2016;3(8):180‒183. DOI: 10.15406/jdmdc.2016.03.00096 The role of PTP1B in insulin signaling of type 2 diabetes mellitus The pathogenesis of type 2 diabetes are associated with gene

RESEARCH ARTICLE Open Access Evaluation of 147 Kampo

Background: Protein tyrosine phosphatase (PTP) 1B, a negative regulator of the insulin and leptin signaling pathways, is currently considered a promising target for the development of novel therapeutic approaches used to treat insulin-resistant type 2 diabetes mellitus (IR-T2DM). In this study, we examined the PTP1B inhibitory activity of

Role of Protein Tyrosine Phosphatase-1B Inhibitors in Type 2

inhibition of Protein-tyrosine phosphatase 1B. Hence, Protein-tyrosine phosphatase 1B inhibition could be a new therapeutic option for treatment of patients with at risk type 2 diabetes mellitus and obesity. Keywords: Type 2 diabetes, Obesity, Insulin, Leptin, Protein-tyrosine phosphatase 1B ISSN: 2231 3788 (Print) 2321 4376 (Online) 2 Review

Molecular Docking and High-Throughput Screening for Novel

inhibitors for the enzyme protein tyrosine phosphatase-1B (PTP1B), a tyrosine phosphatase that has been implicated as a key target for type II diabetes. A corporate library of approximately 400 000 compounds was screened using high-throughput experimental tech-niques for compounds that inhibited PTP1B. Concurrently, molecular docking was used

The Mechanism of Allosteric Inhibition of Protein Tyrosine

As the prototypical member of the PTP family, protein tyrosine phosphatase 1B (PTP1B) is an attractive target for therapeutic interventions in type 2 diabetes. The extremely conserved catalytic site of PTP1B renders the design of selective PTP1B inhibitors intractable.

Inhibitory activity of fractions of Senna nigricans toward

a potential source for the discovery of lead compounds as PTP 1B and DPP IV inhibitors to treat type 2 diabetes mellitus. Key words: Protein tyrosine phosphatase, dipeptidyl peptidase, inhibitors, Senna nigricans. INTRODUCTION Diabetes mellitus is a metabolic disorder which is due to a defect in insulin secretion, insulin action, or both. A

A Review on Structure Based Drug Design of Protein Tyrosine

receptor, including autophosphorylaton of tyrosine (Tyr) residues in the insu-lin-receptor activation loop. This leads to recruitment of insulin receptor A Review on Structure Based Drug Design of Protein Tyrosine Phosphatase 1B Inhibitors for Target for obesity and Type 2 Diabetes Mellitus

Human protein tyrosine phosphatase 1B inhibitors: QSAR by

Protein tyrosine phosphatase 1B (PTP 1B), a negative regulator of insulin receptor signaling system, has emerged as a highly validated, attractive target for the treatment of non-insulin dependent diabetes mellitus (NIDDM) and obesity. As a result there is a growing interest in the development of potent and specific inhibitors for this enzyme.

RESEARCH Open Access Suggestion of suitable animal models for

studies of protein tyrosine phosphatase 1b (PTP1B) inhibitors using computational approaches Xuan Thi-Anh Nguyen1 and Ly Le1,2* Abstract PTP1B is a prototypic enzyme of the superfamily protein tyrosine phosphatases (PTPs) which are critical regulators of tyrosine phosphorylation-dependent signaling events.