ArticleBritish journal of pharmacology2016
A novel protein tyrosine phosphatase 1B inhibitor with therapeutic potential for insulin resistance.
Article in British journal of pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 31 citations in OpenAlex.
- Article
- Watercress-derived glucosinolates as potential allosteric PTP1B inhibitors: a dual in silico and in vitro study on insulin signaling modulation.BMC chemistry · 2025Article
- Antidiabetic Effect of StandardizedJournal of pharmacopuncture · 2023Article
- CX08005, a Protein Tyrosine Phosphatase 1B Inhibitor, Attenuated Hepatic Lipid Accumulation and Microcirculation Dysfunction Associated with Nonalcoholic Fatty Liver Disease.Pharmaceuticals (Basel, Switzerland) · 2023Article
- The Antidiabetic Activities of Neocryptotanshinone: Screened by Molecular Docking and Related to the Modulation of PTP1B.Nutrients · 2022Article
- Potential Therapeutic Target Protein Tyrosine Phosphatase-1B for Modulation of Insulin Resistance with Polyphenols and Its Quantitative Structure-Activity Relationship.Molecules (Basel, Switzerland) · 2022Article
- CYC31, A Natural Bromophenol PTP1B Inhibitor, Activates Insulin Signaling and Improves Long Chain-Fatty Acid Oxidation in C2C12 Myotubes.Marine drugs · 2020Article
- Exploration the Mechanism of Doxorubicin-Induced Heart Failure in Rats by Integration of Proteomics and Metabolomics Data.Frontiers in pharmacology · 2020Article
- Estradiol Protects Neuropeptide Y/Agouti-Related Peptide Neurons against Insulin Resistance in Females.Neuroendocrinology · 2020Article
- Article
- Beneficial effects of murtilla extract and madecassic acid on insulin sensitivity and endothelial function in a model of diet-induced obesity.Scientific reports · 2019Article
- Gene Expression of Protein Tyrosine Phosphatase 1B and Endoplasmic Reticulum Stress During Septic Shock.Frontiers in medicine · 2019Article
- Selectivity, cell permeability and oral availability studies of novel bromophenol derivative HPN as protein tyrosine phosphatase 1B inhibitor.British journal of pharmacology · 2018Article
- A novel protein tyrosine phosphatase 1B inhibitor with therapeutic potential for insulin resistance.British journal of pharmacology · 2016Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeInsulin-sensitizing drugs are currently limited, and identifying new candidates is a challenge. Protein tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signalling, and its inhibition is anticipated to improve insulin resistance. Here, the pharmacological properties of CX08005, a novel PTP1B inhibitor, were investigated. EXPERIMENTAL APPROACH: Recombinant hPTP1B protein was used to study enzyme activity and mode of inhibition. Docking simulation explored the interactions between CX08005 and PTP1B. Insulin sensitivity was evaluated by glucose tolerance test (GTT) in diet-induced obese (DIO) and KKAy mice; glucose-stimulated insulin secretion (GSIS), homeostasis model assessment of insulin resistance index (HOMA-IR) and whole-body insulin sensitivity (ISWB ) were also determined. A hyperinsulinaemic-euglycaemic clamp was performed to evaluate insulin-stimulated glucose disposal in both whole-body and insulin-sensitive tissues. Furthermore, CX08005's effects on muscle, fat and liver cells were determined in vitro. KEY
resultsCX08005 competitively inhibited PTP1B by binding to the catalytic P-loop through hydrogen bonds. In DIO mice, CX08005 ameliorated glucose intolerance dose-dependently (50-200 mg·kg(-1) ·day(-1) ) and decreased the HOMA-IR. In KKAy mice, CX08005 (50 mg·kg(-1) ·day(-1) ) improved glucose intolerance, GSIS, ISWB and hyperglycaemia. CX08005 also enhanced insulin-stimulated glucose disposal, increased glucose infusion rate and glucose uptake in muscle and fat in DIO mice (hyperinsulinaemic-euglycaemic clamp test). CX08005 enhanced insulin-induced glucose uptake in 3T3-L1 adipocytes and C2C12 myotubes, and increased phosphorylation of IRβ/IRS1 and downstream molecules in hepatocytes in a dose- and insulin-dependent manner respectively. CONCLUSIONS AND IMPLICATIONS: Our results strongly suggest that CX08005 directly enhances insulin action in vitro and in vivo through competitive inhibition of PTP1B.
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