alexa 4-((1E)-2-(5-(4-hydroxy-3-methoxystyryl-)-1-phenyl-1H-p
ISSN: 2155-9562

Journal of Neurology & Neurophysiology
Open Access

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Research Article

4-((1E)-2-(5-(4-hydroxy-3-methoxystyryl-)-1-phenyl-1H-pyrazoyl-3- yl) vinyl)-2-methoxy-phenol) (CNB-001) Does Not Regulate Human Recombinant Protein-Tyrosine Phosphatase1B (PTP1B) Activity in vitro

Paul A Lapchak1,2*, Jacqueline A Lara1 and Paul D Boitano1

1Department of Neurology, Cedars-Sinai Medical Center, Advanced Health Sciences Pavilion, Los Angeles, USA

2Department of Neurosurgery, Cedars-Sinai Medical Center, Advanced Health Sciences Pavilion, Los Angeles, USA

Corresponding Author:
Paul A Lapchak
Director of Translational Research
Cedars-Sinai Medical Center Professor
Department of Neurology and Neurosurgery
Advanced Health Sciences Pavilion
Suite 8305, 127 S. San Vicente Blvd, Los Angeles, USA
Tel: 310-248-8188
Fax: 310-248-7568
E-mail: [email protected]

Received date: August 18, 2014; Accepted dat: September 22, 2014; Published date: September 29, 2014

Citation: Lapchak PA, Lara JA, Boitano PD (2014) 4-((1E)-2-(5-(4-hydroxy-3- methoxystyryl-)-1-phenyl-1H-pyrazoyl-3-yl) vinyl)-2-methoxy-phenol) (CNB-001) Does Not Regulate Human Recombinant Protein-Tyrosine Phosphatase1B (PTP1B) Activity in vitro. J Neurol Neurophysiol 5:232. doi:10.4172/2155-9562.1000232

Copyright: © 2014 Lapchak PA, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

 

Abstract

Protein-Tyrosine Phosphatase1B (PTP1B) is a negative regulator of the insulin signaling pathway and is a
potential therapeutic target for treatment of type 2 diabetes, cardiovascular disease, metabolic syndrome and cancer.
It has been postulated that CNB-001 [4-((1E)-2-(5-(4-hydroxy-3-methoxystyryl-)-1-phenyl-1H-pyrazoyl-3-yl) vinyl)-2-
methoxy-phenol)] may regulate PTP1B activity suggested by a computer-based active site docking recognition model.
This possibility was studied using a human recombinant PTP1B assay, and a phospho-peptide fragment of the insulin
receptor β subunit domain (IR5). The positive control, suramin, inhibited PTP1B with an IC50 (half minimal (50%)
inhibitory concentration) value of 16.34 μM; CNB-001 did not affect enzyme activity across the range of 1nM-0.1mM.
This study suggests that PTP1B inhibition is not involved in the beneficial effects of CNB-001 in obese type 2 diabetic
mice.

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