Inhibition of a Protein Tyrosine Phosphatase Using Mesoporous Oxides†

Kapoor, S. ; Girish, T. S. ; Mandal, S. S. ; Gopal, B. ; Bhattacharyya, A. J. (2010) Inhibition of a Protein Tyrosine Phosphatase Using Mesoporous Oxides† The Journal of Physical Chemistry B, 114 (9). pp. 3117-3121. ISSN 1520-6106

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Official URL: http://doi.org/10.1021/jp910166h

Related URL: http://dx.doi.org/10.1021/jp910166h

Abstract

The feasibility of utilizing mesoporous matrices of alumina and silica for the inhibition of enzymatic activity is presented here. These studies were performed on a protein tyrosine phosphatase by the name chick retinal tyrosine phosphotase-2 (CRYP-2), a protein that is identical in sequence to the human glomerular epithelial protein-1 and involved in hepatic carcinoma. The inhibition of CRYP-2 is of tremendous therapeutic importance. Inhibition of catalytic activity was examined using the sustained delivery of p-nitrocatechol sulfate (pNCS) from bare and amine functionalized mesoporous silica (MCM-48) and mesoporous alumina (Al2O3). Among the various mesoporous matrices employed, amine functionalized MCM-48 exhibited the best release of pNCS and also inhibition of CRYP-2. The maximum speed of reaction vmax (=160 ± 10 μmol/mnt/mg) and inhibition constant Ki (=85.0 ± 5.0 μmol) estimated using a competitive inhibition model were found to be very similar to inhibition activities of protein tyrosine phosphatases using other methods.

Item Type:Article
Source:Copyright of this article belongs to American Chemical Society.
ID Code:116869
Deposited On:09 Apr 2021 09:41
Last Modified:09 Apr 2021 09:41

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