2021
DOI: 10.1016/j.ijbiomac.2021.04.061
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Pyrazoles as novel protein tyrosine phosphatase 1B (PTP1B) inhibitors: An in vitro and in silico study

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Cited by 20 publications
(18 citation statements)
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“…[ 6 ]. PTP-1B is a distinctive enzyme that plays a substantial part in insulin signaling pathways that are implicated in type 2 diabetes and associated metabolic disorders as a negative regulator [ 7 ]. This functions by showing improvement in insulin resistance and normalizing insulin and plasma glucose levels without triggering hypoglycemia.…”
Section: Introductionmentioning
confidence: 99%
“…[ 6 ]. PTP-1B is a distinctive enzyme that plays a substantial part in insulin signaling pathways that are implicated in type 2 diabetes and associated metabolic disorders as a negative regulator [ 7 ]. This functions by showing improvement in insulin resistance and normalizing insulin and plasma glucose levels without triggering hypoglycemia.…”
Section: Introductionmentioning
confidence: 99%
“…Following the consideration of results from the in silico evaluation, orientin had the highest negative binding energy value post-MD simulation and was selected for the in vitro analysis. The inhibitory activity of orientin was determined by the hydrolysis of p-NPP to p-nitrophenol (p-NP), using the method of Rocha et al [34] with modifications. Twenty microliters PTP1B (0.2 units/ml) was added to the wells of the 96 well microtiter plate and diluted with a PTP1B reaction buffer containing 50 mM citrate (pH of 6), 0.1 M sodium chloride, 1 mM EDTA, and 1 mM of dithiothreitol (DTT).…”
Section: Methodsmentioning
confidence: 99%
“…This suggests that orientin could either directly bind to the free PTP1B at a site close to its active site or bind to the PTP1B-substrate complex, the consequence of which the overall reaction rate will decrease, and the product will be produced at a slower rate. In contrast, ursolic acid has been reported to be a noncompetitive inhibitor by Rocha et al [34]. Contradictorily, Ha et al [66] reported ursolic acid to exhibit competitive inhibition against PTP1B.…”
Section: In Vitro Evaluationmentioning
confidence: 98%
“…Protein-tyrosine phosphatise 1B (PTP1B) is a protein involved in the insulin signalling pathway and a negative regulator in metabolic disorders [ 33 ].…”
Section: Molecular Targets Involved In Diabetes Mellitusmentioning
confidence: 99%