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Peer-reviewed veterinary case report

Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2007
Authors:
Shrestha, Suja et al.
Affiliation:
Department of Chemistry and Institute of Molecular Cell Biology · South Korea

Abstract

Methylenedisalicylic acid derivatives were synthesized and their inhibitory activities against protein tyrosine phosphatases (PTPases) examined. Two of the compounds, 8 and 9, showed K(i) values of 9.4 and 6.3microM against PTP1B, 4- and 7-fold lower values compared to those against TC-PTP. They were reversible and slow-binding inhibitors against PTP1B. When compound 8 was fed to a mouse model, the weight gain and adipocyte fat storage induced by a high-fat-diet were significantly suppressed.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/17368023/