Abstract
Inhibiting the Inhibitors, PTP1B as a Therapeutic Target in Myocardial Infarction
Highlights
Protein kinase activities are regulated at multiple levels from transcription e.g. mRNA stability and splicing, to translational control and protein turnover through degradation
Pharmacological inhibition using a small molecule inhibitor of protein-tyrosine phosphatase 1B (PTP1B), trodusquemine (MSI-1436) has been tested over the last 10 years in completed Phase I trials for obesity and diabetes and in breast cancer (NCT02524951)
A small-scale (n=92) Phase II trial in diabetes is complete in which inhibition of PTP1Bwas achieved by downregulation using antisense technology (IONISPTP-1BRx, Ionis Pharmaceuticals, https://clinicaltrials.gov/ ID NCT01918865)
Summary
Protein kinase activities are regulated at multiple levels from transcription e.g. mRNA stability and splicing, to translational control and protein turnover through degradation.
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