[HTML][HTML] A potent, selective, and orally bioavailable inhibitor of the protein-tyrosine phosphatase PTP1B improves insulin and leptin signaling in animal models
The protein-tyrosine phosphatase PTP1B is a negative regulator of insulin and leptin
signaling and a highly validated therapeutic target for diabetes and obesity. Conventional
approaches to drug development have produced potent and specific PTP1B inhibitors, but
these inhibitors lack oral bioavailability, which limits their potential for drug development.
Here, we report that DPM-1001, an analog of the specific PTP1B inhibitor trodusquemine
(MSI-1436), is a potent, specific, and orally bioavailable inhibitor of PTP1B. DPM-1001 also …
signaling and a highly validated therapeutic target for diabetes and obesity. Conventional
approaches to drug development have produced potent and specific PTP1B inhibitors, but
these inhibitors lack oral bioavailability, which limits their potential for drug development.
Here, we report that DPM-1001, an analog of the specific PTP1B inhibitor trodusquemine
(MSI-1436), is a potent, specific, and orally bioavailable inhibitor of PTP1B. DPM-1001 also …