2 ms·
Nice find! Looks like they are exploring it for its copper chelating properties, specifically for use with Wilson's Disease (where copper accumulates). The stu
by matznerd 8y ago
Nice find! Looks like they are exploring it for its copper chelating properties, specifically for use with Wilson's Disease (where copper accumulates).
The study you link further addresses the issue with a molecule being "undruggable" because it is not orally bioavailable:
"One of the major challenges faced by PTP1B-based drug discovery efforts has been to generate orally bioavailable inhibitors of the phosphatase. In fact, the lack of oral bioavailability of active site-directed PTP inhibitors was a major factor in industry describing these enzymes as “undruggable.” Our efforts with this class of allosteric inhibitors now provide proof of concept that these challenges associated with active site-directed inhibitors of PTP1B can be overcome...The combination of PTP1B inhibition and copper chelation presented in DPM-1001 reflects a new approach to the treatment of diabetes and obesity that we hope will re-invigorate drug development efforts in this area."
To me, it looks like they will still not utilize the full potential of the drug. But whatever can get DPM-1001 into production, I am for. (Group buy/synthesis anyone? ;)) It looks like their secondary observations of regeneration/restoration might be closer to the true potential for this molecule:
"In studying mice, DPM-1001 reduced liver complications, including enlarged cell size, irregular shape and arrangement in liver tissue."
https://www.cshl.edu/progress-toward-improved-wilsons-disease-drug/ https://www.cshl.edu/progress-toward-improved-wilsons-diseas...