Inhibiting DPP-4 to treat AML

Inhibiting the membrane-bound extracellular peptidase DPP-4, which is targeted by multiple marketed diabetes therapies, could help treat AML by inducing tumor cell apoptosis.

A phenotypic screen of >1,200 cell surface protein-targeting compounds with clinical utility identified the DPP4 inhibitor Tradjenta linagliptin as a suppressor of growth in human and mouse AML cell lines, and subsequent experiments showed Tradjenta and another DPP4 inhibitor Galvus vildagliptin decreased human AML cell growth via apoptosis with IC50s of 223.1 nM and 1,084.8 nM, respectively. ...