title: Evidence for antifibrotic incretin-independent effects of the DPP-4 inhibitor linagliptin.
abstract: Among gliptins, linagliptin is unique, because decreased glomerular filtration rate does not require dose reduction. Linagliptin was originally developed to lower blood glucose by inhibiting dipeptidyl peptidase-4 (DPP-4). However, DPP-4 has numerous additional substrates, and thus gliptins possess a vast range of additional off-target effects. Shi et al. report that linagliptin directly targets interaction of DPP-4 with integrin β1, preventing endothelial-mesenchymal transition and ultimately renal fibrosis, providing additional rationale for use of linagliptin in diabetic nephropathy.
authors: Department of Nephrology and Rheumatology, University Medical Center Göttingen, Georg August University, Göttingen, Germany.
authors: Michael
authors: M
authors: Zeisberg
authors: Department of Cardiology and Pneumology, University Medical Center Göttingen, Georg August University, Göttingen, Germany.
authors: Elisabeth M
authors: EM
authors: Zeisberg
mesh_terms: D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000201:enzymology*; D003928:Diabetic Nephropathies / Q000201:enzymology*; D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism*; D042783:Endothelial Cells / Q000201:enzymology*; D058750:Epithelial-Mesenchymal Transition; D019012:Integrin beta1 / Q000378:metabolism*; D007668:Kidney / Q000201:enzymology*; D008297:Male
chemical_list: D019012:Integrin beta1; D018819:Dipeptidyl Peptidase 4