Small-molecule inhibitor: linagliptin

Name

History: The development of linagliptin was described by Eckhardt et al. (2007).
Peptidases inhibited: Dipeptidyl-peptidase IV is inhibited with IC₅₀ = 1 nM (Eckhardt et al., 2007). There is little Inhibition of dipeptidyl-peptidase 8 or dipeptidyl-peptidase 9 (Deacon & Holst, 2010).
Mechanism: Inhibition is reversible.

CID at PubChem: 10096344
Structure
Chemical/biochemical name: 8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
Formula weight: 473

Inhibitor class: This compound is one of the "gliptins" that are inhibitors of dipeptidyl-peptidase IV, and have been developed for potential use as drugs in the treatment of type 2 diabetes. These compounds suppress the degradation of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide by dipeptidyl-peptidase IV. This helps to correct the defective insulin and glucagon secretion characteristic of this form of diabetes by stimulating insulin secretion and suppressing glucagon release (Chahal & Chowdhury, 2007; Thornberry & Gallwitz, 2009).