Small-molecule inhibitor: alogliptin

Name

Peptidases inhibited: Alogliptin is a potent (IC₅₀ < 10 nM) inhibitor of DPP-4 with greater than 10,000-fold selectivity over dipeptidyl-peptidase 8 and dipeptidyl-peptidase 9 (Feng et al., 2007).
Pharmaceutical relevance: The potential of alogliptin in the treatment of type 2 diabetes has been reviewed by Argyrakopoulou & Doupis (2009).
DrugBank: 618588

CID at PubChem: 16658243
Structure
Chemical/biochemical name: 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile; 2,2,2-trifluoroacetic acid

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).