Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin.
Dipeptidyl peptidase-IV (DPP-IV) is an enzyme responsible for the inactivation of the glucoregulatory incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). In this report, we show that the hypolipidemic agent atorvastatin is a competitive inhibitor of porcine DPP-IV in vitro, with K(i)=57.8+/-2.3 microM. These results may have implications in the development of novel DPP-IV inhibitors based on the use of atorvastatin as a lead compound for the treatment of type 2 diabetes.
Taldone
Tony
T
Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John's University, Jamaica, NY 11439, USA.
Zito
S William
SW
Talele
Tanaji T
TT
D000069059:Atorvastatin; D020134:Catalytic Domain; D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors; D006538:Heptanoic Acids / Q000737:chemistry / Q000494:pharmacology*; D006860:Hydrogen Bonding; D006868:Hydrolysis; D008958:Models, Molecular; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*
D054873:Dipeptidyl-Peptidase IV Inhibitors; D006538:Heptanoic Acids; D011480:Protease Inhibitors; D011758:Pyrroles; D000069059:Atorvastatin; D018819:Dipeptidyl Peptidase 4