A novel fluorescent probe for in vitro and in vivo imaging of dipeptidyl peptidase-4 (DPP-4) was designed and synthesized. This probe is successfully utilized to screen DPP-4 inhibitors in living 3T3-L1 cells and zebrafish, which provides a novel approach for the discovery of anti-diabetes drugs.

Type 1 diabetes (T1D) and latent autoimmune in adults (LADA) represent the most common types of are characterized by different age onset, degrees immune-mediated destruction pancreatic beta cells rates disease progression towards insulin dependence. Several immunotherapies aimed to counteract responses against preserve beta-cell function currently being investigated, particularly T1D. Prelimina...

Hepatocyte nuclear factor 1 was identified as the transcription factor binding to a 20 bp (®150 to ®131) region of the gene for human dipeptidyl peptidase IV, which has been shown to be important for the expression of dipeptidyl peptidase IV in the human intestinal and hepatic epithelial cell lines Caco-2 and HepG2. Functional analysis of the hepatocyte nuclear factor 1 site was performed with ...

A microvillar fraction was prepared from human kidney cortex. This fraction was seven to 10 times enriched in aminopeptidases N and A, gamma-glutamyltransferase, dipeptidyl peptidase IV, neutral endopeptidase and alkaline phosphatase. Dipeptidyl peptidase IV activity of human renal microvilli could be inhibited by di-isopropylphosphorofluoridate and neutral endopeptidase activity by phosphorami...

A novel molecular scaffold has been synthesized, and its synthesis and incorporation into new analogues of biologically active molecules will be discussed. A comparison of the inhibitory activity of these compounds to the known type-2 diabetes compound (sitagliptin) against dipeptidyl peptidase-4 (DPP-4) will be shown.

Dipeptidyl peptidase-4 inhibitors (DPP-4Is) inhibit the inactivation of incretin hormones while also affecting the immune system, since CD26/DPP-4 is involved in immune regulation. The current study shows that the use of DPP-4Is as therapy for type 2 diabetes patients may induce joint symptoms with decrease in plasma SDF-1α level.