DA-1229, a novel and potent DPP4 inhibitor, improves insulin resistance and delays the onset of diabetes.

  title={DA-1229, a novel and potent DPP4 inhibitor, improves insulin resistance and delays the onset of diabetes.},
  author={Mi-kyung Kim and Yu Na Chae and Ha Dong Kim and Eun Kyoung Yang and Eun Jung Cho and Song-hyen Choi and Ye-Hwang Cheong and Hae Sun Kim and Heung Jae Kim and Yeong Woo Jo and Moon Ho Son and Soon-Hoe Kim and Chang-Yell Shin},
  journal={Life sciences},
  volume={90 1-2},

Figures from this paper

DA-1229, a dipeptidyl peptidase IV inhibitor, protects against renal injury by preventing podocyte damage in an animal model of progressive renal injury
It is suggested that activation of DPPIV in the kidney has a role in the progression of renal disease, and that DA-1229 may exert its renoprotective effects by preventing podocyte injury.
Hepatic role in an early glucose-lowering effect by a novel dipeptidyl peptidase 4 inhibitor, evogliptin, in a rodent model of type 2 diabetes.
Hypoglycemic effect and mechanism of isoquercitrin as an inhibitor of dipeptidyl peptidase-4 in type 2 diabetic mice
The findings demonstrated the hypoglycemic effects of isoquercitrin and indicated that isoquERCitrin improved insulin sensitivity by targeting DPP-IV.
Critical Role of Dipeptidyl Peptidase IV: A Therapeutic Target for Diabetes and Cancer.
In comparison to early oral hypoglycemic, DPP-IV inhibitors are well tolerated and provide a better glycemic control over a longer period, which is important in maintaining glucose homeostasis.
Beneficial Effects of Evogliptin, a Novel Dipeptidyl Peptidase 4 Inhibitor, on Adiposity with Increased Ppargc1a in White Adipose Tissue in Obese Mice
It is demonstrated for the first time that pharmacological DPP4 inhibition by evogliptin directly causes fat loss in established obese mice, providing insight into the regulation of energy storage in WAT caused by DPP 4 inhibition.
A Novel Dipeptidyl Peptidase-4 Inhibitor DA-1229 Ameliorates Tubulointerstitial Fibrosis in Cyclosporine Nephrotoxicity in Mice
The results suggest that DPP-4 inhibition by DA-1229 provides renoprotective effects in an animal model of cyclosporine nephrotoxicity via antioxidant, anti-inflammatory, and anti-fibrotic mechanisms.
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?
The biological functions and potential substrates of DPPIV enzymes are reviewed and the characteristics of the DPP IV inhibitors are discussed in view of type 2 diabetes and further therapeutic interest.
Gemigliptin ameliorates Western-diet-induced metabolic syndrome in mice.
Gemigliptin ameliorated WD-induced hepatic inflammation and fibrosis through suppression of oxidative stress and suggest that DPP-4 inhibitors may represent promising therapeutic agents for metabolic syndrome beyond their current role as antihyperglycemic agents.
Effects of Dipeptidyl Peptidase-4 Inhibition with MK-0431 on Syngeneic Mouse Islet Transplantation
The results indicate posttransplant DPP-4 inhibition with MK-0431 in the diabetic recipient with a marginal number of islets is not beneficial to transplantation outcome or islet grafts.


A novel dipeptidyl peptidase IV inhibitor DA-1229 ameliorates streptozotocin-induced diabetes by increasing β-cell replication and neogenesis.
Enteroinsular axis of db/db mice and efficacy of dipeptidyl peptidase IV inhibition.
The results suggest that DPPIV inhibition is a suitable approach for treatment of impaired glucose tolerance (IGT), and type 2 diabetes in the early stage, and the progression of insulin resistance appeared to block the improvement of glucose tolerance through DPPiv inhibition.
Acute and Chronic Effects of the Incretin Enhancer Vildagliptin in Insulin-Resistant Rats
  • B. Burkey, X. Li, P. Wang
  • Medicine, Biology
    Journal of Pharmacology and Experimental Therapeutics
  • 2005
The enzyme dipeptidyl peptidase-IV (DPP-4) inactivates the incretin hormone glucagon-like peptide-1 (GLP-1). Because GLP-1 has therapeutic effects in patients with type 2 diabetes, but its potential
Differential Antidiabetic Efficacy of Incretin Agonists Versus DPP-4 Inhibition in High Fat–Fed Mice
Although none of the therapies increased β-cell mass, only Ex-4–treated mice exhibited increased pancreatic mRNA transcripts for Irs2, Egfr, and Gck, highlighting significant differences between pharmacological administration of incretin receptor agonists and potentiation of endogenous GLP-1 and GIP via DPP-4 inhibition.
Dipeptidyl peptidase inhibitors as new drugs for the treatment of type 2 diabetes
Based on their mode of action, DPP-IV inhibitors seem to be of particular value in early forms of type 2 diabetes, either alone or in combination with other types of oral agents.
Interrelationship of dipeptidyl peptidase IV (DPP4) with the development of diabetes, dyslipidaemia and nephropathy: a streptozotocin-induced model using wild-type and DPP4-deficient rats.
Plasma DPP4 activity increased after STZ treatment, positively correlating to blood glucose, and may be responsible for hyperglycaemia, lipid metabolism and preservation of renal function.
Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9.
Assessment of selectivity of potential clinical candidates may be important to an optimal safety profile for this new class of antihyperglycemic agents, according to the results of toxicity and tolerability studies.
Chronic inhibition of circulating dipeptidyl peptidase IV by FE 999011 delays the occurrence of diabetes in male zucker diabetic fatty rats.
It is demonstrated that DPP-IV inhibitors such as FE 999011 could be of clinical value to delay the progression from impaired glucose tolerance to type 2 diabetes.