Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site

2007 ◽  
Vol 17 (6) ◽  
pp. 1765-1768 ◽  
Author(s):  
Scott M. Sheehan ◽  
Hans-Juergen Mest ◽  
Brian M. Watson ◽  
Valentine J. Klimkowski ◽  
David E. Timm ◽  
...  
Keyword(s):  
Conformational Change ◽  
Active Site ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Dipeptidyl Peptidase Iv Inhibitors

A comparative study of the binding modes of recently launched dipeptidyl peptidase IV inhibitors in the active site

2013 ◽  
Vol 434 (2) ◽  
pp. 191-196 ◽  
Author(s):  
Mika Nabeno ◽  
Fumihiko Akahoshi ◽  
Hiroyuki Kishida ◽  
Ikuko Miyaguchi ◽  
Yoshihito Tanaka ◽  
...  
Keyword(s):  
Comparative Study ◽  
Active Site ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Binding Modes ◽  
Dipeptidyl Peptidase Iv Inhibitors

CoMFA and CoMSIA of diverse pyrrolidine analogues as dipeptidyl peptidase IV inhibitors: active site requirements

2010 ◽  
Vol 15 (2) ◽  
pp. 457-466 ◽  
Author(s):  
Vanangamudi Murugesan ◽  
Nidhi Sethi ◽  
Yenamandra S. Prabhakar ◽  
Seturam B. Katti
Keyword(s):  
Active Site ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Dipeptidyl Peptidase Iv Inhibitors

Dipeptidyl Peptidase IV Inhibitors for Nonalcoholic Fatty Liver Disease – Systematic Review and Metanalysis

2020 ◽  
Vol 16 ◽  
Author(s):  
Lucas Ribeiro dos Santos ◽  
Marcio Luis Duarte ◽  
Maria Stella Peccin ◽  
Antônio Ricardo de Toledo Gagliardi ◽  
Tamara Melnik
Keyword(s):  
Hepatic Steatosis ◽  
Grey Literature ◽  
Specific Treatment ◽  
Reducing Power ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Cochrane Library ◽  
Vast Number ◽  
Dpp Iv ◽  
Dipeptidyl Peptidase Iv Inhibitors

Introduction:: Hepatic steatosis is a frequent condition, that afflicts, especially, obese and insulin resistant patients; diagnosis is made, usually, through imaging tests. Despite the high prevalence and risk of complications, there is no specific treatment approved, though a vast number of medications have been tested. Objective:: To determine the efficacy of dipeptidyl peptidase IV inhibitors (i DPP-IV) in the treatment of NAFLD. Methods:: We searched the electronic databases of the Cochrane Library, MEDLINE, EMBASE and LILACS, as well as reference lists of the included studies and grey literature; 9 studies were selected for inclusion. Results:: 7 studies were used for metanalysis, for 3 outcomes. i DPP-IV showed an ALT-reducing power of MD -10.83 [95% CI 35.23 to 13.57] at 3 months and MD -9.27 [95% CI 10.92 to -7.62] at 6 months of intervention, as well as reduction of hepatic steatosis via MRI of SMD 0.10 [95% CI 0.31 to 0.50]; the overall incidence of adverse events was very low. The studies were considered of low and very low quality by the GRADE evaluation. Conclusion:: Because of the poor overall quality of the studies and heterogeneity of the population analyzed, i DPP-IV did not show efficacy on inflammatory markers or fibrosis in patients with NAFLD.

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