D-420720, A novel orally active sulfonamide compound dipeptidyl peptidase IV inhibitor: structure and activity relationship of arylsulfonamide to dipeptidyl peptidase IV inhibition

2008 ◽  
Vol 69 (8) ◽  
pp. 514-519 ◽  
Author(s):  
Henry J. Tsai ◽  
Shan-Yen Chou ◽  
Shih-Hsien Chuang ◽  
Chien-Cheng Chen ◽  
Feng-Lin Hsu
Keyword(s):  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Activity Relationship ◽  
Dipeptidyl Peptidase Iv Inhibition ◽  
Relationship Of ◽  
Orally Active ◽  
Structure And Activity ◽  
Sulfonamide Compound

Discovery and Preclinical Profile of Saxagliptin (BMS-477118):  A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

2005 ◽  
Vol 48 (15) ◽  
pp. 5025-5037 ◽  
Author(s):  
David J. Augeri ◽  
Jeffrey A. Robl ◽  
David A. Betebenner ◽  
David R. Magnin ◽  
Ashish Khanna ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Long Acting ◽  
Orally Active

scholarly journals Dipeptidyl peptidases 8 and 9: specificity and molecular characterization compared with dipeptidyl peptidase IV

2006 ◽  
Vol 396 (2) ◽  
pp. 391-399 ◽  
Author(s):  
Jais R. Bjelke ◽  
Jesper Christensen ◽  
Per F. Nielsen ◽  
Sven Branner ◽  
Anders B. Kanstrup ◽  
...  
Keyword(s):  
Peptide Yy ◽  
Expression System ◽  
Baculovirus Expression System ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Dipeptidyl Peptidases ◽  
Glucagon Like Peptide ◽  
Glucagon Like Peptide 1 ◽  
Dipeptidyl Peptidase Iv Inhibition

Dipeptidyl peptidases 8 and 9 have been identified as gene members of the S9b family of dipeptidyl peptidases. In the present paper, we report the characterization of recombinant dipeptidyl peptidases 8 and 9 using the baculovirus expression system. We have found that only the full-length variants of the two proteins can be expressed as active peptidases, which are 882 and 892 amino acids in length for dipeptidyl peptidase 8 and 9 respectively. We show further that the purified proteins are active dimers and that they show similar Michaelis–Menten kinetics and substrate specificity. Both cleave the peptide hormones glucagon-like peptide-1, glucagon-like peptide-2, neuropeptide Y and peptide YY with marked kinetic differences compared with dipeptidyl peptidase IV. Inhibition of dipeptidyl peptidases IV, 8 and 9 using the well-known dipeptidyl peptidase IV inhibitor valine pyrrolidide resulted in similar Ki values, indicating that this inhibitor is non-selective for any of the three dipeptidyl peptidases.

scholarly journals Dipeptidyl Peptidase IV Inhibition Activates CREB and Improves Islet Vascularization through VEGF-A/VEGFR-2 Signaling Pathway

PLoS ONE ◽  
2013 ◽  
Vol 8 (12) ◽  
pp. e82639 ◽  
Author(s):  
Balaji Samikannu ◽  
Chunguang Chen ◽  
Neelam Lingwal ◽  
Manju Padmasekar ◽  
Felix B. Engel ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Dipeptidyl Peptidase Iv Inhibition

Synthesis and structure–activity relationship of novel RXR antagonists: Orally active anti-diabetic and anti-obesity agents

2007 ◽  
Vol 17 (17) ◽  
pp. 4804-4807 ◽  
Author(s):  
Junichi Sakaki ◽  
Masashi Kishida ◽  
Kazuhide Konishi ◽  
Hiroki Gunji ◽  
Atsushi Toyao ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of ◽  
Orally Active
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