Discovery of an Orally Active and Long‐Acting DPP‐IV Inhibitor through Property‐Based Optimization with an in Silico Biotransformation Prediction Tool

ChemMedChem ◽  
2020 ◽  
Vol 15 (16) ◽  
pp. 1608-1617
Author(s):  
Shaogao Zeng ◽  
Wenyuan Dou ◽  
Manna Li ◽  
Yang Zhou ◽  
Jiehuang Guo ◽  
...  
Keyword(s):  
In Silico ◽  
Prediction Tool ◽  
Dpp Iv ◽  
Long Acting ◽  
Orally Active

DPP-IV-resistant, long-acting oxyntomodulin derivatives

2011 ◽  
Vol 17 (4) ◽  
pp. 270-280 ◽  
Author(s):  
Alessia Santoprete ◽  
Elena Capitò ◽  
Paul E. Carrington ◽  
Alessandro Pocai ◽  
Marco Finotto ◽  
...  
Keyword(s):  
Dpp Iv ◽  
Long Acting

Prunus amygdalus extract exert antidiabetic effect via inhibition of DPP-IV: in-silico and in-vivo approaches

2020 ◽  
pp. 1-15
Author(s):  
Vikas Kumar ◽  
Richa Sachan ◽  
Mahfoozur Rahman ◽  
Kalicharan Sharma ◽  
Fahad A. Al-Abbasi ◽  
...  
Keyword(s):  
In Silico ◽  
Prunus Amygdalus ◽  
Antidiabetic Effect ◽  
Dpp Iv

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

Combining Hit Identification Strategies: Fragment-Based and in Silico Approaches to Orally Active 2-Aminothieno[2,3-d]pyrimidine Inhibitors of the Hsp90 Molecular Chaperone

2009 ◽  
Vol 52 (15) ◽  
pp. 4794-4809 ◽  
Author(s):  
Paul A. Brough ◽  
Xavier Barril ◽  
Jenifer Borgognoni ◽  
Patrick Chene ◽  
Nicholas G. M. Davies ◽  
...  
Keyword(s):  
Molecular Chaperone ◽  
In Silico ◽  
Hit Identification ◽  
Orally Active

Novel Selective Orally Active CRTH2 Antagonists for Allergic Inflammation Developed from in Silico Derived Hits

2006 ◽  
Vol 49 (23) ◽  
pp. 6638-6641 ◽  
Author(s):  
Trond Ulven ◽  
Jean-Marie Receveur ◽  
Marie Grimstrup ◽  
Øystein Rist ◽  
Thomas M. Frimurer ◽  
...  
Keyword(s):  
In Silico ◽  
Allergic Inflammation ◽  
Orally Active

scholarly journals A Study on the Inhibitory Potential of Dpp-Iv Enzyme by Lobeline through In silico and In vivo Approaches

2021 ◽  
pp. 79-91
Author(s):  
Ghalia Sabbagh ◽  
Boushra Kurdi ◽  
Warid Khayata ◽  
Raghda Lahdo
Keyword(s):  
In Silico ◽  
Inhibitory Effect ◽  
Pharmaceutical Chemistry ◽  
Antidiabetic Activity ◽  
Control Group ◽  
P Value ◽  
Diabetic Mice ◽  
Synthetic Compound ◽  
Dpp Iv

Aims: To evaluate the inhibitory activity of Lobeline natural alkaloid against dipeptidyl peptidase IV (DPP IV) enzyme by in silico and in vivo experiments. Study Design: Evaluation of Antidiabetic Activity of Lobeline alkaloid. Place and Duration of Study: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Aleppo University, Aleppo, Syria, between March 2020 and December 2020. Methodology: in silico study was carried out using iGEM docking software to predict the binding affinity of lobeline with DPP IV enzyme in comparison with the reference synthetic compound Sitagliptin. Then in vivo experiment was performed on HFD/alloxan induced diabetic mice to evaluate the anti hyperglycemic effect of lobeline. After treatment duration of 21 days, FBG and the inhibitory effect on DPP IV enzyme activity were measured. Results: Lobeline bound efficiently to the active site of DPP IV enzyme and consumed less binding energy than Sitagliptin. This finding was confirmed by the in vivo study. Administration of lobe line at a dose of 25 mg/kg in HFD/alloxan induced diabetic mice produced a significant reduction in blood glucose level and in DPP IV activity compared to the diabetic control group (P value> .01). Conclusion: Lobe line could be a good candidate to be developed as a natural compound for treating diabetes mellitus.

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