Docking study of the precursor peptide of matoparan onto its putative processing enzyme, dipeptidyl peptidase IV: a revisit to molecular ticketing

2010 ◽  
Vol 24 (3) ◽  
pp. 213-224
Author(s):  
Soonmin Jang ◽  
Tse-Yu Chung ◽  
Jungho Shin ◽  
Kai-Lun Lin ◽  
Jason T. C. Tzen ◽  
...  
Keyword(s):  
Docking Study ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Processing Enzyme ◽  
Precursor Peptide

Docking Study of Novel Pyrrolidine Derivatives as Potential Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors

2015 ◽  
Vol 12 (4) ◽  
pp. 284-291 ◽  
Author(s):  
Sant Kumar Verma ◽  
Shashi Kant Sharma ◽  
Suresh Thareja
Keyword(s):  
Docking Study ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Dpp Iv

Experimental anxiety-depressive state in rats caused by neonatal exposure to the inhibitor of dipeptidyl peptidase IV, diprotin A: effects of imipramine

2017 ◽  
pp. 4-12
Author(s):  
Н.Н. Хлебникова ◽  
Н.А. Крупина
Keyword(s):  
Forced Swimming Test ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Forced Swimming ◽  
Face Validity ◽  
Neonatal Exposure ◽  
Depressive State ◽  
Serum Corticosterone ◽  
Old Rats ◽  
Swimming Test

В наших предыдущих исследованиях было показано, что ингибитор пролинспецифической пептидазы дипептидилпептидазы-IV (ДП-IV, EC 3.4.14.5) трипептид дипротин А, введенный крысам в 5-18 постнатальные дни, приводит к развитию у крыс подросткового возраста и взрослых животных эмоционально-мотивационных расстройств. Такие расстройства можно рассматривать как модель смешанного тревожно-депрессивного состояния. Однако специальных исследований по валидности данной модели проведено не было. Цель настоящей работы состояла в проверке влияния трициклического антидепрессанта имипрамина (ИМИ) на депрессивноподобное поведение крыс и уровень кортикостерона в сыворотке крови животных на модели смешанного тревожно-депрессивного состояния. Методика. У крыс в возрасте одного и двух мес. определяли уровень тревожности в автоматизированном тесте «Приподнятый крестообразный лабиринт» и оценивали депрессивноподобное поведение в тесте принудительного плавания. ИМИ вводили взрослым животным в течение 10 дней (20 мг/кг/день, интрагастрально). Уровень кортикостерона в сыворотке крови определяли методом твердофазного иммуноферментного анализа. Результаты. Неонатальное действие дипротина А приводило к повышению тревожности у крыс в возрасте 1 мес. Депрессивноподобное поведение обнаружено у животных в возрасте одного и двух мес. ИМИ нормализовал поведение животных в тесте принудительного плавания и снижал уровень кортикостерона в сыворотке крови крыс. Кроме того, ИМИ снижал вес крыс. Заключение. Результаты исследования свидетельствуют в пользу адекватности модели смешанного тревожно-депрессивного расстройства, возникающего у крыс вследствие действия ингибитора ДП-IV дипротина А на второй-третьей неделях постнатального развития, клиническому прообразу заболевания по критериям «внешней схожести», прогностической и конструкционной валидности. Previously, we have shown that the inhibitor of proline-specific peptidase, dipeptidyl peptidase-IV (DP-IV, EC 3.4.14.5), tripeptide diproptin A administered on postnatal days 5-18 induced emotional and motivational disorders in adolescent and adult rats. These disorders can be considered a model of a mixed anxiety-depression-like disorder. However, validation studies of this model are not available. The aim of this work was to test the effect of the tricyclic antidepressant, imipramine (IMI), on depressive-like behavior in rats and the level of serum corticosterone using the model of mixed anxiety-depressive state. Methods. The level of anxiety was assessed by the automated Elevated Plus Maze test and the depressive-like behavior was evaluated by the forced swimming test in one- and two-month old rats. IMI was administered to adult animals for ten days (20 mg/kg a day, intragastrically). Serum corticosterone concentrations were measured using ELISA. Results. The neonatal exposure to diprotin A increased anxiety in one-month old rats. The depressive-like behavior was observed in animals aged one and two months. IMI normalized behavior of animals in the forced swimming test and reduced serum levels of corticosterone. Also, IMI reduced body weight of rats. Conclusion. The results of the study evidenced adequacy of the model of mixed anxiety-depressive state induced by the DP-IV inhibitor, diprotin A, on the second and third postnatal weeks to the clinical prototype of disease according to criteria of face validity, predictive and construct validity.

An Overview of Recent Dipeptidyl Peptidase-IV Inhibitors: Linking their Structure and Physico-Chemical Properties with SAR, Pharmacokinetics and Toxicity

2015 ◽  
Vol 15 (23) ◽  
pp. 2342-2372 ◽  
Author(s):  
Andrija Smelcerovic ◽  
Filip Miljkovic ◽  
Ana Kolarevic ◽  
Jelena Lazarevic ◽  
Aleksandra Djordjevic ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Physico Chemical ◽  
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.

Synthesis, Structural Characterization and Docking Studies of Sulfamoyl- Phenyl Acid Esters as Dipeptidyl Peptidase-IV Inhibitors

2018 ◽  
Vol 14 (2) ◽  
pp. 142-151
Author(s):  
Reema Abu Khalaf ◽  
Dima Sabbah ◽  
Eveen Al-Shalabi ◽  
Iyad Al-Sheikh ◽  
Ghadeer Albadawi ◽  
...  
Keyword(s):  
Structural Characterization ◽  
Dipeptidyl Peptidase ◽  
Docking Studies ◽  
Dipeptidyl Peptidase Iv ◽  
Dipeptidyl Peptidase Iv Inhibitors ◽  
Acid Esters
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