Drug discovery approaches targeting the incretin pathway
作者： Xinxian Deng , Mojdeh S. Tavallaie , Ran Sun , Juntao Wang , Qingqing Cai
DOI: 10.1016/J.BIOORG.2020.103810
关键词: Receptor targeting 、 DPP-4 Inhibitors 、 Bioinformatics 、 Chemistry 、 Receptor 、 Drug discovery 、 Drug 、 Incretin 、 Organic chemistry 、 Biochemistry 、 Molecular biology
摘要: Incretin pathway plays an important role in the development of diabetes medications. Interventions DPP-4 and GLP-1 receptor have shown remarkable efficacy experimental clinical studies imperatively become one most promising therapeutic approaches T2DM drug discovery pipeline. Herein, we analyzed actionmechanismsof targeting incretin treatment. We gave insight into structural requirements for potent inhibitors revealed a classification by stressing on binding modes these ligands to enzyme. then reviewed strategies peptide non-peptide agonists (GLP-1 RAs). Furthermore, design GLP-1R were detailed accurately. This review might provide efficient evidence highly selective RAs, as novel medicines patients suffering from T2DM.
elsevier.com
sci-hub.se 参考文章(169)
Máire E. Doyle, Josephine M. Egan, Mechanisms of action of glucagon-like peptide 1 in the pancreas Pharmacology & Therapeutics. ,vol. 113, pp. 546- 593 ,(2007) , 10.1016/J.PHARMTHERA.2006.11.007
Sachiko Hattori, Sitagliptin reduces albuminuria in patients with type 2 diabetes [Rapid Communication] Endocrine Journal. ,vol. 58, pp. 69- 73 ,(2011) , 10.1507/ENDOCRJ.K10E-382
Sneha R. Sagar, Jessica K. Agarwal, Dhaivat H. Pandya, Ranjeet Prasad Dash, Manish Nivsarkar, Kamala K. Vasu, Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes. Bioorganic & Medicinal Chemistry Letters. ,vol. 25, pp. 4428- 4433 ,(2015) , 10.1016/J.BMCL.2015.09.015
Yukihisa S. Watanabe, Yoshika Yasuda, Yuko Kojima, Shino Okada, Tomoko Motoyama, Ryo Takahashi, Mitsuru Oka, Anagliptin, a potent dipeptidyl peptidase IV inhibitor: its single-crystal structure and enzyme interactions Journal of Enzyme Inhibition and Medicinal Chemistry. ,vol. 30, pp. 981- 988 ,(2015) , 10.3109/14756366.2014.1002402
Annachiara Uccellatore, Stefano Genovese, Ilaria Dicembrini, Edoardo Mannucci, Antonio Ceriello, Comparison Review of Short-Acting and Long-Acting Glucagon-like Peptide-1 Receptor Agonists. Diabetes Therapy. ,vol. 6, pp. 239- 256 ,(2015) , 10.1007/S13300-015-0127-X
Joakim E. Swedberg, Christina I. Schroeder, Justin M. Mitchell, Thomas Durek, David P. Fairlie, David J. Edmonds, David A. Griffith, Roger B. Ruggeri, David R. Derksen, Paula M. Loria, Spiros Liras, David A. Price, David J. Craik, Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists. European Journal of Medicinal Chemistry. ,vol. 103, pp. 175- 184 ,(2015) , 10.1016/J.EJMECH.2015.08.046
Vishal Patel, Amit Joharapurkar, Nirav Dhanesha, Samadhan Kshirsagar, Kartik Patel, Rajesh Bahekar, Gaurang Shah, Mukul Jain, None, Co-agonist of glucagon and GLP-1 reduces cholesterol and improves insulin sensitivity independent of its effect on appetite and body weight in diet-induced obese C57 mice. Canadian Journal of Physiology and Pharmacology. ,vol. 91, pp. 1009- 1015 ,(2013) , 10.1139/CJPP-2013-0189
Tao Jiang, Yuren Zhou, Jianming Zhu, Zhuxi Chen, Peng Sun, Qiang Zhang, Zhen Wang, Qiang Shao, Xiangrui Jiang, Bo Li, Heyao Wang, Weiliang Zhu, Jingshan Shen, Design, Synthesis, and Pharmacological Evaluation of Highly Potent and Selective Dipeptidyl Peptidase-4 Inhibitors Archiv der Pharmazie. ,vol. 348, pp. 399- 407 ,(2015) , 10.1002/ARDP.201500082
Susan Clardy-James, Oleg G. Chepurny, Colin A. Leech, George G. Holz, Robert P. Doyle, Synthesis, Characterization and Pharmacodynamics of Vitamin-B12-Conjugated Glucagon-Like Peptide-1 ChemMedChem. ,vol. 8, pp. 582- 586 ,(2013) , 10.1002/CMDC.201200461
Manjunath Ghate, Shailesh V. Jain, Structure Based Lead Optimization Approach in Discovery of Selective DPP4 Inhibitors Mini-reviews in Medicinal Chemistry. ,vol. 13, pp. 888- 914 ,(2013) , 10.2174/1389557511313060010