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Review Article

Inhibitors of Renin as Potential Therapeutic Agents

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Pages 169-185 | Received 07 Mar 1986, Published online: 27 Sep 2008

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Gianpaolo Reboldi, Giorgio Gentile, Fabio Angeli & Paolo Verdecchia. (2011) Pharmacokinetic, pharmacodynamic and clinical evaluation of aliskiren for hypertension treatment. Expert Opinion on Drug Metabolism & Toxicology 7:1, pages 115-128.
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Paolo Verdecchia, Fabio Angeli, Giovanni Mazzotta, Giorgio Gentile & Gianpaolo Reboldi. (2008) The renin angiotensin system in the development of cardiovascular disease: role of aliskiren in risk reduction. Vascular Health and Risk Management 4:5, pages 971-981.
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Helmy Siragy, Jiqian Huang & David C Lieb. (2008) The development of the direct renin inhibitor aliskiren: treating hypertension and beyond. Expert Opinion on Emerging Drugs 13:3, pages 417-430.
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Huifang Cheng & Raymond C Harris. (2006) Potential side effects of renin inhibitors – mechanisms based on comparison with other renin–angiotensin blockers. Expert Opinion on Drug Safety 5:5, pages 631-641.
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Jürgen Maibaum & David L Feldman. (2003) Renin inhibitors as novel treatments for cardiovascular disease. Expert Opinion on Therapeutic Patents 13:5, pages 589-603.
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Naomi DL Fisher & Norman K Hollenberg. (2001) Is there a future for renin inhibitors?. Expert Opinion on Investigational Drugs 10:3, pages 417-426.
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Peter Raddatz. (1994) Overview Cardiovascular & Renal: Recent developments in renin inhibitors: part 1. Expert Opinion on Therapeutic Patents 4:5, pages 489-504.
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Tomoya Hara, Takeshi Yamamura, Mirei Murakami‐Asahina, Hirokazu Matsumoto, Michiyasu Takeyama, Ray Kanagawa & Tomoyuki Nishimoto. (2020) Development of a novel murine heart failure model overexpressing human renin and angiotensinogen. FEBS Open Bio 10:5, pages 718-725.
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Xingxing Li, Jing Liao, Zhongliang Jiang, Xinyu Liu, Shan Chen, Xia He, Ling Zhu, Xingmei Duan, Zhuyu Xu, Baowen Qi, Xiaoqiang Guo, Rongsheng Tong & Jianyou Shi. (2020) A concise review of recent advances in anti-heart failure targets and its small molecules inhibitors in recent years. European Journal of Medicinal Chemistry 186, pages 111852.
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Tomoya Hara, Satoshi Nishimura, Toshihiro Yamamoto, Yumiko Kajimoto, Keiji Kusumoto, Ray Kanagawa, Shota Ikeda & Tomoyuki Nishimoto. (2018) TAK-272 (imarikiren), a novel renin inhibitor, improves cardiac remodeling and mortality in a murine heart failure model. PLOS ONE 13:8, pages e0202176.
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Hidekazu Tokuhara, Yasuhiro Imaeda, Yoshiyuki Fukase, Koichi Iwanaga, Naohiro Taya, Koji Watanabe, Ray Kanagawa, Keisuke Matsuda, Yumiko Kajimoto, Keiji Kusumoto, Mitsuyo Kondo, Gyorgy Snell, Craig A. Behnke & Takanobu Kuroita. (2018) Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile. Bioorganic & Medicinal Chemistry 26:12, pages 3261-3286.
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Lara McGillewie, Muthusamy Ramesh & Mahmoud E. Soliman. (2017) Sequence, Structural Analysis and Metrics to Define the Unique Dynamic Features of the Flap Regions Among Aspartic Proteases. The Protein Journal 36:5, pages 385-396.
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Estella G. da Mota, Mariene H. Duarte, Elaine F. F. da Cunha & Matheus P. Freitas. (2015) Theoretical design of new indole-3-carboxamide derivatives as renin inhibitors. Medicinal Chemistry Research 24:7, pages 3097-3106.
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Holger Sellner, Sylvain Cottens, Frédéric Cumin, Claus Ehrhardt, Takatoshi Kosaka, Edwige Lorthiois, Nils Ostermann, Randy L. Webb, Dean F. Rigel, Trixie Wagner & Jürgen Maibaum. (2015) trans -3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: Prime site exploration using an oxygen linker. Bioorganic & Medicinal Chemistry Letters 25:8, pages 1787-1791.
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Edwige Lorthiois, Frederic Cumin, Claus Ehrhardt, Takatoshi Kosaka, Holger Sellner, Nils Ostermann, Eric Francotte, Trixie Wagner & Jürgen Maibaum. (2015) trans -(3 S ,4 S )-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: Prime site exploration using an amino linker. Bioorganic & Medicinal Chemistry Letters 25:8, pages 1782-1786.
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Hitesh V. Motwani, Maria De Rosa, Luke R. Odell, Anders Hallberg & Mats Larhed. (2015) Aspartic protease inhibitors containing tertiary alcohol transition-state mimics. European Journal of Medicinal Chemistry 90, pages 462-490.
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Pitchai Balakumar & Gowraganahalli Jagadeesh. (2014) A century old renin–angiotensin system still grows with endless possibilities: AT1 receptor signaling cascades in cardiovascular physiopathology. Cellular Signalling 26:10, pages 2147-2160.
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F. T. HAMMAD, S. AL-SALAM & L. LUBBAD. (2013) Does Aliskiren Protect the Kidney Following Ischemia Reperfusion Injury?. Physiological Research, pages 681-690.
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Hans H. Gorris. (2013) Kinetic analysis of renin and its inhibitors by detecting double-labelled peptidic substrates with an immunoassay. The Analyst 138:7, pages 2104.
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Tao Jing, Jian Feng, Yumei Zuo, Boli Ran, Jianping Liu & Guoxiang He. (2012) Exploring the substructural space of indole-3-carboxamide derivatives binding to renin: a novel active-site spatial partitioning approach. Journal of Molecular Modeling 18:9, pages 4417-4426.
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Haralambos Tzoupis, Georgios Leonis, Grigorios Megariotis, Claudiu T. Supuran, Thomas Mavromoustakos & Manthos G. Papadopoulos. (2012) Dual Inhibitors for Aspartic Proteases HIV-1 PR and Renin: Advancements in AIDS–Hypertension–Diabetes Linkage via Molecular Dynamics, Inhibition Assays, and Binding Free Energy Calculations. Journal of Medicinal Chemistry 55:12, pages 5784-5796.
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Aggeliki Politi , Georgios Leonis, Haralambos Tzoupis , Dimitrios Ntountaniotis, Manthos G. Papadopoulos, Simona Golic Grdadolnik  & Thomas Mavromoustakos . (2011) Conformational Properties and Energetic Analysis of Aliskiren in Solution and Receptor Site. Molecular Informatics 30:11-12, pages 973-985.
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Lanqi Jia, Robert D. Simpson, Jing Yuan, Zhenrong Xu, Wei Zhao, Salvacion Cacatian, Colin M. Tice, Joan Guo, Alexey Ishchenko, Suresh B. Singh, Zhongren Wu, Brian M. McKeever, Yuri Bukhtiyarov, Judith A. Johnson, Christopher P. Doe, Richard K. Harrison, Gerard M. McGeehan, Lawrence W. Dillard, John J. Baldwin & David A. Claremon. (2011) Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility. ACS Medicinal Chemistry Letters 2:10, pages 747-751.
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Bodo Scheiper, Hans Matter, Henning Steinhagen, Zsolt Böcskei, Valérie Fleury & Gary McCort. (2011) Structure-based optimization of potent 4- and 6-azaindole-3-carboxamides as renin inhibitors. Bioorganic & Medicinal Chemistry Letters 21:18, pages 5480-5486.
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Hans Matter, Bodo Scheiper, Henning Steinhagen, Zsolt B?cskei, Val?rie Fleury & Gary McCort. (2011) Structure-based design and optimization of potent renin inhibitors on 5- or 7-azaindole-scaffolds. Bioorganic & Medicinal Chemistry Letters 21:18, pages 5487-5492.
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