Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics

Aretz Christopher D.; Vadukoot Anish K.; Hopkins Corey R.

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Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics

机译：发现小分子肾外髓质钾（romk）通道抑制剂：一种浅谈药用化学方法，培养新型利尿疗法

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The renal outer medullary potassium (ROMK) channel is a member of the inwardly rectifying family of potassium (Kir, Kir1.1) channels. It is primarily expressed in two regions of the kidney, the cortical collecting duct (CCD) and the thick ascending loop of Henle (TALH). At the CCD it tightly regulates potassium secretion while controlling potassium recycling in TALH. As loss-of-function mutations lead to salt wasting and low blood pressure, it has been surmised that inhibitors of ROMK would represent a target for new and improved diuretics for the treatment of hypertension and heart failure. In this review, we discuss and provide an overview of the medicinal chemistry approaches toward the development of small molecule ROMK inhibitors over the past decade.

机译：肾外外髓质钾（ROMK）通道是内侧整流钾（KIR，KIR1.1）通道的成员。它主要在肾脏的两个区域中表达，皮质收集管道（CCD）和HENLE（塔卢）的厚升序环。在CCD，它紧紧地调节钾分泌，同时控制塔卢的钾回收。由于功能丧失突变导致盐浪费和低血压，因此已经抑制了romk的抑制剂将代表新的和改进利尿剂的目标，用于治疗高血压和心力衰竭。在本综述中，我们在过去十年中讨论并讨论了药物化学方法，以朝着过去十年来开发小分子romk抑制剂的概述。

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《Journal of Medicinal Chemistry》 |2019年第19期|共13页
作者
Aretz Christopher D.; Vadukoot Anish K.; Hopkins Corey R.;
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Univ Nebraska Med Ctr Coll Pharm Dept Pharmaceut Sci Omaha NE 68198 USA;

Univ Nebraska Med Ctr Coll Pharm Dept Pharmaceut Sci Omaha NE 68198 USA;

Univ Nebraska Med Ctr Coll Pharm Dept Pharmaceut Sci Omaha NE 68198 USA;

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正文语种 eng
中图分类药学;
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1. Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics [J] . Aretz Christopher D., Vadukoot Anish K., Hopkins Corey R. Journal of Medicinal Chemistry . 2019,第19期

机译：发现小分子肾外髓质钾（romk）通道抑制剂：一种浅谈药用化学方法，培养新型利尿疗法
2. Inhibitor of growth 4 (ING4) is up-regulated by a low K intake and suppresses renal outer medullary K channels (ROMK) by MAPK stimulation [J] . Xin Zhang, Dao-Hong Lin, Yan Jin, Proceedings of the National Academy of Sciences of the United States of America . 2007,第22期

机译：低钾摄入量会上调生长抑制剂4（ING4），并通过MAPK刺激抑制肾外髓质K通道（ROMK）
3. The endosomal trafficking factors CORVET and ESCRT suppress plasma membrane residence of the renal outer medullary potassium channel (ROMK) [J] . Timothy Mackie, Bo-Young Kim, Arohan R. Subramanya, The Journal of biological chemistry . 2018,第9期

机译：内体运输因子CORVET和ESCRT抑制肾外髓质钾通道（ROMK）的质膜滞留
4. A Multiplatform Strategy for the Discovery of Conventional Monoclonal Antibodies That Inhibit the Voltage-Gated Potassium Channel Kvl.3. [C] . Yelena Bisharyan, J. Bednenko, R. Harriman, Protein Engineering Summit. . 2018

机译：一种抑制电压门控钾通道KVL的常规单克隆抗体的多平台策略。
5. The endosomal trafficking factors CORVET and ESCRT suppress plasma membrane residence of the renal outer medullary potassium channel (ROMK) [O] . Timothy D. Mackie, Bo-Young Kim, Arohan R. Subramanya, 2018

机译：内体运输因子CORVET和ESCRT抑制肾外髓质钾通道（ROMK）的质膜滞留
6. Development of a Selective Small-Molecule Inhibitor of Kir1.1, the Renal Outer Medullary Potassium ChannelS⃞ [O] . Bhave, Gautam, Chauder, Brian A., Liu, Wen, 2010

机译：选择性小分子抑制剂的研制肾外延髓钾通道Kir1.1

Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics

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