Literature DB >> 26191360

Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.

Shawn P Walsh1, Aurash Shahripour1, Haifeng Tang1, Nardos Teumelsan1, Jessica Frie1, Yuping Zhu1, Birgit T Priest1, Andrew M Swensen1, Jessica Liu1, Michael Margulis1, Richard Visconti1, Adam Weinglass1, John P Felix1, Richard M Brochu1, Timothy Bailey1, Brande Thomas-Fowlkes1, Magdalena Alonso-Galicia1, Xiaoyan Zhou1, Lee-Yuh Pai1, Aaron Corona1, Caryn Hampton1, Melba Hernandez1, Ross Bentley1, Jing Chen1, Kashmira Shah1, Joseph Metzger1, Michael Forrest1, Karen Owens1, Vincent Tong1, Sookhee Ha1, Sophie Roy1, Gregory J Kaczorowski1, Lihu Yang1, Emma Parmee1, Maria L Garcia1, Kathleen Sullivan1, Alexander Pasternak1.   

Abstract

A new subseries of ROMK inhibitors exemplified by 28 has been developed from the initial screening hit 1. The excellent selectivity for ROMK inhibition over related ion channels and pharmacokinetic properties across preclinical species support further preclinical evaluation of 28 as a new mechanism diuretic. Robust pharmacodynamic effects in both SD rats and dogs have been demonstrated.

Entities:  

Keywords:  ROMK; diuresis; heart failure; hypertension; natriuresis

Year:  2015        PMID： 26191360      PMCID： PMC4499836          DOI： 10.1021/ml500440u

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  25 in total

Review 1.  Molecular mechanisms of human hypertension.

Authors:  R P Lifton; A G Gharavi; D S Geller
Journal:  Cell       Date:  2001-02-23       Impact factor: 41.582

2.  High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1.

Authors:  L Michelle Lewis; Gautam Bhave; Brian A Chauder; Sreedatta Banerjee; Katharina A Lornsen; Rey Redha; Katherine Fallen; Craig W Lindsley; C David Weaver; Jerod S Denton
Journal:  Mol Pharmacol       Date:  2009-08-25       Impact factor: 4.436

3.  Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.

Authors:  Haifeng Tang; Shawn P Walsh; Yan Yan; Reynalda K de Jesus; Aurash Shahripour; Nardos Teumelsan; Yuping Zhu; Sookhee Ha; Karen A Owens; Brande S Thomas-Fowlkes; John P Felix; Jessica Liu; Martin Kohler; Birgit T Priest; Timothy Bailey; Richard Brochu; Magdalena Alonso-Galicia; Gregory J Kaczorowski; Sophie Roy; Lihu Yang; Sander G Mills; Maria L Garcia; Alexander Pasternak
Journal:  ACS Med Chem Lett       Date:  2012-03-28       Impact factor: 4.345

4.  Functional and pharmacological properties of canine ERG potassium channels.

Authors:  Jixin Wang; Kimberly Della Penna; Hao Wang; Jerzy Karczewski; Thomas M Connolly; Kenneth S Koblan; Paul B Bennett; Joseph J Salata
Journal:  Am J Physiol Heart Circ Physiol       Date:  2002-10-03       Impact factor: 4.733

5.  The inwardly rectifying potassium channel Kir1.1: development of functional assays to identify and characterize channel inhibitors.

Authors:  John P Felix; Birgit T Priest; Kelli Solly; Timothy Bailey; Richard M Brochu; Chou J Liu; Martin G Kohler; Laszlo Kiss; Magdalena Alonso-Galicia; Haifeng Tang; Alexander Pasternak; Gregory J Kaczorowski; Maria L Garcia
Journal:  Assay Drug Dev Technol       Date:  2012-08-10       Impact factor: 1.738

Review 6.  The impact of drug-induced QT interval prolongation on drug discovery and development.

Authors:  Bernard Fermini; Anthony A Fossa
Journal:  Nat Rev Drug Discov       Date:  2003-06       Impact factor: 84.694

7.  Cloning and characterization of multiple forms of the human kidney ROM-K potassium channel.

Authors:  M E Shuck; J H Bock; C W Benjamin; T D Tsai; K S Lee; J L Slightom; M J Bienkowski
Journal:  J Biol Chem       Date:  1994-09-30       Impact factor: 5.157

8.  A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel.

Authors:  M C Sanguinetti; C Jiang; M E Curran; M T Keating
Journal:  Cell       Date:  1995-04-21       Impact factor: 41.582

9.  Common variation in the WNK1 gene and blood pressure in childhood: the Avon Longitudinal Study of Parents and Children.

Authors:  Martin D Tobin; Nicholas J Timpson; Louise V Wain; Susan Ring; Louise R Jones; Pauline M Emmett; Thomas M Palmer; Andrew R Ness; Nilesh J Samani; George Davey Smith; Paul R Burton
Journal:  Hypertension       Date:  2008-09-22       Impact factor: 10.190

10.  Rare independent mutations in renal salt handling genes contribute to blood pressure variation.

Authors:  Weizhen Ji; Jia Nee Foo; Brian J O'Roak; Hongyu Zhao; Martin G Larson; David B Simon; Christopher Newton-Cheh; Matthew W State; Daniel Levy; Richard P Lifton
Journal:  Nat Genet       Date:  2008-04-06       Impact factor: 38.330
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  2 in total

1.  Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.

Authors:  Haifeng Tang; Yuping Zhu; Nardos Teumelsan; Shawn P Walsh; Aurash Shahripour; Birgit T Priest; Andrew M Swensen; John P Felix; Richard M Brochu; Timothy Bailey; Brande Thomas-Fowlkes; Lee-Yuh Pai; Caryn Hampton; Aaron Corona; Melba Hernandez; Joseph Metzger; Michael Forrest; Xiaoyan Zhou; Karen Owens; Vincent Tong; Emma Parmee; Sophie Roy; Gregory J Kaczorowski; Lihu Yang; Magdalena Alonso-Galicia; Maria L Garcia; Alexander Pasternak
Journal:  ACS Med Chem Lett       Date:  2016-05-12       Impact factor: 4.345

2.  Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors.

Authors:  Matthew F Sammons; Sujay V Kharade; Kevin J Filipski; Markus Boehm; Aaron C Smith; Andre Shavnya; Dilinie P Fernando; Matthew S Dowling; Philip A Carpino; Neil A Castle; Shannon G Zellmer; Brett M Antonio; James R Gosset; Anthony Carlo; Jerod S Denton
Journal:  ACS Med Chem Lett       Date:  2018-01-19       Impact factor: 4.345
  2 in total

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