Literature DB >> 28337323

Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure.

Marion Lanier1, Jason Pickens1, Simone V Bigi1, Erica L Bradshaw-Pierce1, Alison Chambers1, Zacharia S Cheruvallath1, Derek Cole1, Douglas R Dougan1, Jacques Ermolieff1, Tony Gibson1, Petro Halkowycz1, Aki Hirokawa1, Anthony Ivetac1, Joanne Miura1, Evan Nunez1, Mark Sabat1, John Tyhonas1, Haixia Wang1, Xiaolun Wang1, Steve Swann1.   

Abstract

Apoptosis signal-regulating kinase 1 (ASK1/MAP3K) is a mitogen-activated protein kinase family member shown to contribute to acute ischemia/reperfusion injury. Using structure-based drug design, deconstruction, and reoptimization of a known ASK1 inhibitor, a lead compound was identified. This compound displayed robust MAP3K pathway inhibition and reduction of infarct size in an isolated perfused heart model of cardiac injury.

Entities:  

Keywords:  Apoptosis signal-regulating kinase 1 (ASK1); cardiac injury; structure-based drug design (SBDD)

Year:  2017        PMID： 28337323      PMCID： PMC5346976          DOI： 10.1021/acsmedchemlett.6b00481

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


  12 in total

1.  Ligand efficiency: a useful metric for lead selection.

Authors:  Andrew L Hopkins; Colin R Groom; Alexander Alex
Journal:  Drug Discov Today       Date:  2004-05-15       Impact factor: 7.851

Review 2.  The influence of drug-like concepts on decision-making in medicinal chemistry.

Authors:  Paul D Leeson; Brian Springthorpe
Journal:  Nat Rev Drug Discov       Date:  2007-11       Impact factor: 84.694

3.  Group efficiency: a guideline for hits-to-leads chemistry.

Authors:  Marcel L Verdonk; David C Rees
Journal:  ChemMedChem       Date:  2008-08       Impact factor: 3.466

4.  Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.

Authors:  Yoshito Terao; Hideo Suzuki; Masato Yoshikawa; Hiroaki Yashiro; Shiro Takekawa; Yasushi Fujitani; Kengo Okada; Yoshihisa Inoue; Yoshio Yamamoto; Hideyuki Nakagawa; Shuhei Yao; Tomohiro Kawamoto; Osamu Uchikawa
Journal:  Bioorg Med Chem Lett       Date:  2012-10-23       Impact factor: 2.823

5.  Design of a phase 2 clinical trial of an ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease.

Authors:  Joseph H Lin; Jenny J Zhang; Shao-Lee Lin; Glenn M Chertow
Journal:  Nephron       Date:  2014-12-17       Impact factor: 2.847

Review 6.  The stress-activated protein kinase pathways.

Authors:  L A Tibbles; J R Woodgett
Journal:  Cell Mol Life Sci       Date:  1999-08-15       Impact factor: 9.261

Review 7.  Activation mechanisms of ASK1 in response to various stresses and its significance in intracellular signaling.

Authors:  Shigeru Shiizaki; Isao Naguro; Hidenori Ichijo
Journal:  Adv Biol Regul       Date:  2012-09-13

8.  Intracellular shuttling and mitochondrial function of thioredoxin-interacting protein.

Authors:  Geetu Saxena; Junqin Chen; Anath Shalev
Journal:  J Biol Chem       Date:  2009-12-03       Impact factor: 5.157

9.  Crystal structures of ASK1-inhibtor complexes provide a platform for structure-based drug design.

Authors:  Onkar Singh; Anthony Shillings; Peter Craggs; Ian Wall; Paul Rowland; Tadeusz Skarzynski; Clare I Hobbs; Phil Hardwick; Rob Tanner; Michelle Blunt; David R Witty; Kathrine J Smith
Journal:  Protein Sci       Date:  2013-07-03       Impact factor: 6.725

10.  The roles of ASK family proteins in stress responses and diseases.

Authors:  Kazuki Hattori; Isao Naguro; Christopher Runchel; Hidenori Ichijo
Journal:  Cell Commun Signal       Date:  2009-04-24       Impact factor: 5.712
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  6 in total

1.  Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors.

Authors:  Andrii Monastyrskyi; Simon Bayle; Victor Quereda; Wayne Grant; Michael Cameron; Derek Duckett; William Roush
Journal:  Bioorg Med Chem Lett       Date:  2017-12-13       Impact factor: 2.823

2.  ASK1 contributes to fibrosis and dysfunction in models of kidney disease.

Authors:  John T Liles; Britton K Corkey; Gregory T Notte; Grant R Budas; Eric B Lansdon; Ford Hinojosa-Kirschenbaum; Shawn S Badal; Michael Lee; Brian E Schultz; Sarah Wise; Swetha Pendem; Michael Graupe; Laurie Castonguay; Keith A Koch; Melanie H Wong; Giuseppe A Papalia; Dorothy M French; Theodore Sullivan; Erik G Huntzicker; Frank Y Ma; David J Nikolic-Paterson; Tareq Altuhaifi; Haichun Yang; Agnes B Fogo; David G Breckenridge
Journal:  J Clin Invest       Date:  2018-07-19       Impact factor: 14.808

3.  Investigating the Mechanism of Inhibition of Cyclin-Dependent Kinase 6 Inhibitory Potential by Selonsertib: Newer Insights Into Drug Repurposing.

Authors:  Mohammad Hassan Baig; Mohd Yousuf; Mohd Imran Khan; Imran Khan; Irfan Ahmad; Mohammad Y Alshahrani; Md Imtaiyaz Hassan; Jae-June Dong
Journal:  Front Oncol       Date:  2022-05-26       Impact factor: 5.738

4.  Redox Regulation of Cardiac ASK1 (Apoptosis Signal-Regulating Kinase 1) Controls p38-MAPK (Mitogen-Activated Protein Kinase) and Orchestrates Cardiac Remodeling to Hypertension.

Authors:  Daniel N Meijles; Joshua J Cull; Thomais Markou; Susanna T E Cooper; Zoe H R Haines; Stephen J Fuller; Peter O'Gara; Mary N Sheppard; Sian E Harding; Peter H Sugden; Angela Clerk
Journal:  Hypertension       Date:  2020-09-09       Impact factor: 10.190

5.  Phosphoproteomics identify arachidonic-acid-regulated signal transduction pathways modulating macrophage functions with implications for ovarian cancer.

Authors:  Raimund Dietze; Mohamad K Hammoud; María Gómez-Serrano; Annika Unger; Tim Bieringer; Florian Finkernagel; Anna M Sokol; Andrea Nist; Thorsten Stiewe; Silke Reinartz; Viviane Ponath; Christian Preußer; Elke Pogge von Strandmann; Sabine Müller-Brüsselbach; Johannes Graumann; Rolf Müller
Journal:  Theranostics       Date:  2021-01-01       Impact factor: 11.556

Review 6.  Recent Advances in Pain Management: Relevant Protein Kinases and Their Inhibitors.

Authors:  Francis Giraud; Elisabeth Pereira; Fabrice Anizon; Pascale Moreau
Journal:  Molecules       Date:  2021-05-04       Impact factor: 4.411
  6 in total

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