Literature DB >> 17270434

Structure-activity relationship analysis of a novel necroptosis inhibitor, Necrostatin-5.

Ke Wang1, Jinfeng Li, Alexei Degterev, Emily Hsu, Junying Yuan, Chengye Yuan.   

Abstract

Necrostatin-5 (Nec-5) is a novel potent small-molecule inhibitor of necroptosis structurally distinct from previously described Necrostatin-1 (Nec-1), and therefore, represents a new direction for the inhibition of this cellular caspase-independent necrotic cell death mechanism. Here, we describe a series of structural modifications of Nec-5 and the structure-activity relationship (SAR) of Nec-5 series in inhibiting necroptosis.

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Year:  2006        PMID： 17270434     DOI： 10.1016/j.bmcl.2006.11.056

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  26 in total

Review 1.  Complex Pathologic Roles of RIPK1 and RIPK3: Moving Beyond Necroptosis.

Authors:  Kelby W Wegner; Danish Saleh; Alexei Degterev
Journal:  Trends Pharmacol Sci       Date:  2017-01-23       Impact factor: 14.819

2.  Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors.

Authors:  Xin Teng; Heather Keys; Arumugasamy Jeevanandam; John A Porco; Alexei Degterev; Junying Yuan; Gregory D Cuny
Journal:  Bioorg Med Chem Lett       Date:  2007-10-17       Impact factor: 2.823

3.  Identification of RIP1 kinase as a specific cellular target of necrostatins.

Authors:  Alexei Degterev; Junichi Hitomi; Megan Germscheid; Irene L Ch'en; Olga Korkina; Xin Teng; Derek Abbott; Gregory D Cuny; Chengye Yuan; Gerhard Wagner; Stephen M Hedrick; Scott A Gerber; Alexey Lugovskoy; Junying Yuan
Journal:  Nat Chem Biol       Date:  2008-05       Impact factor: 15.040

4.  Optimization of tricyclic Nec-3 necroptosis inhibitors for in vitro liver microsomal stability.

Authors:  Sungwoon Choi; Heather Keys; Richard J Staples; Junying Yuan; Alexei Degterev; Gregory D Cuny
Journal:  Bioorg Med Chem Lett       Date:  2012-07-06       Impact factor: 2.823

Review 5.  Neuroprotective strategies targeting apoptotic and necrotic cell death for stroke.

Authors:  Junying Yuan
Journal:  Apoptosis       Date:  2009-04       Impact factor: 4.677

6.  Necrostatin-1 reduces histopathology and improves functional outcome after controlled cortical impact in mice.

Authors:  Zerong You; Sean I Savitz; Jinsheng Yang; Alexei Degterev; Junying Yuan; Gregory D Cuny; Michael A Moskowitz; Michael J Whalen
Journal:  J Cereb Blood Flow Metab       Date:  2008-05-21       Impact factor: 6.200

7.  Structure-activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors.

Authors:  Xin Teng; Heather Keys; Junying Yuan; Alexei Degterev; Gregory D Cuny
Journal:  Bioorg Med Chem Lett       Date:  2008-04-25       Impact factor: 2.823

8.  4-Acetoxyphenol Prevents RPE Oxidative Stress-Induced Necrosis by Functioning as an NRF2 Stabilizer.

Authors:  Jakub Hanus; Alexander Kolkin; Julia Chimienti; Sara Botsay; Shusheng Wang
Journal:  Invest Ophthalmol Vis Sci       Date:  2015-08       Impact factor: 4.799

Review 9.  Generation of small molecules to interfere with regulated necrosis.

Authors:  Alexei Degterev; Andreas Linkermann
Journal:  Cell Mol Life Sci       Date:  2016-04-05       Impact factor: 9.261

10.  RIPK3 upregulation confers robust proliferation and collateral cystine-dependence on breast cancer recurrence.

Authors:  James V Alvarez; Jen-Tsan Chi; Chao-Chieh Lin; Nathaniel W Mabe; Yi-Tzu Lin; Wen-Hsuan Yang; Xiaohu Tang; Lisa Hong; Tianai Sun; Jeremy Force; Jeffrey R Marks; Tso-Pang Yao
Journal:  Cell Death Differ       Date:  2020-01-27       Impact factor: 15.828
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