Literature DB >> 16002288

Structure-activity relationship studies of salubrinal lead to its active biotinylated derivative.

Kai Long1, Michael Boyce, He Lin, Junying Yuan, Dawei Ma.   

Abstract

The synthesis and structure-activity relationships (SAR) of salubrinal, a small molecule that protects cells from apoptosis induced by endoplasmic reticulum (ER) stress, are described. It is revealed that the trichloromethyl group greatly contributes to the activity. Based on the SAR results, salubrinal was converted into a biotinylated derivative which retains activity and can be used as a biological tool for target identification.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 16002288     DOI: 10.1016/j.bmcl.2005.05.120

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


  9 in total

Review 1.  Therapeutic Opportunities in Eukaryotic Translation.

Authors:  Jennifer Chu; Jerry Pelletier
Journal:  Cold Spring Harb Perspect Biol       Date:  2018-06-01       Impact factor: 10.005

2.  Salubrinal promotes healing of surgical wounds in rat femurs.

Authors:  Ping Zhang; Kazunori Hamamura; Chang Jiang; Liming Zhao; Hiroki Yokota
Journal:  J Bone Miner Metab       Date:  2012-05-19       Impact factor: 2.626

3.  Synthesis, maturation, and trafficking of human Na+-dicarboxylate cotransporter NaDC1 requires the chaperone activity of cyclophilin B.

Authors:  Marc J Bergeron; Marc Bürzle; Gergely Kovacs; Alexandre Simonin; Matthias A Hediger
Journal:  J Biol Chem       Date:  2011-01-21       Impact factor: 5.157

4.  ICP34.5-dependent and -independent activities of salubrinal in herpes simplex virus-1 infected cells.

Authors:  Kevin F Bryant; Elizabeth R Macari; Natasha Malik; Michael Boyce; Junying Yuan; Donald M Coen
Journal:  Virology       Date:  2008-08-06       Impact factor: 3.616

Review 5.  Experimental Evidence Shows Salubrinal, an eIF2α Dephosphorylation Inhibitor, Reduces Xenotoxicant-Induced Cellular Damage.

Authors:  Masato Matsuoka; Yuta Komoike
Journal:  Int J Mol Sci       Date:  2015-07-17       Impact factor: 5.923

6.  A general method for the metal-free, regioselective, remote C-H halogenation of 8-substituted quinolines.

Authors:  Damoder Reddy Motati; Dilipkumar Uredi; E Blake Watkins
Journal:  Chem Sci       Date:  2018-01-05       Impact factor: 9.825

7.  Molecular docking studies of salubrinal and its analogs as inhibitors of the GADD34:PP1 enzyme.

Authors:  Pavlo V Zadorozhnii; Ihor O Pokotylo; Vadym V Kiselev; Oxana V Okhtina; Aleksandr V Kharchenko
Journal:  ADMET DMPK       Date:  2019-04-05

8.  Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitors.

Authors:  Hannes C A Drexler
Journal:  PLoS One       Date:  2009-01-08       Impact factor: 3.240

9.  The HSV-1 mechanisms of cell-to-cell spread and fusion are critically dependent on host PTP1B.

Authors:  Jillian C Carmichael; Hiroki Yokota; Rebecca C Craven; Anthony Schmitt; John W Wills
Journal:  PLoS Pathog       Date:  2018-05-09       Impact factor: 6.823

  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.