Literature DB >> 29068506

Click Chemistry: Novel Applications in Cell Biology and Drug Discovery.

Matthias Gehringer1, Stefan A Laufer1.   

Abstract

A safe BET: Apart from target engagement, subcellular location and tissue distribution are critical parameters in drug discovery. A novel, generalizable approach has been reported that involves exploiting click chemistry to elucidate these parameters. By using clickable analogues of known Bromodomain and extraterminal domain (BET) inhibitors, various labels were introduced in situ and utilized to determine the biological fate of these probes.
© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Keywords:  bromodomains; click chemistry; drug discovery; fluorescent probes; inhibitors

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Year:  2017        PMID： 29068506     DOI： 10.1002/anie.201710195

Source DB:  PubMed          Journal:  Angew Chem Int Ed Engl        ISSN： 1433-7851            Impact factor:   15.336


  5 in total

1.  (Radio)fluoroclick Reaction Enabled by a Hydrogen-Bonding Cluster.

Authors:  Xiaojun Zeng; Junling Li; Chin K Ng; Gerald B Hammond; Bo Xu
Journal:  Angew Chem Int Ed Engl       Date:  2018-02-13       Impact factor: 15.336

2.  Chemoenzymatic route to stereodefined 2-(azidophenyl)oxazolines for click chemistry.

Authors:  Paige J Monsen; Frederick A Luzzio
Journal:  Tetrahedron Lett       Date:  2020-12-17       Impact factor: 2.415

3.  'Second-generation' 1,2,3-triazole-based inhibitors of Porphyromonas gingivalis adherence to oral streptococci and biofilm formation.

Authors:  Pravin C Patil; Jinlian Tan; Donald R Demuth; Frederick A Luzzio
Journal:  Medchemcomm       Date:  2019-01-15       Impact factor: 3.597

4.  Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury.

Authors:  Tianpeng Chen; Yingying Wei; Gaoyang Zhu; Huajun Zhao; Xingxian Zhang
Journal:  Eur J Med Chem       Date:  2021-08-12       Impact factor: 6.514

5.  Design and Synthesis of (2-oxo-1,2-Dihydroquinolin-4-yl)-1,2,3-triazole Derivatives via Click Reaction: Potential Apoptotic Antiproliferative Agents.

Authors:  Essmat M El-Sheref; Mohammed A I Elbastawesy; Alan B Brown; Ahmed M Shawky; Hesham A M Gomaa; Stefan Bräse; Bahaa G M Youssif
Journal:  Molecules       Date:  2021-11-10       Impact factor: 4.411
  5 in total

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