A Small Molecule Tubulin Depolymerizing Agent Identified by a Phenotypic Drug Discovery Approach

  1. José M.Padrón 1
  2. Elena Díaz-Rodríguez 2
  3. Rubén M. Buey 3
  4. Carla Ríos Luci 1
  5. Miguel X. Fernandes 1
  6. Atanasio Pandiella 2
  7. Inês J. Sousa 4
  1. 1 Universidad de La Laguna
    info

    Universidad de La Laguna

    San Cristobal de La Laguna, España

    GRID grid.10041.34

  2. 2 Instituto de Biología Molecular y Celular del Cáncer de Salamanca / Centro de Investigación del Cáncer
    info

    Instituto de Biología Molecular y Celular del Cáncer de Salamanca / Centro de Investigación del Cáncer

    Salamanca, España

    GRID grid.428472.f

  3. 3 Universidad de Salamanca
    info

    Universidad de Salamanca

    Salamanca, España

    GRID grid.11762.33

  4. 4 University of Madeira
    info

    University of Madeira

    Funchal, Portugal

    GRID grid.26793.39

Journal:
Journal of Molecular and Clinical Medicine

ISSN: 2616-3632

Year of publication: 2018

Volume: 1

Issue: 2

Pages: 67-76

Type: Article

Export: RIS
DOI: 10.31083/j.jmcm.2018.02.003 GOOGLE SCHOLAR lock_openOpen access editor

Abstract

In the scenario of drug discovery, numerousin vitrotesting initiatives had been established. Thus far, no general methodology isreputable and literature on this hot topic is scarce. In this respect, we propose a strategy based on a Phenotypic Drug Discoveryapproach. Within our program directed at the discovery of new antitumor agents, we have focused our attention on compoundsthat disturb the cell cycle. Our strategy relies on the use of a set of biological assays organized in a modular fashion. Herein, weexemplified this strategy with a family of propargylic enol ether derivatives. Using different assays in sequential stages and in astepwise manner, our studies allowed us to understand the bioactivity of this family of compounds and led us to identify tubulinas the main molecular target.

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