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

    ROR https://ror.org/01r9z8p25

  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

    ROR https://ror.org/04rxrdv16

  3. 3 Universidad de Salamanca
    info

    Universidad de Salamanca

    Salamanca, España

    ROR https://ror.org/02f40zc51

  4. 4 Universidade da Madeira
    info

    Universidade da Madeira

    Funchal, Portugal

    ROR https://ror.org/0442zbe52

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Journal:
Journal of Molecular and Clinical Medicine

ISSN: 2616-3632,  2617-5282

Year of publication: 2018

Volume: 1

Issue: 2

Pages: 67-76

Type: Article

DOI: 10.31083/J.JMCM.2018.02.003 GOOGLE SCHOLAR lock_openOpen access editor

More publications in: Journal of Molecular and Clinical Medicine

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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