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Related Concept Videos

Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

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Related Experiment Video

Updated: May 9, 2026

A Strategy to Identify Compounds that Affect Cell Growth and Survival in Cultured Mammalian Cells at Low-to-Moderate Throughput
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Published on: September 22, 2019

Structure-guided identification of small molecules potentially able to modulate GDF15 activity.

Antonio Chiariello1, Lorenzo Lenti2, Lorenzo Trofarello1

  • 1Department of Medical and Surgical Sciences (DIMEC), University of Bologna, 40126, Bologna, Italy.

Scientific Reports
|May 7, 2026
PubMed
Summary

Small organic molecules (SOMs) can inhibit Growth Differentiation Factor 15 (GDF15). A novel SOM, SOM D, disrupted GDF15 dimers and modulated downstream signaling in cancer cells, showing therapeutic potential.

Keywords:
GDF15Ovarian cancer cellsSmall organic moleculesVirtual screening

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Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
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Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library

Published on: September 30, 2019

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Last Updated: May 9, 2026

A Strategy to Identify Compounds that Affect Cell Growth and Survival in Cultured Mammalian Cells at Low-to-Moderate Throughput
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Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
07:32

Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library

Published on: September 30, 2019

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Growth Differentiation Factor 15 (GDF15) is implicated in pathological conditions like cancer cachexia.
  • Current GDF15 inhibitors include monoclonal antibodies and peptide antagonists.
  • The potential of small organic molecules (SOMs) to target GDF15 remains unexplored.

Purpose of the Study:

  • To identify SOMs capable of inhibiting GDF15 activity.
  • To evaluate the efficacy of identified SOMs in vitro and in cellular models.
  • To assess the therapeutic potential of SOMs as GDF15 inhibitors.

Main Methods:

  • Structure-based in silico screening of a compound library against GDF15.
  • In vitro testing of top-ranking SOMs in acellular systems.
  • In vitro testing in normal (dermal fibroblasts) and cancer (ovarian) cells with varying GDF15 expression.

Main Results:

  • A dioxoimidazolidin derivative (SOM D) showed promise in inhibiting GDF15.
  • SOM D disrupted GDF15 dimer stability and GDF15-GFRAL interaction.
  • SOM D modulated downstream GDF15 signaling (IL-6, NF-κB) in ovarian cancer cells.

Conclusions:

  • GDF15 activity can be modulated by SOMs.
  • SOM D demonstrates potential as a GDF15 inhibitor.
  • Further optimization and studies are warranted to assess therapeutic potential.