Abstract
Protein-protein interactions (PPIs) can be useful targets for different pathologies. In fact controlling a function or attempting to repair an anomaly often means interfering with the cross-talk among different proteins. In order to have a general view of these cross-talks, Molecular Interaction Maps (MIMs) are used, organizing the enormous available information that is added every day and trying to understand the most suitable and accurate targets for any specific cell alteration. In this paper the c-Myc protein is taken as an example to explain the use of a map. The discovery of a peptidomimetic antagonist of c-Myc, active against proliferation of cancer cell lines, is reported and a possible mechanism of action is explained. To interfere with a specific protein-protein contact, a good starting point can be to consider a protein entity. Because the interaction between two proteins is normally characterized by a wide zone of contact, relative large inhibitors could be more convenient in the first approaches. Therefore, peptides mimicking the interacting zone can be considered as potential leads in the rational design of effective molecules. Here different examples of peptides as protein-protein interaction inhibitors are reported.
Keywords: Protein-protein interactions (PPIs), molecular interaction maps (MIMs), peptides, c-Myc
Current Topics in Medicinal Chemistry
Title: Interfering with Protein-Protein Contact: Molecular Interaction Maps and Peptide Modulators
Volume: 7 Issue: 1
Author(s): Erika Nieddu and Stefania Pasa
Affiliation:
Keywords: Protein-protein interactions (PPIs), molecular interaction maps (MIMs), peptides, c-Myc
Abstract: Protein-protein interactions (PPIs) can be useful targets for different pathologies. In fact controlling a function or attempting to repair an anomaly often means interfering with the cross-talk among different proteins. In order to have a general view of these cross-talks, Molecular Interaction Maps (MIMs) are used, organizing the enormous available information that is added every day and trying to understand the most suitable and accurate targets for any specific cell alteration. In this paper the c-Myc protein is taken as an example to explain the use of a map. The discovery of a peptidomimetic antagonist of c-Myc, active against proliferation of cancer cell lines, is reported and a possible mechanism of action is explained. To interfere with a specific protein-protein contact, a good starting point can be to consider a protein entity. Because the interaction between two proteins is normally characterized by a wide zone of contact, relative large inhibitors could be more convenient in the first approaches. Therefore, peptides mimicking the interacting zone can be considered as potential leads in the rational design of effective molecules. Here different examples of peptides as protein-protein interaction inhibitors are reported.
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Cite this article as:
Nieddu Erika and Pasa Stefania, Interfering with Protein-Protein Contact: Molecular Interaction Maps and Peptide Modulators, Current Topics in Medicinal Chemistry 2007; 7 (1) . https://dx.doi.org/10.2174/156802607779318271
DOI https://dx.doi.org/10.2174/156802607779318271 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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