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Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells

The involvement of the ubiquitin–proteasome pathway in the degradation of critical intracellular regulatory proteins suggested a few years ago the potential use of proteasome inhibitors as novel therapeutic agents being applicable in many different disease indications, and in particular for cancer t...

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Detalles Bibliográficos
Autor principal: García-Echeverría, Carlos
Formato: Texto
Lenguaje:English
Publicado: Kluwer Academic Publishers 2006
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2710986/
https://www.ncbi.nlm.nih.gov/pubmed/19617921
http://dx.doi.org/10.1007/s10989-005-9001-4
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author García-Echeverría, Carlos
author_facet García-Echeverría, Carlos
author_sort García-Echeverría, Carlos
collection PubMed
description The involvement of the ubiquitin–proteasome pathway in the degradation of critical intracellular regulatory proteins suggested a few years ago the potential use of proteasome inhibitors as novel therapeutic agents being applicable in many different disease indications, and in particular for cancer therapy. This article reviews recent salient medicinal chemistry achievements in the design, synthesis, and biological characterization of both synthetic and natural peptide-like proteasome inhibitors, updating recent reviews on this class of agents. As shown herein, different compound classes are capable of modulating the subunit-specific proteolytic activities of the 20S proteasome in ways not previously possible, and one of them, bortezomib, has provided proof-of-concept for this therapeutic approach in cancer clinical settings.
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spelling pubmed-27109862009-07-16 Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells García-Echeverría, Carlos Int J Pept Res Ther Article The involvement of the ubiquitin–proteasome pathway in the degradation of critical intracellular regulatory proteins suggested a few years ago the potential use of proteasome inhibitors as novel therapeutic agents being applicable in many different disease indications, and in particular for cancer therapy. This article reviews recent salient medicinal chemistry achievements in the design, synthesis, and biological characterization of both synthetic and natural peptide-like proteasome inhibitors, updating recent reviews on this class of agents. As shown herein, different compound classes are capable of modulating the subunit-specific proteolytic activities of the 20S proteasome in ways not previously possible, and one of them, bortezomib, has provided proof-of-concept for this therapeutic approach in cancer clinical settings. Kluwer Academic Publishers 2006-03-04 2006-03 /pmc/articles/PMC2710986/ /pubmed/19617921 http://dx.doi.org/10.1007/s10989-005-9001-4 Text en © Springer Science+Business Media, Inc. 2006
spellingShingle Article
García-Echeverría, Carlos
Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells
title Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells
title_full Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells
title_fullStr Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells
title_full_unstemmed Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells
title_short Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells
title_sort peptide and peptide-like modulators of 20s proteasome enzymatic activity in cancer cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2710986/
https://www.ncbi.nlm.nih.gov/pubmed/19617921
http://dx.doi.org/10.1007/s10989-005-9001-4
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