A novel proteasome inhibitor NPI-0052 as an anticancer therapy

Proteasome inhibitor Bortezomib/Velcade has emerged as an effective anticancer therapy for the treatment of relapsed and/or refractory multiple myeloma (MM), but prolonged treatment can be associated with toxicity and development of drug resistance. In this review, we discuss the recent discovery of...

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Autores principales: Chauhan, D, Hideshima, T, Anderson, K C
Formato: Texto
Lenguaje:English
Publicado: Nature Publishing Group 2006
Materias:
Minireview
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2360698/
https://www.ncbi.nlm.nih.gov/pubmed/17047643
http://dx.doi.org/10.1038/sj.bjc.6603406
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author Chauhan, D
Hideshima, T
Anderson, K C
author_facet Chauhan, D
Hideshima, T
Anderson, K C
author_sort Chauhan, D
collection PubMed
description Proteasome inhibitor Bortezomib/Velcade has emerged as an effective anticancer therapy for the treatment of relapsed and/or refractory multiple myeloma (MM), but prolonged treatment can be associated with toxicity and development of drug resistance. In this review, we discuss the recent discovery of a novel proteasome inhibitor, NPI-0052, that is distinct from Bortezomib in its chemical structure, mechanisms of action, and effects on proteasomal activities; most importantly, it overcomes resistance to conventional and Bortezomib therapies. In vivo studies using human MM xenografts shows that NPI-0052 is well tolerated, prolongs survival, and reduces tumour recurrence. These preclinical studies provided the basis for Phase-I clinical trial of NPI-0052 in relapsed/refractory MM patients.
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spelling pubmed-23606982009-09-10 A novel proteasome inhibitor NPI-0052 as an anticancer therapy Chauhan, D Hideshima, T Anderson, K C Br J Cancer Minireview Proteasome inhibitor Bortezomib/Velcade has emerged as an effective anticancer therapy for the treatment of relapsed and/or refractory multiple myeloma (MM), but prolonged treatment can be associated with toxicity and development of drug resistance. In this review, we discuss the recent discovery of a novel proteasome inhibitor, NPI-0052, that is distinct from Bortezomib in its chemical structure, mechanisms of action, and effects on proteasomal activities; most importantly, it overcomes resistance to conventional and Bortezomib therapies. In vivo studies using human MM xenografts shows that NPI-0052 is well tolerated, prolongs survival, and reduces tumour recurrence. These preclinical studies provided the basis for Phase-I clinical trial of NPI-0052 in relapsed/refractory MM patients. Nature Publishing Group 2006-10-23 2006-10-17 /pmc/articles/PMC2360698/ /pubmed/17047643 http://dx.doi.org/10.1038/sj.bjc.6603406 Text en Copyright © 2006 Cancer Research UK https://creativecommons.org/licenses/by/4.0/This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material.If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit https://creativecommons.org/licenses/by/4.0/.
spellingShingle Minireview
Chauhan, D
Hideshima, T
Anderson, K C
A novel proteasome inhibitor NPI-0052 as an anticancer therapy
title A novel proteasome inhibitor NPI-0052 as an anticancer therapy
title_full A novel proteasome inhibitor NPI-0052 as an anticancer therapy
title_fullStr A novel proteasome inhibitor NPI-0052 as an anticancer therapy
title_full_unstemmed A novel proteasome inhibitor NPI-0052 as an anticancer therapy
title_short A novel proteasome inhibitor NPI-0052 as an anticancer therapy
title_sort novel proteasome inhibitor npi-0052 as an anticancer therapy
topic Minireview
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2360698/
https://www.ncbi.nlm.nih.gov/pubmed/17047643
http://dx.doi.org/10.1038/sj.bjc.6603406
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