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Macrocyclic Proteasome Inhibitors
Current Medicinal Chemistry, 2011Proteasome inhibitors have proven to be effective anticancer agents. Despite the success of the first on the market proteasome inhibitor bortezomib in chemotherapy, alternative clinically useful proteasome inhibitors are still urgently needed as bortezomib therapy causes severe side effects and is limited by arising drug resistance.
Krahn, D., Ottmann, C., Kaiser, Markus
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Current Protocols in Immunology, 2015
AbstractProteasome inhibitors are indispensable research tools in immunology and cell biology. With numerous proteasome inhibitors available commercially, choosing the appropriate compound for a biological experiment may be challenging, especially for a novice. This unit provides an overview of the proteasome inhibitors commonly used in research.
Downey, S.L. +3 more
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AbstractProteasome inhibitors are indispensable research tools in immunology and cell biology. With numerous proteasome inhibitors available commercially, choosing the appropriate compound for a biological experiment may be challenging, especially for a novice. This unit provides an overview of the proteasome inhibitors commonly used in research.
Downey, S.L. +3 more
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Annual Review of Pharmacology and Toxicology, 2020
Proteasomes are large, multicatalytic protein complexes that cleave cellular proteins into peptides. There are many distinct forms of proteasomes that differ in catalytically active subunits, regulatory subunits, and associated proteins. Proteasome inhibitors are an important class of drugs for the treatment of multiple myeloma and mantle cell ...
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Proteasomes are large, multicatalytic protein complexes that cleave cellular proteins into peptides. There are many distinct forms of proteasomes that differ in catalytically active subunits, regulatory subunits, and associated proteins. Proteasome inhibitors are an important class of drugs for the treatment of multiple myeloma and mantle cell ...
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Gan to kagaku ryoho. Cancer & chemotherapy, 2004
Bortezomib, one of the proteasome inhibitors, has been approved in the United States for multiple myeloma as a second-line chemotherapy. In Japan, bortezomib has been used for for phase I clinical trials for multiple myeloma. As the action mechanism, it has been proposed that bortezomib inhibits NF-kappaB via IkappaB alpha.
Kiyohiko, Hatake +2 more
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Bortezomib, one of the proteasome inhibitors, has been approved in the United States for multiple myeloma as a second-line chemotherapy. In Japan, bortezomib has been used for for phase I clinical trials for multiple myeloma. As the action mechanism, it has been proposed that bortezomib inhibits NF-kappaB via IkappaB alpha.
Kiyohiko, Hatake +2 more
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Proteasome inhibitors as therapeutics
Essays in Biochemistry, 2005The ubiquitin–proteasome pathway is a principle intracellular mechanism for controlled protein degradation and has recently emerged as an attractive target for anticancer therapies, because of the pleiotropic cell-cycle regulators and modulators of apoptosis that are controlled by proteasome function. In this chapter, we review the current state of the
Constantine S, Mitsiades +4 more
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Non-Covalent Proteasome Inhibitors
Current Pharmaceutical Design, 2013Regulator of a vast array of vital cellular processes including cell-cycle progression, apoptosis and antigen presentation, the proteasome represents a major therapeutic target. Therefore, selective inhibitors of the proteasome are promising candidates to develop new treatments for diseases like inflammation, immune diseases and cancer.
Julia, Kaffy +2 more
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Proteasome inhibitors as anticancer agents
Expert Opinion on Therapeutic Patents, 2023The therapeutic targeting of the ubiquitin-proteasome pathway (UPP) through inhibitors of the 20S proteasome core proteolytic activities has revolutionized the treatment of hematological malignancies and is paving the way for its extension to solid tumors.This review covers the progress made in the field of proteasome inhibitors, ranging from the first-
Gazzaroli G. +3 more
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Hydroxyureas as Noncovalent Proteasome Inhibitors
Angewandte Chemie International Edition, 2011Inhibitors with a new mechanism of action are needed for 20S proteasome (CP) inhibition owing to the ineffectiveness of current market drugs against some types of solid tumors. A novel class of nonpeptidic CP inhibitors has been developed, which display reversible and noncovalent binding.
Gallastegui, Nerea +5 more
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Arecoline Tripeptide Inhibitors of Proteasome
Journal of Medicinal Chemistry, 2004The 26S proteasome is a multicatalytic protease complex that plays an essential role in intracellular protein degradation. We have synthesized and tested a series of arecoline peptide derivatives where the peptide portion derives from a screening of tripeptide sequences, and the arecoline moiety has been considered as a potential substrate for ...
MARASTONI, Mauro +6 more
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Nihon rinsho. Japanese journal of clinical medicine, 2010
The ubiquitin-proteasome pathway plays an important role in the regulation of cellular proteins with regard to cell cycle control, transcription, apoptosis, cell adhesion, angiogenesis and tumor growth. Proteasome inhibition is a novel approach to the treatment of solid tumors.
Masahiro, Yamamura +2 more
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The ubiquitin-proteasome pathway plays an important role in the regulation of cellular proteins with regard to cell cycle control, transcription, apoptosis, cell adhesion, angiogenesis and tumor growth. Proteasome inhibition is a novel approach to the treatment of solid tumors.
Masahiro, Yamamura +2 more
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