Results 241 to 250 of about 752,942 (288)
Hydroxyureas as Noncovalent Proteasome Inhibitors
Angewandte Chemie International Edition, 2011 Inhibitors 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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Proteasome inhibitors as anticancer agents
Expert Opinion on Therapeutic Patents, 2023 Introduction: The 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 ...
Roberto Ronca +2 more
exaly +2 more sources
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Materials and Methods, 2012
In May 2003, the US Food and Drug Administration (FDA) granted accelerated approval for the use of the first-in-class proteasome inhibitor bortezomib as a third-line therapy in multiple myeloma, and the European Union followed suit a year later. Bortezomib has subsequently been approved for multiple myeloma as a second-line treatment on its own and as ...
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In May 2003, the US Food and Drug Administration (FDA) granted accelerated approval for the use of the first-in-class proteasome inhibitor bortezomib as a third-line therapy in multiple myeloma, and the European Union followed suit a year later. Bortezomib has subsequently been approved for multiple myeloma as a second-line treatment on its own and as ...
+5 more sources
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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THE PROTEASOME AND PROTEASOME INHIBITORS IN CANCER THERAPY
Annual Review of Pharmacology and Toxicology, 2006▪ Abstract The proteasome, a multicatalytic proteinase complex, is responsible for the majority of intracellular protein degradation. Pharmacologic inhibitors of the proteasome possess in vitro and in vivo antitumor activity, and bortezomib, the first such agent to undergo clinical testing, has significant efficacy against multiple myeloma and non ...
Peter M, Voorhees, Robert Z, Orlowski
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The proteasome and proteasome inhibitors in multiple myeloma
Cancer and Metastasis Reviews, 2017Proteasome inhibitors are one of the most important classes of agents to have emerged for the treatment of multiple myeloma in the past two decades, and now form one of the backbones of treatment. Three agents in this class have been approved by the United States Food and Drug Administration-the first-in-class compound bortezomib, the second-generation
Sara, Gandolfi +5 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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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 ...
openaire +2 more sources
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 ...
openaire +2 more sources
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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Bioorganic & Medicinal Chemistry Letters, 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.
Mauro Marastoni +6 more
openaire +3 more sources
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.
Mauro Marastoni +6 more
openaire +3 more sources