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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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Bortezomib: a proteasome inhibitor for the treatment of autoimmune diseases
InflammoPharmacology, 2021Naeemeh Khalesi +4 more
semanticscholar +1 more source
Hematology Meeting Reports, 2009
The ubiquitin proteasome pathway plays a central role in controlling intracellular turnover of proteins regulating cell growth and survival, stress responses, apoptosis and cell cycle.1 Proteasome inhibitors were initially developed in order to investigate the mechanisms of cellular proteolysis; early studies, however, showed that these compounds ...
P Tosi +3 more
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The ubiquitin proteasome pathway plays a central role in controlling intracellular turnover of proteins regulating cell growth and survival, stress responses, apoptosis and cell cycle.1 Proteasome inhibitors were initially developed in order to investigate the mechanisms of cellular proteolysis; early studies, however, showed that these compounds ...
P Tosi +3 more
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Nihon rinsho. Japanese journal of clinical medicine, 2010
The 26S proteasome is a multicatalytic enzyme responsible for degradation of a large fraction of intracellular proteins. Targeting the proteasome activity is a rational and novel strategy for cancer therapy that can lead to cell death for transformed cells.
Yasushi, Saeki +2 more
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The 26S proteasome is a multicatalytic enzyme responsible for degradation of a large fraction of intracellular proteins. Targeting the proteasome activity is a rational and novel strategy for cancer therapy that can lead to cell death for transformed cells.
Yasushi, Saeki +2 more
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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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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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