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Novel proteasome inhibitors

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
openaire   +1 more source

[Proteasome inhibitors].

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
openaire   +1 more source

The proteasome and proteasome inhibitors in multiple myeloma

Cancer and Metastasis Reviews, 2017
Proteasome 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
openaire   +2 more sources

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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New cyclic peptide proteasome inhibitors

Bioorganic & Medicinal Chemistry Letters, 2009
Here we report the study of a new series of vinyl ester cyclopeptide analogues synthesized on the basis of our previous development of a class of cyclopeptides derived from our linear prototype inhibitors. In these compounds, the exocyclic pharmacophoric unit Leu-VE was linked to the gamma-carboxyl group of the glutamic acid residue at the C-terminal ...
BALDISSEROTTO, Anna   +3 more
openaire   +3 more sources

Proteasome inhibitors for cancer therapy

Bioorganic & Medicinal Chemistry, 2012
Proteasome, a large multicatalytic proteinase complex that plays an important role in processing of proteins, has been shown to possess multiple catalytic activities. Among its various activities, the 'chymotrypsin-like' activity of proteasome has emerged as the focus of drug discovery efforts in cancer therapy. Herein we report chiral boronate derived
Mohamed, Iqbal   +6 more
openaire   +2 more sources

Proteasome inhibitor patents (2010 – present)

Expert Opinion on Therapeutic Patents, 2014
Over the past 3 years, numerous patents and patent applications have been submitted and published involving compounds designed to inhibit the proteasome. Proteasome inhibition has been of great interest in cancer research since disruption of proteolysis leads to a significant buildup of cytotoxic proteins and activation of apoptotic pathways ...
Rainer, Metcalf   +3 more
openaire   +2 more sources

Proteasome Inhibitors

Oncology (Williston Park, N.Y.), 2008
Dharminder Chauhan, Kenneth C. Anderson
openaire   +3 more sources

[Proteasome inhibitor].

Nihon rinsho. Japanese journal of clinical medicine, 2014
The ubiquitin-proteasome system plays an essential role in degradation of eukaryotic intracellular protein, including cell cycle regulation, cell growth and proliferation, and survival. Cancer cells generally have higher level of proteasome activity compared with normal cells, suggesting proteasome inhibition could be therapeutic target in oncology ...
openaire   +1 more source

Proteasome inhibitors in lung cancer

Critical Reviews in Oncology/Hematology, 2006
Proteasome inhibition is a novel therapeutic approach that is being investigated in non-small cell and small cell lung cancer (NSCLC and SCLC). Proteasome inhibition affects a range of intracellular signals and disrupts the levels of numerous proteins, causing apoptosis via multiple pathways.
openaire   +3 more sources

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