Results 221 to 230 of about 107,253 (254)

Macrocyclic Proteasome Inhibitors

Current Medicinal Chemistry, 2011
Proteasome 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 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, Jacob P, Laubach, Teru, Hideshima, Dharminder, Chauhan, Kenneth C, Anderson, Paul G, Richardson   +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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Proteasome inhibitors as therapeutics

Essays in Biochemistry, 2005
The 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, Nicholas, Mitsiades, Teru, Hideshima, Paul G, Richardson, Kenneth C, Anderson   +4 more
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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, Beck, Philipp, Arciniega, Marcelino, Huber, Robert, Hillebrand, Stefan, Groll, Michael   +5 more
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Proteasome Inhibitor Drugs

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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Arecoline Tripeptide Inhibitors of Proteasome

Journal of Medicinal Chemistry, 2004
The 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, BALDISSEROTTO, Anna, CANELLA, Alessandro, GAVIOLI, Riccardo, DE RISI, Carmela, POLLINI, Gian Piero, TOMATIS, Roberto   +6 more
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Proteasome inhibitors

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, John McDonald, Anna Baldisserotto, Alessandro Canella, Carmela De Risi, Gian Piero Pollini, Roberto Tomatis   +6 more
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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, Patricia A, Messina McLaughlin, Derek, Dunn, Satish, Mallya, Jean, Husten, Mark A, Ator, Sankar, Chatterjee   +6 more
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Hypericin?an inhibitor of proteasome function

Cancer Chemotherapy and Pharmacology, 2005
Hypericin is the presumed active moiety within Saint John's wort. Extracts of Saint John's wort are widely used as an effective treatment for depression. Available as "over-the-counter" drugs, they are frequently part of the self-medication of patients undergoing radiation therapy for malignant diseases.
Pajonk, Frank-Gerald B., Scholber, Jutta Ursula, Fiebich, Bernd L.   +2 more
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