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Proteasome inhibitor information


Chemical structure of bortezomib, the first proteasome inhibitor approved for use.

Proteasome inhibitors (INN stem –zomib)[1] are drugs that block the action of proteasomes, cellular complexes that break down proteins. They are being studied in the treatment of cancer; three are approved for use in treating multiple myeloma.

  1. ^ "The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances" (PDF). World Health Organization. Retrieved 5 November 2016.

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Proteasome inhibitor

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non-peptidic proteasome inhibitor discovered was the natural product lactacystin. Disulfiram has been proposed as another proteasome inhibitor. Epigallocatechin-3-gallate...

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Proteasome

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seem to justify use of proteasome inhibitor combined with chemotherapy, for B-cell acute lymphoblastic leukemia Proteasome inhibitors can kill some types...

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Bortezomib

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syndrome. It is in the class of medications known as proteasome inhibitor. It works by inhibiting proteasomes, cellular complexes that break down proteins. Bortezomib...

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Multiple myeloma

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anti-CD38 monoclonal antibody, a proteasome inhibitor, and an immunomodulatory agent. carfilzomib: a proteasome inhibitor that is indicated: as a single...

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Carfilzomib

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name Kyprolis, is an anti-cancer medication acting as a selective proteasome inhibitor. Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin...

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MG132

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MG132 is a potent, reversible, and cell-permeable proteasome inhibitor (Ki = 4 nM). It belongs to the class of synthetic peptide aldehydes. It reduces...

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Epoxomicin

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Epoxomicin is a naturally occurring selective proteasome inhibitor with anti-inflammatory activity. It was originally discovered in 1992. Injected, it...

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Talquetamab

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multiple myeloma who have received prior lines of therapy, including a proteasome inhibitor, an immunomodulatory agent, and an anti-CD38 monoclonal antibody...

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Salinosporamide A

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Salinosporamide A (Marizomib) is a potent proteasome inhibitor being studied as a potential anticancer agent. It entered phase I human clinical trials...

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Elranatamab

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have received at least four prior lines of therapy, including a proteasome inhibitor, an immunomodulatory agent, and an anti-CD38 monoclonal antibody...

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Lactacystin

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certain protein substrates. Lactacystin was the first non-peptidic proteasome inhibitor discovered and is widely used as a research tool in biochemistry...

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Isatuximab

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received at least two prior therapies including lenalidomide and a proteasome inhibitor. It is also indicated in combination with carfilzomib and dexamethasone...

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Ixazomib

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bortezomib (which can only be given by injection), it acts as a proteasome inhibitor, has orphan drug status in the US and Europe, and is a boronic acid...

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Oprozomib

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second-generation proteasome inhibitor developed by Proteolix, which was acquired by Onyx Pharmaceuticals, an Amgen subsidiary, in 2009. It selectively inhibits chymotrypsin-like...

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Proteolix

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orally-bioavailable proteasome inhibitor for oncology (PR-047), and an agent preferentially targeting the immuno form of the proteasome (PR-957), with potential...

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Ciltacabtagene autoleucel

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multiple myeloma after four or more prior lines of therapy, including a proteasome inhibitor, an immunomodulatory agent, and an anti-CD38 monoclonal antibody...

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Disulfiram

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"The value of proteasome inhibition in cancer. Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor?". Drug Discovery...

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Proteostasis

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proteins that accumulate, and the function these proteins have. Proteasome inhibitor bortezomib was the first drug of this type to receive approval for...

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Takeda Oncology

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other therapies for the disease. Velcade — the first FDA-approved proteasome inhibitor — reached the market in record time and represented the first treatment...

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GNF6702

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parasites, which share similar biology. GNF6702 acts as allosteric proteasome inhibitor which was effective against infection with any of the three protozoal...

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Siddhartha Mukherjee

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D.; Schoonmaker, J. A.; Mulay, S.; et al. (2010). "A Proteasome Inhibitor, Bortezomib, Inhibits Breast Cancer Growth and Reduces Osteolysis by Downregulating...

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Melphalan flufenamide

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lines of therapy and whose disease is refractory to at least one proteasome inhibitor, one immunomodulatory agent, and one CD-38 directed monoclonal antibody...

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ATC code L01

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acid Dihydrofolate reductase inhibitor (Aminopterin Methotrexate# Pemetrexed Pralatrexate) Thymidylate synthase inhibitor (Pemetrexed Raltitrexed) Purine...

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Daratumumab

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and refractory multiple myeloma, whose prior therapy included a proteasome inhibitor and an immunomodulatory agent and who have demonstrated disease progression...

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