ENGÜR, Selin Anadolu Üniversitesi - Sağlık Bilimleri Enstitüsü - Farmakoloji ABD, Turkey , DİKMEN, Miriş Anadolu Üniversitesi - Eczacılık Fakültesi - Farmakoloji ABD, Turkey

The Importance of Proteasome Inhibitors in Cancer Therapy

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In recent years the ubiquitin–proteasome system has been identified as essential for maintaining a important balance between cell growth and death, the progression of human malignancies, and the development of drug resistance in cancer. Inhibition of proteasome function has emerged as strong strategy for anti-cancer therapy. Clinical confirmation of the proteasome as a therapeutic target was achieved with bortezomib which is the first proteasome inhibitor to be implemented in the treatment of malignant disease and has prompted the development of a second generation of proteasome inhibitors with improved pharmacological properties. Other novel proteasome inhibitors, such as ixazomib, delanzomib, oprozomib and marizomib, have recently been developed and are being tested in clinical trials. This review summarises the main mechanisms of action of proteasome inhibitors in cancer especially inhibition of NF-κB, the development of proteasome inhibitors as therapeutic agents and the properties and progress of next generation proteasome inhibitors in the clinic.

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Bortezomib , cancer , NF , κB , Proteasome inhibitor

Erciyes University Journal Of The Institute Of Science an‎d Technology

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