Proteasome 20S

Proteasomes are protein complexes inside all eukaryotes and archaea, and in some bacteria which main function is to degrade unneeded or damaged proteins by proteolysis. The 26S proteasome is a eukaryotic ATP-dependent protease (EC 3.4.-) that is known to collaborate with the ubiquitin system,  the system that tags proteins with polyubiquitin chains as a marker for protein degradation in eukaryotic cells that degrades ubiquitin conjugates[1]. It consists of no less than 31 principal subunits arranged into two subcomplexes, the 20S core protease (CP) and the 19S regulatory particle (RP). The CP is a broad spectrum ATP- and ubiquitin-independent protease. It is a cylindrical stack created by the assembly of four heptameric rings. The two peripheral rings are composed of seven related α-subunits and the two central rings are composed of seven related β-subunits. The subunits have active sites with various hydrolase cleavage capacities, enabling the 26S proteasome to cleave most, if not all, peptide bonds[2]. Bortezomib (Axon 1810) is a specific inhibitor of 26S proteasome activity with approved application for use in multiple myeloma[3].

[1] S. Murata, H. Yashiroda, K. Tanaka. Molecular mechanisms of proteasome assembly. Nat. Rev. Mol. Cell Biol. 2009, 10, 104-115.
[2] J. Smalle, R.D. Vierstra. The ubiquitin 26S proteasome proteolytic pathway. Annu. Rev. Plant Biol. 2004, 55, 555-590.
[3] Mechanisms of Proteasome Inhibitor PS-341-induced G2-M-Phase Arrest and Apoptosis in Human Non-Small Cell Lung Cancer Cell Lines. Y Ling et al. Clin. Cancer Res. 2003, 9, 1145-1154.

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Axon ID Name Description From price
4218 Carfilzomib Irreversible proteasome inhibitor  Recently added Inquire
2556 MLN2238 Selective and reversible 20S proteasome inhibitor €85.00
2557 MLN9708 Citrate prodrug of MLN2238, selective and reversible 20S proteasome inhibitor €95.00
3849 Oprozomib Orally active and irreversible inhibitor of 20S proteasome Inquire

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