[Proteasome inhibitors in cancer therapy].
Proteasomes are multisubunit enzyme complexes. They contain three enzymatic active sites which are termed chymotrypsin-like, trypsin-like, and caspase-like. The elementary function of the proteasomes is degradation of damaged proteins. Proteasome inhibition leads to accumulation of damaged protein, which leads to caspase activation and cell death. This relationship is used in cancer therapy. Bortezomib is the first proteasome inhibitor approved by the US Food and Drug Administration for the treatment of relapsed/refractory multiple myeloma. Carfilzomib belongs to the second generation of drugs, which was approved by the US FDA in 2012. Currently in the study phase there are four new inhibitors: ixazomib (MLN9780/MLN2238), delanzomib (CEP-18770), oprozomib (ONX0912/PR-047) and marizomib (NPI-0052).
Klinika Hematologii z Pododdziałem Chorób Naczyń, Uniwersytet Medyczny w Białymstoku.
Wioletta
W
Romaniuk
Klinika Hematologii z Pododdziałem Chorób Naczyń, Uniwersytet Medyczny w Białymstoku.
Agnieszka Ewa
AE
Ołdziej
Zakład Patomorfologii Ogólnej, Uniwersytet Medyczny w Białymstoku.
Justyna
J
Zińczuk
Klinika Hematologii z Pododdziałem Chorób Naczyń, Uniwersytet Medyczny w Białymstoku.
Janusz
J
Kłoczko
D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D001897:Boronic Acids / Q000627:therapeutic use; D000069286:Bortezomib / Q000627:therapeutic use; D020169:Caspases / Q000378:metabolism; D004151:Dipeptides; D006801:Humans; D007783:Lactones / Q000627:therapeutic use; D009101:Multiple Myeloma / Q000188:drug therapy; D009369:Neoplasms / Q000188:drug therapy*; D009842:Oligopeptides / Q000627:therapeutic use; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D061988:Proteasome Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D059748:Proteolysis; D011758:Pyrroles / Q000627:therapeutic use; D013844:Thiazoles; D013912:Threonine / Q000031:analogs & derivatives / Q000627:therapeutic use
C540947:3-methoxy-2-(3-methoxy-2-((2-methyl-1,3-thiazol-5-yl)formamido)propanamido)-N-(1-(2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)propanamide; D000970:Antineoplastic Agents; D001897:Boronic Acids; D004151:Dipeptides; D007783:Lactones; D009842:Oligopeptides; D061988:Proteasome Inhibitors; D011758:Pyrroles; D013844:Thiazoles; D013912:Threonine; D000069286:Bortezomib; C527966:delanzomib; C475865:marizomib; C524865:carfilzomib; D020169:Caspases; D046988:Proteasome Endopeptidase Complex