Literature summary for 3.4.25.1 extracted from

Roccaro, A.M.; Sacco, A.; Aujay, M.; Ngo, H.T.; Azab, A.K.; Azab, F.; Quang, P.; Maiso, P.; Runnels, J.; Anderson, K.C.; Demo, S.; Ghobrial, I.M.
Selective inhibition of chymotrypsin-like activity of the immunoproteasome and constitutive proteasome in Waldenstrom macroglobulinemia (2010), Blood, 115, 4051-4060.

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Inhibitors

Inhibitors	Comment	Organism	Structure
bortezomib	ONX0912 acts synergistically with bortezomib	Homo sapiens
ONX0912	a selective, irreversible inhibitor of the chymotrypsin-like activity of constitutive proteasome 20S and immunoproteasome 20S. ONX0912 exerts toxicity in Waldenstroem macroglobulinemia cells, by reducing bone marrow-derived interleukin-6 and insulin-like growth factor 1 secretion, thus inhibiting BM-induced p-Akt and phosphorylated extracellular signal-related kinase activation in Waldenstroem macroglobulinemia cells, overview. ONX0912 acts synergistically with bortezomib	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
BCWM.1 cell	-	Homo sapiens	-
bone marrow	primary Waldenstroem macroglobulinemia cells	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O	chymotrypsin-like proteasome activity	Homo sapiens	N-succinyl-LLVY + 7-amino-4-methylcoumarin	-	?

Synonyms

Synonyms	Comment	Organism
c20S	-	Homo sapiens
constitutive proteasome 20S	-	Homo sapiens
i20S	-	Homo sapiens
immunoproteasome 20S	-	Homo sapiens

General Information

General Information	Comment	Organism
additional information	primary Waldenstroem macroglobulinemia cells express higher level of immunoproteasome 20S compared with constitutive proteasome 20S. Selective inhibition of the chymotrypsin-like activity of constitutive proteasome 20S and immunoproteasome 20S represents a sufficient and successful strategy to induce antineoplastic effect in hematologic tumors	Homo sapiens

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Release 2023.1 (January 2023)