Preferred Label : LMP7 Inhibitor M3258;
NCIt synonyms : Immunoproteasome Inhibitor M3258;
NCIt definition : An orally bioavailable, potent, selective, reversible inhibitor of the large multifunctional
peptidase 7 (LMP7, Beta5i, PSMB8), a chymotrypsin-like, proteolytic subunit of the
immunoproteasome, with potential antineoplastic activity. Upon oral administration,
LMP7 inhibitor M3258 targets and inhibits the proteolytic activity of the LMP7 subunit
of immunoproteasome, thereby blocking its deubiquitylating activity. This blocks the
ubiquitin proteasome degradation pathway, prevents the degradation of defective proteins,
and leads to an accumulation of poly-ubiquitylated proteins. This induces the unfolded
protein response (UPR) and results in both the induction of tumor cell apoptosis and
the inhibition of tumor cell growth. Proteasomes are large multi-subunit protease
complexes that degrade unneeded or damaged proteins that have been ubiquitinated,
thereby restoring protein homeostasis. Unlike the constitutive proteasome, which is
expressed in most tissues, immunoproteasome is specifically present in normal and
malignant hematopoietic cells, including multiple myeloma. Immunoproteasome degrades
ubiquitinated proteins, generates peptides for presentation on MHC class I, and plays
a key role in the adaptive immune response and inflammatory diseases.;
Molecule name : M 3258; M-3258;
NCI Metathesaurus CUI : CL1378863;
Origin ID : C169060;
UMLS CUI : C5239352;
Semantic type(s)
- UMLS correspondences (same concept)
- M3258 [MeSH Supplementary Concept]
- concept_is_in_subset
- has_target
