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Literature summary for 6.2.1.45 extracted from

  • Yang, Y.; Kitagaki, J.; Dai, R.M.; Tsai, Y.C.; Lorick, K.L.; Ludwig, R.L.; Pierre, S.A.; Jensen, J.P.; Davydov, I.V.; Oberoi, P.; Li, C.C.; Kenten, J.H.; Beutler, J.A.; Vousden, K.H.; Weissman, A.M.
    Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics (2007), Cancer Res., 67, 9472-9481.
    View publication on PubMed
Search for more literature for 6.2.1.45

Inhibitors

Inhibitors Comment Organism Structure
4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester i.e. Pyr-41. Inhibitor blocks loading of immobilized His6-tagged E1 with ubiquitin. PYR-41 does not affect the transfer of ubiquitin to E2 from E1 that is preloaded with ubiquitin, it directly inhibits E1, but not E2 enzymes. In addition to blocking ubiquitylation, PYR-41 increases total sumoylation in cells. PYR-41 attenuates cytokine-mediated nuclear factor-kappaB activation. This correlates with inhibition of nonproteasomal Lys63 ubiquitylation of TRAF6, which is essential to IkappaB kinase activation Homo sapiens
4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester i.e. PYR-41, potential of the inhibitor as therapeutic in cancer Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
2B4-T cell
-
 Homo sapiens
-
A-9 cell
-
 Homo sapiens
-
HEK-293 Tet-On 3G cell
-
 Homo sapiens
-
HeLa cell
-
 Homo sapiens
-
JURKAT cell
-
 Homo sapiens
-
L-929 cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
ubiquitin-activating enzyme E1
-
 Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
 inhibitor blocks loading of immobilized His6-tagged E1 with ubiquitin with an IC50 below 10 microM Homo sapiens 4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester