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Literature summary for 6.2.1.45 extracted from

  • Xu, G.W.; Ali, M.; Wood, T.E.; Wong, D.; Maclean, N.; Wang, X.; Gronda, M.; Skrtic, M.; Li, X.; Hurren, R.; Mao, X.; Venkatesan, M.; Beheshti Zavareh, R.; Ketela, T.; Reed, J.C.; Rose, D.; Moffat, J.; Batey, R.A.; Dhe-Paganon, S.; Schimmer, A.D.
    The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma (2010), Blood, 115, 2251-2259.
    View publication on PubMedView publication on EuropePMC
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Application

Application Comment Organism
medicine in a mouse model of leukemia, intraperitoneal administration of inhibitor 1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione, i.e. PYZD-4409, decreases tumor weight and volume compared with control without untoward toxicity Mus musculus
medicine knockdown of E1 decreases the abundance of ubiquitinated proteins in leukemia and myeloma cells and induces cell death. Inhibitor 1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione, i.e. PYZD-4409, induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells compared with normal hematopoietic cells. Mechanistically, genetic or chemical inhibition of E1 increases expression of E1 stress markers. ER membrane protein BI-1 overexpression blocks cell death after E1 inhibition Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione i.e. PYZD-4409, small molecule inhibitor. PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells compared with normal hematopoietic cells Homo sapiens
1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione i.e. PYZD-4409. In a mouse model of leukemia, intraperitoneal administration of PYZD-4409 decreases tumor weight and volume compared with control without untoward toxicity Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Mus musculus
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Source Tissue

Source Tissue Comment Organism Textmining
leukemia cell
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 Homo sapiens
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additional information primary leukemia and multiple myolema patient samples Homo sapiens
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General Information

General Information Comment Organism
physiological function knockdown of E1 decreases the abundance of ubiquitinated proteins in leukemia and myeloma cells and induces cell death. Inhibitor 1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione, i.e. PYZD-4409, induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells compared with normal hematopoietic cells. Mechanistically, genetic or chemical inhibition of E1 increases expression of E1 stress markers. ER membrane protein BI-1 overexpression blocks cell death after E1 inhibition Homo sapiens