EC Number |
Application |
Reference |
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6.2.1.45 | drug development |
the ubiquitin-activating enzyme E1 is a therapeutic target for the treatment of restenosis |
744190 |
6.2.1.45 | medicine |
functional foods, e.g. ginsenoside Rg1 in Panax ginseng root, targeting the ubiquitin-activating enzyme (E1) of the ubiquitin-proteasome pathway as anti-tumour agents are considered to be important for cancer chemoprevention |
734395 |
6.2.1.45 | 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 |
707854 |
6.2.1.45 | 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 |
707854 |
6.2.1.45 | medicine |
the ubiquitin-activating enzyme E1 is a therapeutic target for the treatment of restenosis |
744190 |
6.2.1.45 | synthesis |
510 mg of histidine-tagged mouse ubiquitin-activating enzyme E1 can be easily obtained from a 1 l Escherichia coli culture. A low temperature during the protein induction step is critical to obtain an active enzyme |
725950 |
6.2.1.45 | synthesis |
expression of the full length of human UBE1 in Escherichia coli and purification by Ni-NTA superflow sepharose and strep-tactin sepharose which is based on UB-UBE1 high-energy thioester bonded intermediate complex. Purified UBE1 can activate and conjugate UB to ubiquitin-conjugating enzyme E2s |
709881 |