6.2.1.45: E1 ubiquitin-activating enzyme

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For detailed information about E1 ubiquitin-activating enzyme, go to the full flat file.

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Synonyms

AtUBA1, AtUBA2, E1, E1 ubiquitin-activating enzyme, HsUba1a, non-canonical ubiquitin activating enzyme, SUMO E1, UB activating enzyme, Ub E1 activating enzyme, Ub-activating enzyme, Ub-activating ligase, Uba1, Uba1/E1, Uba1a, UBA1p, UBA2, UBA5, Uba6, UBA7, UBE1, UBE1DC1, UBE1DC1A, UBE1DC1B, UBE1L, UBE1L2, ubiquitin activating enzyme, ubiquitin activating enzyme 2, ubiquitin activating enzyme E1, ubiquitin activating enzyme E1-like, ubiquitin E1, ubiquitin protein ligase E1, Ubiquitin-activating enzyme, ubiquitin-activating enzyme (E1), ubiquitin-activating enzyme 1, ubiquitin-activating enzyme 5, ubiquitin-activating enzyme 6, ubiquitin-activating enzyme E1, ubiquitin-activating enzyme E1 domain-containing protein 1, ubiquitin-activating enzyme E1-domain containing 1, ubiquitin-activating enzyme, UBE1, ubiquitin-conjugating enzyme, ubiquitin-like modifier-activating enzyme 1, ubiquitin-like modifier-activating enzyme 5, ubiquitin-like modifier-activating enzyme 6, ubiquitin-like modifier-activating enzyme 7 isoform X2

ECTree

     6 Ligases

         6.2 Forming carbon-sulfur bonds

             6.2.1 Acid-thiol ligases

                6.2.1.45 E1 ubiquitin-activating enzyme

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Results	in table
4	Activating Compound
2393	AA Sequence
7	Application
31	Cloned(Commentary)
16	Cofactor
7	Crystallization (Commentary)
861	Disease/ Diagnostics
4	Expression
43	General Information
3	IC50 Value
27	Inhibitors
1	Ki Value [mM]
28	KM Value [mM]
11	Localization
17	Metals/Ions
16	Molecular Weight [Da]
25	Natural Substrates/ Products (Substrates)
52	Organism
1	Pathway
42	PDB ID
7	pH Optimum
1	pI Value
3	Posttranslational Modification
33	Protein Variants
16	Purification (Commentary)
5	Reaction
49	Reference
62	Source Tissue
2	Storage Stability
55	Substrates and Products (Substrate)
16	Subunits
100	Synonyms
1	Systematic Name
7	Temperature Optimum [°C]
30	Turnover Number [1/s]

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Application on EC 6.2.1.45 - E1 ubiquitin-activating enzyme

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APPLICATION

ORGANISM

UNIPROT

COMMENTARY

LITERATURE

drug development

Homo sapiens

P22314

the ubiquitin-activating enzyme E1 is a therapeutic target for the treatment of restenosis

744190

medicine

4 entries

synthesis

2 entries

medicine

Mus musculus

-

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

medicine

Homo sapiens

-

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

medicine

Homo sapiens

-

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

medicine

Homo sapiens

P22314

the ubiquitin-activating enzyme E1 is a therapeutic target for the treatment of restenosis

744190

synthesis

Homo sapiens

Q712V1

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

synthesis

Mus musculus

-

5–10 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