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Literature summary extracted from

  • Ungermannova, D.; Parker, S.J.; Nasveschuk, C.G.; Wang, W.; Quade, B.; Zhang, G.; Kuchta, R.D.; Phillips, A.J.; Liu, X.
    Largazole and its derivatives selectively inhibit ubiquitin activating enzyme (E1) (2012), PLoS ONE, 7, e29208.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
6.2.1.45 recombinant baculovirus-mediated expression of the GST-tagged enzyme in Hi5 insect cells using the pFastBacHTA vector Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.2.1.45 (3E)-4-[(5R,8S)-5-methyl-6,9,13-trioxo-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-trien-11-yl]but-3-en-1-yl octanoate
-
 Homo sapiens
6.2.1.45 (3E)-4-[(5R,8S)-5-methyl-6,9,13-trioxo-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-trien-11-yl]but-3-en-1-yl octanoate
-
 Schizosaccharomyces pombe
6.2.1.45 (5R,8S)-11-ethenyl-5-methyl-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
 Homo sapiens
6.2.1.45 (5R,8S)-11-ethenyl-5-methyl-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
 Schizosaccharomyces pombe
6.2.1.45 (5R,8S)-5-methyl-11-[(1E)-6-oxotridec-1-en-1-yl]-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
 Homo sapiens
6.2.1.45 (5R,8S)-5-methyl-11-[(1E)-6-oxotridec-1-en-1-yl]-8-(propan-2-yl)-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
 Schizosaccharomyces pombe
6.2.1.45 (5R,8S)-5-methyl-8-(propan-2-yl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
 Homo sapiens
6.2.1.45 (5R,8S)-5-methyl-8-(propan-2-yl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1~2,5~]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
 Schizosaccharomyces pombe
6.2.1.45 largazole largazole and its ester and ketone analogues selectively inhibit human UBA1 enzyme and inhibit ubiquitin conjugation to cyclin-dependent kinase inhibitor p27Kip1 and TRF1 in vitro, mechanism of E1 inhibition, overview. Largazole and its derivatives specifically inhibit the adenylation step of the E1 reaction while having no effect on thioester bond formation between ubiquitin and E1. Upon incubation with E1, largazole or largazole ester reduce the amount of ubiquitin molecules that are transferred from E1 to E2 in a dose-dependent fashion. E1 inhibition appears to be specific to human E1. Largazole analogues do not significantly inhibit SUMO E1 Homo sapiens
6.2.1.45 additional information largazole and its ester and ketone analogues selectively inhibit ubiquitin conjugation to p27Kip1 and TRF1 in vitro, but the inhibition appears to be specific to human E1. Largazole analogues do not significantly inhibit Uba1p Schizosaccharomyces pombe
6.2.1.45 S-[(3E)-5-hydroxy-7-({[(4R)-4-{[(3S)-2-methoxy-4-methylpent-1-en-3-yl]carbamoyl}-4-methyl[4,5-dihydro[2,4'-bi-1,3-thiazole]]-2'-yl]methyl}amino)-7-oxohept-3-en-1-yl] octanethioate
-
 Homo sapiens
6.2.1.45 S-[(3E)-5-hydroxy-7-({[(4R)-4-{[(3S)-2-methoxy-4-methylpent-1-en-3-yl]carbamoyl}-4-methyl[4,5-dihydro[2,4'-bi-1,3-thiazole]]-2'-yl]methyl}amino)-7-oxohept-3-en-1-yl] octanethioate
-
 Schizosaccharomyces pombe
6.2.1.45 trichostatin A
-
 Schizosaccharomyces pombe

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
6.2.1.45 Mg2+ required Homo sapiens
6.2.1.45 Mg2+ required Schizosaccharomyces pombe

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
6.2.1.45 ATP + ubiquitin + [E1 ubiquitin-activating enzyme]-L-cysteine Homo sapiens
-
 AMP + diphosphate + S-ubiquitinyl-[E1 ubiquitin-activating enzyme]-L-cysteine
-
 ?
6.2.1.45 ATP + ubiquitin + [E1 ubiquitin-activating enzyme]-L-cysteine Schizosaccharomyces pombe
-
 AMP + diphosphate + S-ubiquitinyl-[E1 ubiquitin-activating enzyme]-L-cysteine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
6.2.1.45 Homo sapiens
-
-
-
6.2.1.45 Schizosaccharomyces pombe
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
6.2.1.45 recombinant GST-tagged enzyme from Hi5 insect cells by glutathione affinity chromatography, tag cleavage by thrombin, and gel filtration Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.2.1.45 ATP + ubiquitin + [E1 ubiquitin-activating enzyme]-L-cysteine
-
 Homo sapiens AMP + diphosphate + S-ubiquitinyl-[E1 ubiquitin-activating enzyme]-L-cysteine
-
 ?
6.2.1.45 ATP + ubiquitin + [E1 ubiquitin-activating enzyme]-L-cysteine
-
 Schizosaccharomyces pombe AMP + diphosphate + S-ubiquitinyl-[E1 ubiquitin-activating enzyme]-L-cysteine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
6.2.1.45 E1
-
 Homo sapiens
6.2.1.45 E1
-
 Schizosaccharomyces pombe
6.2.1.45 SUMO E1
-
 Homo sapiens
6.2.1.45 Uba1
-
 Homo sapiens
6.2.1.45 UBA1p
-
 Schizosaccharomyces pombe
6.2.1.45 ubiquitin E1
-
 Homo sapiens
6.2.1.45 Ubiquitin-activating enzyme
-
 Homo sapiens
6.2.1.45 Ubiquitin-activating enzyme
-
 Schizosaccharomyces pombe

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
6.2.1.45 30
-
 assay at Homo sapiens
6.2.1.45 30
-
 assay at Schizosaccharomyces pombe

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
6.2.1.45 7.5
-
 assay at Homo sapiens
6.2.1.45 7.5
-
 assay at Schizosaccharomyces pombe

Cofactor

EC Number Cofactor Comment Organism Structure
6.2.1.45 ATP
-
 Homo sapiens
6.2.1.45 ATP
-
 Schizosaccharomyces pombe