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2.3.2.26: HECT-type E3 ubiquitin transferase

This is an abbreviated version!
For detailed information about HECT-type E3 ubiquitin transferase, go to the full flat file.

Word Map on EC 2.3.2.26

Reaction

[E2 ubiquitin-conjugating enzyme]-S-ubiquitinyl-L-cysteine
+
[acceptor protein]-L-lysine
=
[E2 ubiquitin-conjugating enzyme]-L-cysteine
 +
[acceptor protein]-N6-ubiquitinyl-L-lysine

Synonyms

AIP2, AIP4, apoptosis-resistant E3 ligase 1, AREL1, atrophin-1 interacting protein 2, DDB_G0286931, E3 ligase, E3 ubiquitin-protein ligase NEDD4, E3 ubiquitin-protein ligase TOM1, E6-AP, E6AP, ETC-1, HECT domain E3 ubiquitin ligase, HECT ligase, HECT-domain ubiquitin ligase, HECT-type E3 ligase, HECT-type ubiquitin E3 ligase, HECTD3, HectPH1, HECTWWP2, Herc4, Huwe1, Itch, Nedd4, Nedd4 HECT, Nedd4-1, Nedd4L, NEDL1, NleL, RSP5, Smurf1, Smurf2, sog-1, TRIP12, Trp120, UBE3B, Ube3C, ubiquitin-protein ligase E3C, UBR E3 ubiquitin ligase homolog, Ubr-5, UBR1, UBR5, UPL3, UPL5, WW domain-containing E3 Ub–protein ligase 2, WWP1, WWP2

ECTree

     2 Transferases
         2.3 Acyltransferases
             2.3.2 Aminoacyltransferases
                2.3.2.26 HECT-type E3 ubiquitin transferase

Inhibitors

Inhibitors on EC 2.3.2.26 - HECT-type E3 ubiquitin transferase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4-[[(3-chloro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)amino]methyl]-N-(pyridin-4-yl)benzamide
compound exhibits remarkable anticancer activity with tumor growth inhibition values of 98.3% and 100% at 25 mg/kg and 50 mg/kg orally daily, respectively, against human RPMI-8226 multiple myeloma xenograft. Treatment with the compound also shows a decrease of Itch level in human RPMI-8226 multiple myeloma cells
-
Calmodulin
UBE3B interacts with calmodulin via its N-terminal isoleucine-glutamine motif. Deletion of the motif (amino acids 29-58) results in loss of calmodulin binding and a significant increase in the in vitro ubiquitylation activity of UBE3B. Changes in calcium levels in vitro disrupt the calmodulin-UBE3B interaction
chlorpromazine
minimum inhibitory concentration is 0.3 mM
chlorprothixene
minimum inhibitory concentration is 0.3 mM
clomipramine
antidepressant drug, specifically blocks isoform ITCH auto-ubiquitylation, as well as p73 ubiquitylation. Treating a panel of breast, prostate and bladder cancer cell lines with clomipramine, or its homologs, leads to reduced cancer cell growth, and synergize with gemcitabine or mitomycin in killing cancer cells by blocking autophagy. Minimum inhibitory concentration is 0.3 mM
N-acetylphenylalanylamide
-
i.e. Phe-823 mimic, acts as a noncompetitive inhibitor of polyubiquitin chain elongation by destabilizing the active trimer
norclomipramine
minimum inhibitory concentration is 0.3 mM
additional information
autoinhibition mechanism of domains C2-HECT is not observed in isoform Smurf1
-