Ubiquitin Ligase (E1)
Ubiquitination of proteins is achieved through an enzymatic cascade involving ubiquitin-activating (E1), ubiquitin-conjugating (E2), and ubiquitin-ligating (E3) enzymes (EC 6.3.2.19). Two major types of E3s exist in eukaryotes, defined by the presence of either a HECT or a RING domain[1]. The SCF (Skp1, Cullins, F-box proteins) multisubunit E3 ubiquitin ligase, also known as CRL (Cullin-RING ubiquitin Ligase) is the largest E3 ubiquitin ligase family that promotes the ubiquitination of various regulatory proteins for targeted degradation, thus regulating many biological processes, including cell cycle progression, signal transduction, and DNA replication[2].
[1] R.J. Deshaies, C.A.P. Joazeiro. RING Domain E3 Ubiquitin Ligases. Annu. Rev. Biochem. 2009, 78, 399-434.
[2] L. Jia et al. SCF E3 ubiquitin ligases as anticancer targets. Curr Cancer Drug Targets. 2011 Mar;11(3):347-56.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 3797 | TAK-981 oxalate | Inhibitor of SUMOylation | €110.00 | |
| 3829 | MLN7243 | Cell permeable small molecule inhibitor targeting ubiquitin-activating enzymes (UAE, also known as E1 enzymes) | Inquire | |
| 2038 | MLN4924 | Inhibitor of NEDD8 Activating Enzyme (NAE) | €60.00 | |
| 3109 | ML-792 | Potent and selective inhibitor of SUMO-activating enzyme (SAE) | €145.00 | |
| 3709 | DKM 2-93 | Selective inhibitor of UBA5 | €70.00 | |
| 2935 | COH000 | First-in-class, highly specific, covalent allosteric inhibitor of SUMO E1 | €175.00 | |