C65: Otubains

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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There are two human genes that encode otubain proteins: OTUB1 and OTUB2 [1]. They are deubiquitinases that are classified within the C65 family of cysteine proteases in the MEROPS system.

Enzymes

OTU deubiquitinase, ubiquitin aldehyde binding 1 / otubain-1 Show summary »« Hide summary

Target Id

3208

Nomenclature

OTU deubiquitinase, ubiquitin aldehyde binding 1

Systematic nomenclature

otubain-1

Previous and unofficial names

OTB1 | OTU1 | otubain-1

Genes

OTUB1 (Hs), Otub1 (Mm), Otub1 (Rn)

Ensembl ID

ENSG00000167770 (Hs), ENSMUSG00000024767 (Mm), ENSRNOG00000021175 (Rn)

UniProtKB AC

Q96FW1 (Hs), Q7TQI3 (Mm), B2RYG6 (Rn)

EC number

3.4.19.12

Inhibitors

compound 61 [PMID: 36221183] pIC₅₀ 9.8 [3]

Comment

A cysteine protease with deubiquitinase activity that cleaves ubiquitin from branched poly-ubiquitin chains, but not from ubiquitinated proteins. Predicted to promote immune evasion (likely via inhibiting cytokine gene transcription and immune cell functions in the tumour microenvironment) and tumourigenesis, and is therefore a molecular target for anti-tumour drug discovery [2-3].

References

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1. Balakirev MY, Tcherniuk SO, Jaquinod M, Chroboczek J. (2003) Otubains: a new family of cysteine proteases in the ubiquitin pathway. EMBO Rep, 4 (5): 517-22. [PMID:12704427]

2. Liao Y, Yang M, Wang K, Wang Y, Zhong B, Jiang N. (2022) Deubiquitinating enzyme OTUB1 in immunity and cancer: Good player or bad actor?. Cancer Lett, 526: 248-258. [PMID:34875341]

3. Tan L, Shan H, Han C, Zhang Z, Shen J, Zhang X, Xiang H, Lu K, Qi C, Li Y et al.. (2022) Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. J Med Chem, [Epub ahead of print]. DOI: 10.1021/acs.jmedchem.2c00408 [PMID:36221183]

How to cite this family page

Database page citation:

C65: Otubains. Accessed on 29/03/2023. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=1071.

Concise Guide to PHARMACOLOGY citation:

Alexander SP, Fabbro D, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Enzymes. Br J Pharmacol. 178 Suppl 1:S313-S411.