Inhibitors of NF-kappaB (IκB) family proteins

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Inhibitors of NF-kappaB (IκB) family proteins

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).

Targets

Targets of relevance to immunopharmacology are highlighted in blue

BCL3 transcription coactivator Show summary »« Hide summary

Target Id

3232

Nomenclature

BCL3 transcription coactivator

Previous and unofficial names

BCL3, transcription coactivator | B cell CLL/lymphoma 3 | B-cell leukemia/lymphoma 3 | Bcl-3

Genes

BCL3 (Hs), Bcl3 (Mm), Bcl3 (Rn)

Ensembl ID

ENSG00000069399 (Hs), ENSMUSG00000053175 (Mm), ENSRNOG00000043416 (Rn)

UniProtKB AC

P20749 (Hs), Q9Z2F6 (Mm)

Inhibitors

BCL3 inhibitor JS6 pIC₅₀ 7.3 [6]

Comment

BCL3 is an atypical member of the IκB family. It is involved in immune cell differentiation and function [3] and it has been described as a proto-oncogene/oncoprotein that is associated with some cancers. Although the oncogenic nature of BCL3 was initially discovered in leukemia, it is also overexpressed in a number of solid tumours [1-2,4]. The design of small molecule inhibitors of BCL3 function, for use in oncology, is an active research focus for drug developers.

IκBζ (NFKB inhibitor zeta) Show summary »« Hide summary More detailed page go icon to follow link

Target Id	3008
Nomenclature	NFKB inhibitor zeta
Common abbreviation	IκBζ
Previous and unofficial names	nuclear factor of kappa light polypeptide gene enhancer in B cells inhibitor, zeta \| nuclear factor of kappa light polypeptide gene enhancer in B cells inhibitor \| IL-1 inducible nuclear ankyrin-repeat protein \| molecule possessing ankyrin repeats induced by lipopolysaccharide \| NF-kappa-B inhibitor zeta \| nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, zeta \| MAIL \| INAP
Genes	NFKBIZ (Hs), Nfkbiz (Mm), Nfkbiz (Rn)
Ensembl ID	ENSG00000144802 (Hs), ENSMUSG00000035356 (Mm), ENSRNOG00000031163 (Rn)
UniProtKB AC	Q9BYH8 (Hs), Q9EST8 (Mm)
Comment	IκBζ is an atypical member of the IκB protein family, that like Bcl3 and IκBNS resides in the nucleus. IκBζ is involved in regulation of NF-κB transcription factor complexes, principally as an inhibitor of NF-κB transcriptional activity.

Comments

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References

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1. Ahlqvist K, Saamarthy K, Syed Khaja AS, Bjartell A, Massoumi R. (2013) Expression of Id proteins is regulated by the Bcl-3 proto-oncogene in prostate cancer. Oncogene, 32 (12): 1601-8. [PMID:22580608]

2. de Souza Braga M, da Silva Paiva KB, Foguer K, Barbosa Chaves KC, de Sá Lima L, Scavone C, Bellini MH. (2014) Involvement of the NF-кB/p50/Bcl-3 complex in response to antiangiogenic therapy in a mouse model of metastatic renal cell carcinoma. Biomed Pharmacother, 68 (7): 873-9. [PMID:25113400]

3. Liu H, Zeng L, Yang Y, Guo C, Wang H. (2022) Bcl-3: A Double-Edged Sword in Immune Cells and Inflammation. Front Immunol, 13: 847699. [PMID:35355979]

4. Saamarthy K, Björner S, Johansson M, Landberg G, Massoumi R, Jirström K, Masoumi KC. (2015) Early diagnostic value of Bcl-3 localization in colorectal cancer. BMC Cancer, 15: 341. [PMID:25929479]

5. Viatour P, Merville MP, Bours V, Chariot A. (2005) Phosphorylation of NF-kappaB and IkappaB proteins: implications in cancer and inflammation. Trends Biochem Sci, 30 (1): 43-52. [PMID:15653325]

6. Westwell AD, Brancale A, Clarkson RWE, Soukupova J. (2015) 2-benzoylaminobenzamide derivatives as bcl-3 inhibitors. Patent number: WO2015014972A1. Assignee: University College Cardiff Consultants Limited. Priority date: 31/07/2014. Publication date: 05/02/2015.

How to cite this family page

Database page citation:

Inhibitors of NF-kappaB (IκB) family proteins. Accessed on 27/09/2023. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=996.

Concise Guide to PHARMACOLOGY citation:

Alexander SP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Introduction and Other Protein Targets. Br J Pharmacol. 178 Suppl 1:S1-S26.