Methyllysine reader proteins | Other protein targets | IUPHAR/BPS Guide to IMMUNOPHARMACOLOGY

Methyllysine reader proteins C

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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Methyllysine reader proteins bind to methylated proteins, such as histones, allowing regulation of gene expression.

Targets

Targets of relevance to immunopharmacology are highlighted in blue

L3MBTL histone methyl-lysine binding protein 3 C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2830

Nomenclature

L3MBTL histone methyl-lysine binding protein 3

Previous and unofficial names

Genes

L3MBTL3 (Hs), L3mbtl3 (Mm), L3mbtl3 (Rn)

Ensembl ID

ENSG00000198945 (Hs), ENSMUSG00000039089 (Mm), ENSRNOG00000011720 (Rn)

UniProtKB AC

Q96JM7 (Hs), Q8BLB7 (Mm)

Selective agonists

UNC1215 [1]

spindlin 1 Show summary »« Hide summary

Target Id

3274

Nomenclature

spindlin 1

Previous and unofficial names

TDRD24

Genes

SPIN1 (Hs), Spin1 (Mm), Spin1 (Rn)

Ensembl ID

ENSG00000106723 (Hs), ENSMUSG00000021395 (Mm), ENSRNOG00000067284 (Rn)

UniProtKB AC

Q9Y657 (Hs), Q3TLC3 (Mm), Q4V8J7 (Rn)

Inhibitors

MS8535 (Binding) pK_d 7.5 [3]

MS31 (Binding) pK_d 7.0

MS31 pIC₅₀ 7.1 [2]

MS8535 pIC₅₀ 6.7 [3]

Comment

The SPIN1 gene encodes the spindlin 1 methyl-lysine reader protein. It recognises dimethylated histone H3 arginine 8 (H3R8me2a) and trimethylated histone H3 lysine 4 (H3K4me3) modifications and acts as a transcriptional coactivator. It has non-reader functions including roles in spindle stability maintenance and chromosome segregation. SPIN1 is overexpressed in several types of malignancies, making it a target for anti-cancer drug development.

References

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1. James LI, Barsyte-Lovejoy D, Zhong N, Krichevsky L, Korboukh VK, Herold JM, MacNevin CJ, Norris JL, Sagum CA, Tempel W et al.. (2013) Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol, 9 (3): 184-91. [PMID:23292653]

2. Xiong Y, Greschik H, Johansson C, Seifert L, Bacher J, Park KS, Babault N, Martini M, Fagan V, Li F et al.. (2019) Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). J Med Chem, 62 (20): 8996-9007. [PMID:31260300]

3. Xiong Y, Greschik H, Johansson C, Seifert L, Gamble V, Park KS, Fagan V, Li F, Chau I, Vedadi M et al.. (2024) Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor. J Med Chem, 67 (7): 5837-5853. [PMID:38533580]

How to cite this family page

Database page citation:

Methyllysine reader proteins. Accessed on 03/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=902.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Buneman OP, Faccenda E, Harding SD, Spedding M, Cidlowski JA, Fabbro D, Davenport AP, Striessnig J, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets. Br J Pharmacol. 180 Suppl 2:S1-22.