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lysine demethylase 5C

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Target not currently curated in GtoImmuPdb

Target id: 2682

Nomenclature: lysine demethylase 5C

Family: 1.14.11.- Histone demethylases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1560 Xp11.22 KDM5C lysine demethylase 5C
Mouse - 1554 X 68.46 cM Kdm5c lysine demethylase 5C
Rat - - Xq21 Kdm5c lysine demethylase 5C
Previous and Unofficial Names Click here for help
JARID1C | SMCX | MRX13 | jumonji AT rich interactive domain 1C | mental retardation X-linked 13 | lysine (K)-specific demethylase 5C
Database Links Click here for help
Alphafold P41229 (Hs), P41230 (Mm)
CATH/Gene3D 3.30.40.10
ChEMBL Target CHEMBL2163176 (Hs)
Ensembl Gene ENSG00000126012 (Hs), ENSMUSG00000025332 (Mm), ENSRNOG00000057706 (Rn)
Entrez Gene 8242 (Hs), 20591 (Mm), 317432 (Rn)
Human Protein Atlas ENSG00000126012 (Hs)
KEGG Gene hsa:8242 (Hs), mmu:20591 (Mm), rno:317432 (Rn)
OMIM 314690 (Hs)
Pharos P41229 (Hs)
RefSeq Nucleotide NM_004187 (Hs), NM_013668 (Mm)
RefSeq Protein NP_004178 (Hs), NP_038696 (Mm)
UniProtKB P41229 (Hs), P41230 (Mm)
Wikipedia KDM5C (Hs)

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
IOX2 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 1
⤷ pIC50 6.8 (IC50 1.59x10-7 M) [1]
GSK-J1 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.3 pIC50 2
⤷ pIC50 6.3 (IC50 5.5x10-7 M) [2]
PBIT Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.3 pIC50 4
⤷ pIC50 5.3 (IC50 4.9x10-6 M) [4]
GSK-J4 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 4.8 pIC50 2
⤷ pIC50 4.8 (IC50 1.5x10-5 M) [2]
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Syndromic X-linked mental retardation due to JARID1C mutation
Description: This syndrome is characterised by mild to severe intellectual deficit associated with variable clinical manifestations including spasticity, cryptorchidism, maxillary hypoplasia, alopecia areata, epilepsy, short stature, impaired speech and behavioural problems.
Synonyms: Mental retardation, X-linked, syndromic, Claes-Jensen type
OMIM: 300534
Orphanet: ORPHA85279
Comments:  To date more than ten JARID1C mutations have been reported in patients with X-linked mental retardation. The degree of mental retardation associated with JARID1C mutations ranges from mild to severe, and may be accompanied by additional disorders such as epilepsy, short stature, or behavioral problems.
References:  3,5

References

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1. Chowdhury R, Candela-Lena JI, Chan MC, Greenald DJ, Yeoh KK, Tian YM, McDonough MA, Tumber A, Rose NR, Conejo-Garcia A et al.. (2013) Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases. ACS Chem Biol, 8 (7): 1488-96. [PMID:23683440]

2. Heinemann B, Nielsen JM, Hudlebusch HR, Lees MJ, Larsen DV, Boesen T, Labelle M, Gerlach LO, Birk P, Helin K. (2014) Inhibition of demethylases by GSK-J1/J4. Nature, 514 (7520): E1-2. [PMID:25279926]

3. Iwase S, Lan F, Bayliss P, de la Torre-Ubieta L, Huarte M, Qi HH, Whetstine JR, Bonni A, Roberts TM, Shi Y. (2007) The X-linked mental retardation gene SMCX/JARID1C defines a family of histone H3 lysine 4 demethylases. Cell, 128 (6): 1077-88. [PMID:17320160]

4. Sayegh J, Cao J, Zou MR, Morales A, Blair LP, Norcia M, Hoyer D, Tackett AJ, Merkel JS, Yan Q. (2013) Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. J Biol Chem, 288 (13): 9408-17. [PMID:23408432]

5. Tzschach A, Lenzner S, Moser B, Reinhardt R, Chelly J, Fryns JP, Kleefstra T, Raynaud M, Turner G, Ropers HH et al.. (2006) Novel JARID1C/SMCX mutations in patients with X-linked mental retardation. Hum Mutat, 27 (4): 389. [PMID:16541399]

How to cite this page

1.14.11.- Histone demethylases: lysine demethylase 5C. Last modified on 30/03/2016. Accessed on 19/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2682.