Details of the Target

General Information of Target

Target ID LDTP07778
Target Name Lysine-specific demethylase 7A (KDM7A)
Gene Name KDM7A
Gene ID 80853
Synonyms
JHDM1D; KDM7; KIAA1718; Lysine-specific demethylase 7A; JmjC domain-containing histone demethylation protein 1D; Lysine-specific demethylase 7; [histone H3]-dimethyl-L-lysine9 demethylase 7A; EC 1.14.11.65
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGAAAAVAAGAAAGAAAAAVSVAAPGRASAPPPPPPVYCVCRQPYDVNRFMIECDICKD
WFHGSCVGVEEHHAVDIDLYHCPNCAVLHGSSLMKKRRNWHRHDYTEIDDGSKPVQAGTR
TFIKELRSRVFPSADEIIIKMHGSQLTQRYLEKHGFDVPIMVPKLDDLGLRLPSPTFSVM
DVERYVGGDKVIDVIDVARQADSKMTLHNYVKYFMNPNRPKVLNVISLEFSDTKMSELVE
VPDIAKKLSWVENYWPDDSVFPKPFVQKYCLMGVQDSYTDFHIDFGGTSVWYHVLWGEKI
FYLIKPTDENLARYESWSSSVTQSEVFFGDKVDKCYKCVVKQGHTLFVPTGWIHAVLTSQ
DCMAFGGNFLHNLNIGMQLRCYEMEKRLKTPDLFKFPFFEAICWFVAKNLLETLKELRED
GFQPQTYLVQGVKALHTALKLWMKKELVSEHAFEIPDNVRPGHLIKELSKVIRAIEEENG
KPVKSQGIPIVCPVSRSSNEATSPYHSRRKMRKLRDHNVRTPSNLDILELHTREVLKRLE
MCPWEEDILSSKLNGKFNKHLQPSSTVPEWRAKDNDLRLLLTNGRIIKDERQPFADQSLY
TADSENEEDKRRTKKAKMKIEESSGVEGVEHEESQKPLNGFFTRVKSELRSRSSGYSDIS
ESEDSGPECTALKSIFTTEESESSGDEKKQEITSNFKEESNVMRNFLQKSQKPSRSEIPI
KRECPTSTSTEEEAIQGMLSMAGLHYSTCLQRQIQSTDCSGERNSLQDPSSCHGSNHEVR
QLYRYDKPVECGYHVKTEDPDLRTSSWIKQFDTSRFHPQDLSRSQKCIRKEGSSEISQRV
QSRNYVDSSGSSLQNGKYMQNSNLTSGACQISNGSLSPERPVGETSFSVPLHPTKRPASN
PPPISNQATKGKRPKKGMATAKQRLGKILKLNRNGHARFFV
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
JHDM1 histone demethylase family, JHDM1D subfamily
Subcellular location
Nucleus
Function
Histone demethylase required for brain development. Specifically demethylates dimethylated 'Lys-9', 'Lys-27' and 'Lys-36' (H3K9me2, H3K27me2, H3K36me2, respectively) of histone H3 and monomethylated histone H4 'Lys-20' residue (H4K20Me1), thereby playing a central role in histone code. Specifically binds trimethylated 'Lys-4' of histone H3 (H3K4me3), affecting histone demethylase specificity: in presence of H3K4me3, it has no demethylase activity toward H3K9me2, while it has high activity toward H3K27me2. Demethylates H3K9me2 in absence of H3K4me3. Has activity toward H4K20Me1 only when nucleosome is used as a substrate and when not histone octamer is used as substrate.
TTD ID
T18784
Uniprot ID
Q6ZMT4
DrugMap ID
TT0NYMP
Ensemble ID
ENST00000397560.7
HGNC ID
HGNC:22224
ChEMBL ID
CHEMBL2163177

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A431 SNV: p.K341N .
CAMA1 SNV: p.R515Ter .
CCK81 SNV: p.D78G .
CHL1 SNV: p.G343E .
HT1080 SNV: p.V8G .
IM95 Deletion: p.R97GfsTer41 .
KASUMI2 SNV: p.L853P .
MCC13 SNV: p.E545D .
MFE319 Insertion: p.R97KfsTer8 .
RPMI7951 SNV: p.L410V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
AHL-Pu-1
 Probe Info  		C542(6.98)  LDD0171  [1]
IA-alkyne
 Probe Info  		C492(5.27)  LDD1704  [2]
DBIA
 Probe Info  		C542(0.85)  LDD1512  [3]
CY-1
 Probe Info  		N.A.  LDD0246  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA DM93 C542(6.98)  LDD0171  [1]
 LDCM0259  AC14 HEK-293T C542(0.85)  LDD1512  [3]
 LDCM0282  AC22 HEK-293T C542(0.88)  LDD1521  [3]
 LDCM0284  AC24 HEK-293T C542(0.87)  LDD1523  [3]
 LDCM0291  AC30 HEK-293T C542(0.98)  LDD1530  [3]
 LDCM0293  AC32 HEK-293T C542(0.80)  LDD1532  [3]
 LDCM0299  AC38 HEK-293T C542(1.04)  LDD1538  [3]
 LDCM0302  AC40 HEK-293T C542(0.83)  LDD1541  [3]
 LDCM0308  AC46 HEK-293T C542(0.93)  LDD1547  [3]
 LDCM0310  AC48 HEK-293T C542(0.91)  LDD1549  [3]
 LDCM0317  AC54 HEK-293T C542(0.77)  LDD1556  [3]
 LDCM0319  AC56 HEK-293T C542(0.77)  LDD1558  [3]
 LDCM0323  AC6 HEK-293T C542(1.21)  LDD1562  [3]
 LDCM0326  AC62 HEK-293T C542(0.99)  LDD1565  [3]
 LDCM0328  AC64 HEK-293T C542(0.80)  LDD1567  [3]
 LDCM0345  AC8 HEK-293T C542(0.69)  LDD1569  [3]
 LDCM0275  AKOS034007705 HEK-293T C542(0.95)  LDD1514  [3]
 LDCM0367  CL1 HEK-293T C55(1.00); C58(1.00)  LDD1571  [3]
 LDCM0368  CL10 HEK-293T C542(1.37)  LDD1572  [3]
 LDCM0370  CL101 HEK-293T C55(0.95); C58(0.95)  LDD1574  [3]
 LDCM0372  CL103 HEK-293T C791(1.15)  LDD1576  [3]
 LDCM0374  CL105 HEK-293T C55(1.00); C58(1.00)  LDD1578  [3]
 LDCM0376  CL107 HEK-293T C791(1.05)  LDD1580  [3]
 LDCM0378  CL109 HEK-293T C55(1.18); C58(1.18)  LDD1582  [3]
 LDCM0381  CL111 HEK-293T C791(1.03)  LDD1585  [3]
 LDCM0383  CL113 HEK-293T C55(1.09); C58(1.09)  LDD1587  [3]
 LDCM0385  CL115 HEK-293T C791(1.07)  LDD1589  [3]
 LDCM0387  CL117 HEK-293T C55(1.20); C58(1.20)  LDD1591  [3]
 LDCM0389  CL119 HEK-293T C791(1.10)  LDD1593  [3]
 LDCM0390  CL12 HEK-293T C542(0.74)  LDD1594  [3]
 LDCM0392  CL121 HEK-293T C55(1.02); C58(1.02)  LDD1596  [3]
 LDCM0394  CL123 HEK-293T C791(1.04)  LDD1598  [3]
 LDCM0396  CL125 HEK-293T C55(1.02); C58(1.02)  LDD1600  [3]
 LDCM0398  CL127 HEK-293T C791(1.07)  LDD1602  [3]
 LDCM0400  CL13 HEK-293T C55(0.86); C58(0.86)  LDD1604  [3]
 LDCM0402  CL15 HEK-293T C791(1.03)  LDD1606  [3]
 LDCM0410  CL22 HEK-293T C542(1.08)  LDD1614  [3]
 LDCM0412  CL24 HEK-293T C542(0.70)  LDD1616  [3]
 LDCM0413  CL25 HEK-293T C55(0.95); C58(0.95)  LDD1617  [3]
 LDCM0415  CL27 HEK-293T C791(1.04)  LDD1619  [3]
 LDCM0418  CL3 HEK-293T C791(0.95)  LDD1622  [3]
 LDCM0423  CL34 HEK-293T C542(0.89)  LDD1627  [3]
 LDCM0425  CL36 HEK-293T C542(0.86)  LDD1629  [3]
 LDCM0426  CL37 HEK-293T C55(1.11); C58(1.11)  LDD1630  [3]
 LDCM0428  CL39 HEK-293T C791(1.01)  LDD1632  [3]
 LDCM0436  CL46 HEK-293T C542(0.85)  LDD1640  [3]
 LDCM0438  CL48 HEK-293T C542(1.02)  LDD1642  [3]
 LDCM0439  CL49 HEK-293T C55(1.03); C58(1.03)  LDD1643  [3]
 LDCM0449  CL58 HEK-293T C542(0.86)  LDD1652  [3]
 LDCM0452  CL60 HEK-293T C542(0.88)  LDD1655  [3]
 LDCM0453  CL61 HEK-293T C55(1.08); C58(1.08)  LDD1656  [3]
 LDCM0455  CL63 HEK-293T C791(1.04)  LDD1658  [3]
 LDCM0463  CL70 HEK-293T C542(0.81)  LDD1666  [3]
 LDCM0465  CL72 HEK-293T C542(0.76)  LDD1668  [3]
 LDCM0466  CL73 HEK-293T C55(0.96); C58(0.96)  LDD1669  [3]
 LDCM0476  CL82 HEK-293T C542(0.84)  LDD1679  [3]
 LDCM0478  CL84 HEK-293T C542(0.91)  LDD1681  [3]
 LDCM0479  CL85 HEK-293T C55(0.94); C58(0.94)  LDD1682  [3]
 LDCM0481  CL87 HEK-293T C791(1.24)  LDD1684  [3]
 LDCM0489  CL94 HEK-293T C542(0.92)  LDD1692  [3]
 LDCM0491  CL96 HEK-293T C542(0.80)  LDD1694  [3]
 LDCM0492  CL97 HEK-293T C55(1.05); C58(1.05)  LDD1695  [3]
 LDCM0494  CL99 HEK-293T C791(1.04)  LDD1697  [3]
 LDCM0495  E2913 HEK-293T C791(1.02)  LDD1698  [3]
 LDCM0468  Fragment33 HEK-293T C791(1.00)  LDD1671  [3]
 LDCM0022  KB02 T cell-activated C492(5.27)  LDD1704  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Daminozide Small molecular drug D0B2WZ

References

1 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
2 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
3 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
4 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.