Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTV8CRH)

• DTT Name: Lysine-specific demethylase 4C (KDM4C)
• Synonyms: KIAA0780; Jumonji domain-containing protein 2C; JmjC domain-containing histone demethylation protein 3C; JMJD2C; JHDM3C; Gene amplified in squamous cell carcinoma 1 protein; GASC1; GASC-1 protein
• Gene Name: KDM4C
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: Paired donor oxygen oxidoreductase
• UniProt ID: KDM4C_HUMAN
• TTD ID: T73863
• EC Number: EC 1.14.11.-
• Sequence:
  MEVAEVESPLNPSCKIMTFRPSMEEFREFNKYLAYMESKGAHRAGLAKVIPPKEWKPRQC
  YDDIDNLLIPAPIQQMVTGQSGLFTQYNIQKKAMTVKEFRQLANSGKYCTPRYLDYEDLE
  RKYWKNLTFVAPIYGADINGSIYDEGVDEWNIARLNTVLDVVEEECGISIEGVNTPYLYF
  GMWKTTFAWHTEDMDLYSINYLHFGEPKSWYAIPPEHGKRLERLAQGFFPSSSQGCDAFL
  RHKMTLISPSVLKKYGIPFDKITQEAGEFMITFPYGYHAGFNHGFNCAESTNFATVRWID
  YGKVAKLCTCRKDMVKISMDIFVRKFQPDRYQLWKQGKDIYTIDHTKPTPASTPEVKAWL
  QRRRKVRKASRSFQCARSTSKRPKADEEEEVSDEVDGAEVPNPDSVTDDLKVSEKSEAAV
  KLRNTEASSEEESSASRMQVEQNLSDHIKLSGNSCLSTSVTEDIKTEDDKAYAYRSVPSI
  SSEADDSIPLSSGYEKPEKSDPSELSWPKSPESCSSVAESNGVLTEGEESDVESHGNGLE
  PGEIPAVPSGERNSFKVPSIAEGENKTSKSWRHPLSRPPARSPMTLVKQQAPSDEELPEV
  LSIEEEVEETESWAKPLIHLWQTKSPNFAAEQEYNATVARMKPHCAICTLLMPYHKPDSS
  NEENDARWETKLDEVVTSEGKTKPLIPEMCFIYSEENIEYSPPNAFLEEDGTSLLISCAK
  CCVRVHASCYGIPSHEICDGWLCARCKRNAWTAECCLCNLRGGALKQTKNNKWAHVMCAV
  AVPEVRFTNVPERTQIDVGRIPLQRLKLKCIFCRHRVKRVSGACIQCSYGRCPASFHVTC
  AHAAGVLMEPDDWPYVVNITCFRHKVNPNVKSKACEKVISVGQTVITKHRNTRYYSCRVM
  AVTSQTFYEVMFDDGSFSRDTFPEDIVSRDCLKLGPPAEGEVVQVKWPDGKLYGAKYFGS
  NIAHMYQVEFEDGSQIAMKREDIYTLDEELPKRVKARFSTASDMRFEDTFYGADIIQGER
  KRQRVLSSRFKNEYVADPVYRTFLKSSFQKKCQKRQ
• Function: Does not demethylate histone H3 'Lys-4', H3 'Lys-27' nor H4 'Lys-20'. Demethylates trimethylated H3 'Lys-9' and H3 'Lys-36' residue, while it has no activity on mono- and dimethylated residues. Demethylation of Lys residue generates formaldehyde and succinate. Histone demethylase that specifically demethylates 'Lys-9' and 'Lys-36' residues of histone H3, thereby playing a central role in histone code.
• Reactome Pathway:
  Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 (R-HSA-5625886)
  HDMs demethylate histones (R-HSA-3214842)
• BioCyc Pathway: MetaCyc:ENSG00000107077-MON

Molecular Interaction Atlas (MIA) of This DTT

13 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Flavonoid derivative 6	DM0E38G	N. A.	N. A.	Patented	[1]
Hydroxamate analog 1	DMGATHZ	N. A.	N. A.	Patented	[1]
PMID25468267-Compound-46	DMSKCEH	N. A.	N. A.	Patented	[1]
PMID25468267-Compound-47	DMG2JEK	N. A.	N. A.	Patented	[1]
PMID25468267-Compound-55	DMIXQRY	N. A.	N. A.	Patented	[1]
PMID25468267-Compound-56	DMAI19Z	N. A.	N. A.	Patented	[1]
Pyrido[1,2-a]indole-1.-carboxylic acid analog 1	DMF0XI3	N. A.	N. A.	Patented	[1]
Pyrido[1,2-a]indole-1.-carboxylic acid analog 2	DMWMV48	N. A.	N. A.	Patented	[1]
Pyrido[1,2-a]indole-1.-carboxylic acid analog 3	DMCLKBY	N. A.	N. A.	Patented	[1]
Pyrido[1,2-a]indole-1.-carboxylic acid analog 4	DM09FOQ	N. A.	N. A.	Patented	[1]
Pyrido[1,2-a]indole-1.-carboxylic acid analog 5	DMO3QDW	N. A.	N. A.	Patented	[1]
Pyrido[1,2-a]indole-1.-carboxylic acid analog 6	DMRQ1ZB	N. A.	N. A.	Patented	[1]
Pyrido[1,2-a]indole-1.-carboxylic acid analog 7	DMXY3F0	N. A.	N. A.	Patented	[1]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
IOX1	DMYG0M5	Discovery agent	N.A.	Investigative	[2]

References

• [1] KDM4 histone demethylase inhibitors for anti-cancer agents: a patent review.Expert Opin Ther Pat. 2015 Feb;25(2):135-44.
• [2] A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9(3):566-71.