General Information of Drug Off-Target (DOT) (ID: OTC59BCO)

DOT Name Histone-lysine N-methyltransferase 2C (KMT2C)
Synonyms Lysine N-methyltransferase 2C; EC 2.1.1.364; Homologous to ALR protein; Myeloid/lymphoid or mixed-lineage leukemia protein 3
Gene Name KMT2C
Related Disease
Estrogen-receptor positive breast cancer ( )
Neurodevelopmental disorder ( )
Syndromic intellectual disability ( )
Acute lymphocytic leukaemia ( )
Acute myelogenous leukaemia ( )
Adenocarcinoma ( )
Advanced cancer ( )
Autism spectrum disorder ( )
Bone osteosarcoma ( )
Breast neoplasm ( )
Colorectal carcinoma ( )
Dilated cardiomyopathy 1A ( )
Endometrial cancer ( )
Endometrial carcinoma ( )
Esophageal squamous cell carcinoma ( )
Gastric cancer ( )
Gastric neoplasm ( )
Glioma ( )
Head and neck carcinoma ( )
Hepatocellular carcinoma ( )
Hereditary diffuse gastric adenocarcinoma ( )
Intellectual disability, autosomal dominant 40 ( )
Kleefstra syndrome 2 ( )
leukaemia ( )
Medulloblastoma ( )
Myelodysplastic syndrome ( )
Neoplasm ( )
Osteosarcoma ( )
Pancreatic tumour ( )
Prostate cancer ( )
Prostate neoplasm ( )
Schizophrenia ( )
Sezary syndrome ( )
Stomach cancer ( )
Intellectual disability ( )
Nasopharyngeal carcinoma ( )
Cholangiocarcinoma ( )
Intrahepatic cholangiocarcinoma ( )
Leukemia ( )
Lung cancer ( )
Lung carcinoma ( )
Transitional cell carcinoma ( )
Urinary bladder cancer ( )
Urinary bladder neoplasm ( )
UniProt ID
KMT2C_HUMAN
PDB ID
2YSM; 2YUK; 3UVL; 4ERY; 5F59; 5F6K; 6KIW; 6MLC; 7W6L
EC Number
2.1.1.364
Pfam ID
PF05965 ; PF05964 ; PF00628 ; PF00856 ; PF13771 ; PF13832
Sequence
MSSEEDKSVEQPQPPPPPPEEPGAPAPSPAAADKRPRGRPRKDGASPFQRARKKPRSRGK
TAVEDEDSMDGLETTETETIVETEIKEQSAEEDAEAEVDNSKQLIPTLQRSVSEESANSL
VSVGVEAKISEQLCAFCYCGEKSSLGQGDLKQFRITPGFILPWRNQPSNKKDIDDNSNGT
YEKMQNSAPRKQRGQRKERSPQQNIVSCVSVSTQTASDDQAGKLWDELSLVGLPDAIDIQ
ALFDSTGTCWAHHRCVEWSLGVCQMEEPLLVNVDKAVVSGSTERCAFCKHLGATIKCCEE
KCTQMYHYPCAAGAGTFQDFSHIFLLCPEHIDQAPERSKEDANCAVCDSPGDLLDQFFCT
TCGQHYHGMCLDIAVTPLKRAGWQCPECKVCQNCKQSGEDSKMLVCDTCDKGYHTFCLQP
VMKSVPTNGWKCKNCRICIECGTRSSSQWHHNCLICDNCYQQQDNLCPFCGKCYHPELQK
DMLHCNMCKRWVHLECDKPTDHELDTQLKEEYICMYCKHLGAEMDRLQPGEEVEIAELTT
DYNNEMEVEGPEDQMVFSEQAANKDVNGQESTPGIVPDAVQVHTEEQQKSHPSESLDTDS
LLIAVSSQHTVNTELEKQISNEVDSEDLKMSSEVKHICGEDQIEDKMEVTENIEVVTHQI
TVQQEQLQLLEEPETVVSREESRPPKLVMESVTLPLETLVSPHEESISLCPEEQLVIERL
QGEKEQKENSELSTGLMDSEMTPTIEGCVKDVSYQGGKSIKLSSETESSFSSSADISKAD
VSSSPTPSSDLPSHDMLHNYPSALSSSAGNIMPTTYISVTPKIGMGKPAITKRKFSPGRP
RSKQGAWSTHNTVSPPSWSPDISEGREIFKPRQLPGSAIWSIKVGRGSGFPGKRRPRGAG
LSGRGGRGRSKLKSGIGAVVLPGVSTADISSNKDDEENSMHNTVVLFSSSDKFTLNQDMC
VVCGSFGQGAEGRLLACSQCGQCYHPYCVSIKITKVVLSKGWRCLECTVCEACGKATDPG
RLLLCDDCDISYHTYCLDPPLQTVPKGGWKCKWCVWCRHCGATSAGLRCEWQNNYTQCAP
CASLSSCPVCYRNYREEDLILQCRQCDRWMHAVCQNLNTEEEVENVADIGFDCSMCRPYM
PASNVPSSDCCESSLVAQIVTKVKELDPPKTYTQDGVCLTESGMTQLQSLTVTVPRRKRS
KPKLKLKIINQNSVAVLQTPPDIQSEHSRDGEMDDSREGELMDCDGKSESSPEREAVDDE
TKGVEGTDGVKKRKRKPYRPGIGGFMVRQRSRTGQGKTKRSVIRKDSSGSISEQLPCRDD
GWSEQLPDTLVDESVSVTESTEKIKKRYRKRKNKLEETFPAYLQEAFFGKDLLDTSRQSK
ISLDNLSEDGAQLLYKTNMNTGFLDPSLDPLLSSSSAPTKSGTHGPADDPLADISEVLNT
DDDILGIISDDLAKSVDHSDIGPVTDDPSSLPQPNVNQSSRPLSEEQLDGILSPELDKMV
TDGAILGKLYKIPELGGKDVEDLFTAVLSPANTQPTPLPQPPPPTQLLPIHNQDAFSRMP
LMNGLIGSSPHLPHNSLPPGSGLGTFSAIAQSSYPDARDKNSAFNPMASDPNNSWTSSAP
TVEGENDTMSNAQRSTLKWEKEEALGEMATVAPVLYTNINFPNLKEEFPDWTTRVKQIAK
LWRKASSQERAPYVQKARDNRAALRINKVQMSNDSMKRQQQQDSIDPSSRIDSELFKDPL
KQRESEHEQEWKFRQQMRQKSKQQAKIEATQKLEQVKNEQQQQQQQQFGSQHLLVQSGSD
TPSSGIQSPLTPQPGNGNMSPAQSFHKELFTKQPPSTPTSTSSDDVFVKPQAPPPPPAPS
RIPIQDSLSQAQTSQPPSPQVFSPGSSNSRPPSPMDPYAKMVGTPRPPPVGHSFSRRNSA
APVENCTPLSSVSRPLQMNETTANRPSPVRDLCSSSTTNNDPYAKPPDTPRPVMTDQFPK
SLGLSRSPVVSEQTAKGPIAAGTSDHFTKPSPRADVFQRQRIPDSYARPLLTPAPLDSGP
GPFKTPMQPPPSSQDPYGSVSQASRRLSVDPYERPALTPRPIDNFSHNQSNDPYSQPPLT
PHPAVNESFAHPSRAFSQPGTISRPTSQDPYSQPPGTPRPVVDSYSQSSGTARSNTDPYS
QPPGTPRPTTVDPYSQQPQTPRPSTQTDLFVTPVTNQRHSDPYAHPPGTPRPGISVPYSQ
PPATPRPRISEGFTRSSMTRPVLMPNQDPFLQAAQNRGPALPGPLVRPPDTCSQTPRPPG
PGLSDTFSRVSPSAARDPYDQSPMTPRSQSDSFGTSQTAHDVADQPRPGSEGSFCASSNS
PMHSQGQQFSGVSQLPGPVPTSGVTDTQNTVNMAQADTEKLRQRQKLREIILQQQQQKKI
AGRQEKGSQDSPAVPHPGPLQHWQPENVNQAFTRPPPPYPGNIRSPVAPPLGPRYAVFPK
DQRGPYPPDVASMGMRPHGFRFGFPGGSHGTMPSQERFLVPPQQIQGSGVSPQLRRSVSV
DMPRPLNNSQMNNPVGLPQHFSPQSLPVQQHNILGQAYIELRHRAPDGRQRLPFSAPPGS
VVEASSNLRHGNFIPRPDFPGPRHTDPMRRPPQGLPNQLPVHPDLEQVPPSQQEQGHSVH
SSSMVMRTLNHPLGGEFSEAPLSTSVPSETTSDNLQITTQPSDGLEEKLDSDDPSVKELD
VKDLEGVEVKDLDDEDLENLNLDTEDGKVVELDTLDNLETNDPNLDDLLRSGEFDIIAYT
DPELDMGDKKSMFNEELDLPIDDKLDNQCVSVEPKKKEQENKTLVLSDKHSPQKKSTVTN
EVKTEVLSPNSKVESKCETEKNDENKDNVDTPCSQASAHSDLNDGEKTSLHPCDPDLFEK
RTNRETAGPSANVIQASTQLPAQDVINSCGITGSTPVLSSLLANEKSDNSDIRPSGSPPP
PTLPASPSNHVSSLPPFIAPPGRVLDNAMNSNVTVVSRVNHVFSQGVQVNPGLIPGQSTV
NHSLGTGKPATQTGPQTSQSGTSSMSGPQQLMIPQTLAQQNRERPLLLEEQPLLLQDLLD
QERQEQQQQRQMQAMIRQRSEPFFPNIDFDAITDPIMKAKMVALKGINKVMAQNNLGMPP
MVMSRFPFMGQVVTGTQNSEGQNLGPQAIPQDGSITHQISRPNPPNFGPGFVNDSQRKQY
EEWLQETQQLLQMQQKYLEEQIGAHRKSKKALSAKQRTAKKAGREFPEEDAEQLKHVTEQ
QSMVQKQLEQIRKQQKEHAELIEDYRIKQQQQCAMAPPTMMPSVQPQPPLIPGATPPTMS
QPTFPMVPQQLQHQQHTTVISGHTSPVRMPSLPGWQPNSAPAHLPLNPPRIQPPIAQLPI
KTCTPAPGTVSNANPQSGPPPRVEFDDNNPFSESFQERERKERLREQQERQRIQLMQEVD
RQRALQQRMEMEQHGMVGSEISSSRTSVSQIPFYSSDLPCDFMQPLGPLQQSPQHQQQMG
QVLQQQNIQQGSINSPSTQTFMQTNERRQVGPPSFVPDSPSIPVGSPNFSSVKQGHGNLS
GTSFQQSPVRPSFTPALPAAPPVANSSLPCGQDSTITHGHSYPGSTQSLIQLYSDIIPEE
KGKKKRTRKKKRDDDAESTKAPSTPHSDITAPPTPGISETTSTPAVSTPSELPQQADQES
VEPVGPSTPNMAAGQLCTELENKLPNSDFSQATPNQQTYANSEVDKLSMETPAKTEEIKL
EKAETESCPGQEEPKLEEQNGSKVEGNAVACPVSSAQSPPHSAGAPAAKGDSGNELLKHL
LKNKKSSSLLNQKPEGSICSEDDCTKDNKLVEKQNPAEGLQTLGAQMQGGFGCGNQLPKT
DGGSETKKQRSKRTQRTGEKAAPRSKKRKKDEEEKQAMYSSTDTFTHLKQQNNLSNPPTP
PASLPPTPPPMACQKMANGFATTEELAGKAGVLVSHEVTKTLGPKPFQLPFRPQDDLLAR
ALAQGPKTVDVPASLPTPPHNNQEELRIQDHCGDRDTPDSFVPSSSPESVVGVEVSRYPD
LSLVKEEPPEPVPSPIIPILPSTAGKSSESRRNDIKTEPGTLYFASPFGPSPNGPRSGLI
SVAITLHPTAAENISSVVAAFSDLLHVRIPNSYEVSSAPDVPSMGLVSSHRINPGLEYRQ
HLLLRGPPPGSANPPRLVSSYRLKQPNVPFPPTSNGLSGYKDSSHGIAESAALRPQWCCH
CKVVILGSGVRKSFKDLTLLNKDSRESTKRVEKDIVFCSNNCFILYSSTAQAKNSENKES
IPSLPQSPMRETPSKAFHQYSNNISTLDVHCLPQLPEKASPPASPPIAFPPAFEAAQVEA
KPDELKVTVKLKPRLRAVHGGFEDCRPLNKKWRGMKWKKWSIHIVIPKGTFKPPCEDEID
EFLKKLGTSLKPDPVPKDYRKCCFCHEEGDGLTDGPARLLNLDLDLWVHLNCALWSTEVY
ETQAGALINVELALRRGLQMKCVFCHKTGATSGCHRFRCTNIYHFTCAIKAQCMFFKDKT
MLCPMHKPKGIHEQELSYFAVFRRVYVQRDEVRQIASIVQRGERDHTFRVGSLIFHTIGQ
LLPQQMQAFHSPKALFPVGYEASRLYWSTRYANRRCRYLCSIEEKDGRPVFVIRIVEQGH
EDLVLSDISPKGVWDKILEPVACVRKKSEMLQLFPAYLKGEDLFGLTVSAVARIAESLPG
VEACENYTFRYGRNPLMELPLAVNPTGCARSEPKMSAHVKRFVLRPHTLNSTSTSKSFQS
TVTGELNAPYSKQFVHSKSSQYRKMKTEWKSNVYLARSRIQGLGLYAARDIEKHTMVIEY
IGTIIRNEVANRKEKLYESQNRGVYMFRMDNDHVIDATLTGGPARYINHSCAPNCVAEVV
TFERGHKIIISSSRRIQKGEELCYDYKFDFEDDQHKIPCHCGAVNCRKWMN
Function
Histone methyltransferase that catalyzes methyl group transfer from S-adenosyl-L-methionine to the epsilon-amino group of 'Lys-4' of histone H3 (H3K4). Part of chromatin remodeling machinery predominantly forms H3K4me1 methylation marks at active chromatin sites where transcription and DNA repair take place. Likely plays a redundant role with KMT2D in enriching H3K4me1 mark on primed and active enhancer elements.
Tissue Specificity
Highly expressed in testis and ovary, followed by brain and liver. Also expressed in placenta, peripherical blood, fetal thymus, heart, lung and kidney. Within brain, expression was highest in hippocampus, caudate nucleus, and substantia nigra. Not detected in skeletal muscle and fetal liver.
KEGG Pathway
Lysine degradation (hsa00310 )
Metabolic pathways (hsa01100 )
Reactome Pathway
Activation of anterior HOX genes in hindbrain development during early embryogenesis (R-HSA-5617472 )
RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function (R-HSA-8936459 )
Formation of WDR5-containing histone-modifying complexes (R-HSA-9772755 )
PKMTs methylate histone lysines (R-HSA-3214841 )
BioCyc Pathway
MetaCyc:HS00685-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

44 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Estrogen-receptor positive breast cancer DIS1H502 Definitive Genetic Variation [1]
Neurodevelopmental disorder DIS372XH Definitive Biomarker [2]
Syndromic intellectual disability DISH7SDF Definitive Autosomal dominant [3]
Acute lymphocytic leukaemia DISPX75S Strong Biomarker [4]
Acute myelogenous leukaemia DISCSPTN Strong Genetic Variation [5]
Adenocarcinoma DIS3IHTY Strong Biomarker [6]
Advanced cancer DISAT1Z9 Strong Biomarker [7]
Autism spectrum disorder DISXK8NV Strong Biomarker [8]
Bone osteosarcoma DIST1004 Strong Biomarker [9]
Breast neoplasm DISNGJLM Strong Altered Expression [10]
Colorectal carcinoma DIS5PYL0 Strong Genetic Variation [11]
Dilated cardiomyopathy 1A DIS0RK9Z Strong Altered Expression [12]
Endometrial cancer DISW0LMR Strong Genetic Variation [13]
Endometrial carcinoma DISXR5CY Strong Genetic Variation [13]
Esophageal squamous cell carcinoma DIS5N2GV Strong Biomarker [14]
Gastric cancer DISXGOUK Strong Genetic Variation [15]
Gastric neoplasm DISOKN4Y Strong Biomarker [6]
Glioma DIS5RPEH Strong Biomarker [16]
Head and neck carcinoma DISOU1DS Strong Biomarker [17]
Hepatocellular carcinoma DIS0J828 Strong Genetic Variation [18]
Hereditary diffuse gastric adenocarcinoma DISUIBYS Strong Biomarker [6]
Intellectual disability, autosomal dominant 40 DISAI0IH Strong Autosomal dominant [19]
Kleefstra syndrome 2 DISD3NER Strong Autosomal dominant [20]
leukaemia DISS7D1V Strong Genetic Variation [21]
Medulloblastoma DISZD2ZL Strong Genetic Variation [22]
Myelodysplastic syndrome DISYHNUI Strong Biomarker [23]
Neoplasm DISZKGEW Strong Genetic Variation [24]
Osteosarcoma DISLQ7E2 Strong Biomarker [9]
Pancreatic tumour DIS3U0LK Strong Biomarker [25]
Prostate cancer DISF190Y Strong Biomarker [26]
Prostate neoplasm DISHDKGQ Strong Biomarker [26]
Schizophrenia DISSRV2N Strong Biomarker [27]
Sezary syndrome DISFMTC7 Strong Biomarker [28]
Stomach cancer DISKIJSX Strong Genetic Variation [15]
Intellectual disability DISMBNXP moderate Biomarker [8]
Nasopharyngeal carcinoma DISAOTQ0 moderate Biomarker [7]
Cholangiocarcinoma DIS71F6X Limited Biomarker [29]
Intrahepatic cholangiocarcinoma DIS6GOC8 Limited Biomarker [29]
Leukemia DISNAKFL Limited Genetic Variation [21]
Lung cancer DISCM4YA Limited Biomarker [30]
Lung carcinoma DISTR26C Limited Biomarker [30]
Transitional cell carcinoma DISWVVDR Limited Biomarker [31]
Urinary bladder cancer DISDV4T7 Limited Biomarker [31]
Urinary bladder neoplasm DIS7HACE Limited Biomarker [31]
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⏷ Show the Full List of 44 Disease(s)
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
2 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the methylation of Histone-lysine N-methyltransferase 2C (KMT2C). [32]
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 affects the phosphorylation of Histone-lysine N-methyltransferase 2C (KMT2C). [48]
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19 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Tretinoin DM49DUI Approved Tretinoin increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [33]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [34]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [35]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [36]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [37]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [38]
Vorinostat DMWMPD4 Approved Vorinostat decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [39]
Marinol DM70IK5 Approved Marinol increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [40]
Ethanol DMDRQZU Approved Ethanol decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [41]
Nicotine DMWX5CO Approved Nicotine decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [42]
Tubocurarine DMBZIVP Approved Tubocurarine decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [42]
Urethane DM7NSI0 Phase 4 Urethane increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [43]
Epigallocatechin gallate DMCGWBJ Phase 3 Epigallocatechin gallate increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [44]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [45]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [46]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [47]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [37]
Milchsaure DM462BT Investigative Milchsaure increases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [49]
GALLICACID DM6Y3A0 Investigative GALLICACID decreases the expression of Histone-lysine N-methyltransferase 2C (KMT2C). [50]
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⏷ Show the Full List of 19 Drug(s)

References

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