Details of the Target
General Information of Target
| Target ID | LDTP09879 | |||||
|---|---|---|---|---|---|---|
| Target Name | Histone-lysine N-methyltransferase EZH1 (EZH1) | |||||
| Gene Name | EZH1 | |||||
| Gene ID | 2145 | |||||
| Synonyms |
KIAA0388; Histone-lysine N-methyltransferase EZH1; EC 2.1.1.356; ENX-2; Enhancer of zeste homolog 1 |
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| 3D Structure | ||||||
| Sequence |
MASGSGDSVTRRSVASQFFTQEEGPGIDGMTTSERVVDLLNQAALITNDSKITVLKQVQE
LIINKDPTLLDNFLDEIIAFQADKSIEVRKFVIGFIEEACKRDIELLLKLIANLNMLLRD ENVNVVKKAILTMTQLYKVALQWMVKSRVISELQEACWDMVSAMAGDIILLLDSDNDGIR THAIKFVEGLIVTLSPRMADSEIPRRQEHDISLDRIPRDHPYIQYNVLWEEGKAALEQLL KFMVHPAISSINLTTALGSLANIARQRPMFMSEVIQAYETLHANLPPTLAKSQVSSVRKN LKLHLLSVLKHPASLEFQAQITTLLVDLGTPQAEIARNMPSSKDTRKRPRDDSDSTLKKM KLEPNLGEDDEDKDLEPGPSGTSKASAQISGQSDTDITAEFLQPLLTPDNVANLVLISMV YLPEAMPASFQAIYTPVESAGTEAQIKHLARLMATQMTAAGLGPGVEQTKQCKEEPKEEK VVKTESVLIKRRLSAQGQAISVVGSLSSMSPLEEEAPQAKRRPEPIIPVTQPRLAGAGGR KKIFRLSDVLKPLTDAQVEAMKLGAVKRILRAEKAVACSGAAQVRIKILASLVTQFNSGL KAEVLSFILEDVRARLDLAFAWLYQEYNAYLAAGASGSLDKYEDCLIRLLSGLQEKPDQK DGIFTKVVLEAPLITESALEVVRKYCEDESRTYLGMSTLRDLIFKRPSRQFQYLHVLLDL SSHEKDKVRSQALLFIKRMYEKEQLREYVEKFALNYLQLLVHPNPPSVLFGADKDTEVAA PWTEETVKQCLYLYLALLPQNHKLIHELAAVYTEAIADIKRTVLRVIEQPIRGMGMNSPE LLLLVENCPKGAETLVTRCLHSLTDKVPPSPELVKRVRDLYHKRLPDVRFLIPVLNGLEK KEVIQALPKLIKLNPIVVKEVFNRLLGTQHGEGNSALSPLNPGELLIALHNIDSVKCDMK SIIKATNLCFAERNVYTSEVLAVVMQQLMEQSPLPMLLMRTVIQSLTMYPRLGGFVMNIL SRLIMKQVWKYPKVWEGFIKCCQRTKPQSFQVILQLPPQQLGAVFDKCPELREPLLAHVR SFTPHQQAHIPNSIMTILEASGKQEPEAKEAPAGPLEEDDLEPLTLAPAPAPRPPQDLIG LRLAQEKALKRQLEEEQKLKPGGVGAPSSSSPSPSPSARPGPPPSEEAMDFREEGPECET PGIFISMDDDSGLTEAALLDSSLEGPLPKETAAGGLTLKEERSPQTLAPVGEDAMKTPSP AAEDAREPEAKGNS |
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| Target Type |
Clinical trial
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| Target Bioclass |
Enzyme
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| Family |
Class V-like SAM-binding methyltransferase superfamily, Histone-lysine methyltransferase family, EZ subfamily
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| Subcellular location |
Nucleus
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| Function |
Polycomb group (PcG) protein. Catalytic subunit of the PRC2/EED-EZH1 complex, which methylates 'Lys-27' of histone H3, leading to transcriptional repression of the affected target gene. Able to mono-, di- and trimethylate 'Lys-27' of histone H3 to form H3K27me1, H3K27me2 and H3K27me3, respectively. Required for embryonic stem cell derivation and self-renewal, suggesting that it is involved in safeguarding embryonic stem cell identity. Compared to EZH2-containing complexes, it is less abundant in embryonic stem cells, has weak methyltransferase activity and plays a less critical role in forming H3K27me3, which is required for embryonic stem cell identity and proper differentiation.
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| TTD ID | ||||||
| Uniprot ID | ||||||
| DrugMap ID | ||||||
| Ensemble ID | ||||||
| HGNC ID | ||||||
| ChEMBL ID | ||||||
Target Site Mutations in Different Cell Lines
| Cell line | Mutation details | Probe for labeling this protein in this cell | |||
|---|---|---|---|---|---|
| G415 | SNV: p.A427S | DBIA Probe Info | |||
| HCT15 | SNV: p.E191D | . | |||
| HEC1 | SNV: p.R321C | . | |||
| HEC1B | SNV: p.R321C | . | |||
| IM95 | SNV: p.R443Ter | . | |||
| JURKAT | SNV: p.R557H | . | |||
| KURAMOCHI | SNV: p.R557C | . | |||
| MCC13 | SNV: p.R360C;p.S632F;p.Q718Ter Substitution: p.S358I |
. | |||
| MEWO | SNV: p.P133L | DBIA Probe Info | |||
| MFE319 | SNV: p.Q467R | . | |||
| MOLT4 | SNV: p.G200E | . | |||
| NCIH1155 | SNV: p.R287W | DBIA Probe Info | |||
| REH | SNV: p.C537Y | . | |||
| SKMEL30 | Substitution: p.R708Q | . | |||
| SKMEL5 | SNV: p.P4L | DBIA Probe Info | |||
| SUDHL4 | SNV: p.I3V | . | |||
| SUPT1 | SNV: p.E163Ter | . | |||
| TC71 | SNV: p.R443Ter | . | |||
| UACC62 | SNV: p.G222S | DBIA Probe Info | |||
Probe(s) Labeling This Target
ABPP Probe
| Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
|---|---|---|---|---|---|
|
DBIA Probe Info |
 |
C17(2.90) | LDD3312 | [1] | |
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BTD Probe Info |
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C696(1.30) | LDD2107 | [2] | |
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AHL-Pu-1 Probe Info |
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C504(2.18) | LDD0171 | [3] | |
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IA-alkyne Probe Info |
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C11(5.99) | LDD1703 | [4] | |
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NAIA_4 Probe Info |
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N.A. | LDD2226 | [5] | |
Competitor(s) Related to This Target
| Competitor ID | Name | Cell line | Binding Site(Ratio) | Interaction ID | Ref |
|---|---|---|---|---|---|
| LDCM0026 | 4SU-RNA+native RNA | DM93 | C504(2.18) | LDD0171 | [3] |
| LDCM0022 | KB02 | T cell | C11(5.99) | LDD1703 | [4] |
| LDCM0023 | KB03 | A101D | C17(5.45) | LDD2667 | [1] |
| LDCM0024 | KB05 | HMCB | C17(2.90) | LDD3312 | [1] |
| LDCM0514 | Nucleophilic fragment 20a | MDA-MB-231 | C696(1.30) | LDD2107 | [2] |
| LDCM0532 | Nucleophilic fragment 29a | MDA-MB-231 | C605(1.14) | LDD2125 | [2] |
| LDCM0543 | Nucleophilic fragment 38 | MDA-MB-231 | C605(1.26) | LDD2136 | [2] |
| LDCM0546 | Nucleophilic fragment 40 | MDA-MB-231 | C605(0.80) | LDD2140 | [2] |
The Interaction Atlas With This Target
The Protein(s) Related To This Target
Other
| Protein name | Family | Uniprot ID | |||
|---|---|---|---|---|---|
| Polycomb protein EED (EED) | WD repeat ESC family | O75530 | |||
The Drug(s) Related To This Target
Approved
| Drug Name | Drug Type | External ID | |||
|---|---|---|---|---|---|
| Tazemetostat | Small molecular drug | DB12887 | |||
Phase 2
| Drug Name | Drug Type | External ID | |||
|---|---|---|---|---|---|
| Ds-3201b | Small molecular drug | DNM79H | |||
Phase 1
| Drug Name | Drug Type | External ID | |||
|---|---|---|---|---|---|
| Hh2853 | Small molecular drug | D6EU7R | |||
| Ds-3201 | . | D0LG8T | |||
Investigative
| Drug Name | Drug Type | External ID | |||
|---|---|---|---|---|---|
| Gsk343 | Small molecular drug | D02TVQ | |||
References