Details of the Target

General Information of Target

Target ID LDTP05392
Target Name Histone-lysine N-methyltransferase MECOM (MECOM)
Gene Name MECOM
Gene ID 2122
Synonyms
EVI1; MDS1; PRDM3; Histone-lysine N-methyltransferase MECOM; EC 2.1.1.367; Ecotropic virus integration site 1 protein homolog; EVI-1; MDS1 and EVI1 complex locus protein; Myelodysplasia syndrome 1 protein; Myelodysplasia syndrome-associated protein 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRSKGRARKLATNNECVYGNYPEIPLEEMPDADGVASTPSLNIQEPCSPATSSEAFTPKE
GSPYKAPIYIPDDIPIPAEFELRESNMPGAGLGIWTKRKIEVGEKFGPYVGEQRSNLKDP
SYGWEILDEFYNVKFCIDASQPDVGSWLKYIRFAGCYDQHNLVACQINDQIFYRVVADIA
PGEELLLFMKSEDYPHETMAPDIHEERQYRCEDCDQLFESKAELADHQKFPCSTPHSAFS
MVEEDFQQKLESENDLQEIHTIQECKECDQVFPDLQSLEKHMLSHTEEREYKCDQCPKAF
NWKSNLIRHQMSHDSGKHYECENCAKVFTDPSNLQRHIRSQHVGARAHACPECGKTFATS
SGLKQHKHIHSSVKPFICEVCHKSYTQFSNLCRHKRMHADCRTQIKCKDCGQMFSTTSSL
NKHRRFCEGKNHFAAGGFFGQGISLPGTPAMDKTSMVNMSHANPGLADYFGANRHPAGLT
FPTAPGFSFSFPGLFPSGLYHRPPLIPASSPVKGLSSTEQTNKSQSPLMTHPQILPATQD
ILKALSKHPSVGDNKPVELQPERSSEERPFEKISDQSESSDLDDVSTPSGSDLETTSGSD
LESDIESDKEKFKENGKMFKDKVSPLQNLASINNKKEYSNHSIFSPSLEEQTAVSGAVND
SIKAIASIAEKYFGSTGLVGLQDKKVGALPYPSMFPLPFFPAFSQSMYPFPDRDLRSLPL
KMEPQSPGEVKKLQKGSSESPFDLTTKRKDEKPLTPVPSKPPVTPATSQDQPLDLSMGSR
SRASGTKLTEPRKNHVFGGKKGSNVESRPASDGSLQHARPTPFFMDPIYRVEKRKLTDPL
EALKEKYLRPSPGFLFHPQMSAIENMAEKLESFSALKPEASELLQSVPSMFNFRAPPNAL
PENLLRKGKERYTCRYCGKIFPRSANLTRHLRTHTGEQPYRCKYCDRSFSISSNLQRHVR
NIHNKEKPFKCHLCDRCFGQQTNLDRHLKKHENGNMSGTATSSPHSELESTGAILDDKED
AYFTEIRNFIGNSNHGSQSPRNVEERMNGSHFKDEKALVTSQNSDLLDDEEVEDEVLLDE
EDEDNDITGKTGKEPVTSNLHEGNPEDDYEETSALEMSCKTSPVRYKEEEYKSGLSALDH
IRHFTDSLKMRKMEDNQYSEAELSSFSTSHVPEELKQPLHRKSKSQAYAMMLSLSDKESL
HSTSHSSSNVWHSMARAAAESSAIQSISHV
Target Bioclass
Enzyme
Subcellular location
Nucleus
Function
[Isoform 1]: Functions as a transcriptional regulator binding to DNA sequences in the promoter region of target genes and regulating positively or negatively their expression. Oncogene which plays a role in development, cell proliferation and differentiation. May also play a role in apoptosis through regulation of the JNK and TGF-beta signaling. Involved in hematopoiesis.; [Isoform 7]: Displays histone methyltransferase activity and monomethylates 'Lys-9' of histone H3 (H3K9me1) in vitro. Probably catalyzes the monomethylation of free histone H3 in the cytoplasm which is then transported to the nucleus and incorporated into nucleosomes where SUV39H methyltransferases use it as a substrate to catalyze histone H3 'Lys-9' trimethylation. Likely to be one of the primary histone methyltransferases along with PRDM16 that direct cytoplasmic H3K9me1 methylation.
Uniprot ID
Q03112
Ensemble ID
ENST00000264674.7
HGNC ID
HGNC:3498
ChEMBL ID
CHEMBL5214865

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C1119(1.03)  LDD1492  [1]
Phosphinate-6
 Probe Info  		C156(0.00); C392(0.00)  LDD0018  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C156(1.04)  LDD1507  [1]
 LDCM0276  AC17 HEK-293T C156(0.83)  LDD1515  [1]
 LDCM0284  AC24 HEK-293T C1119(1.03)  LDD1523  [1]
 LDCM0285  AC25 HEK-293T C156(0.83)  LDD1524  [1]
 LDCM0293  AC32 HEK-293T C1119(0.98)  LDD1532  [1]
 LDCM0294  AC33 HEK-293T C156(0.84)  LDD1533  [1]
 LDCM0302  AC40 HEK-293T C1119(0.87)  LDD1541  [1]
 LDCM0303  AC41 HEK-293T C156(1.01)  LDD1542  [1]
 LDCM0310  AC48 HEK-293T C1119(0.90)  LDD1549  [1]
 LDCM0311  AC49 HEK-293T C156(1.33)  LDD1550  [1]
 LDCM0319  AC56 HEK-293T C1119(1.06)  LDD1558  [1]
 LDCM0320  AC57 HEK-293T C156(0.90)  LDD1559  [1]
 LDCM0328  AC64 HEK-293T C1119(1.32)  LDD1567  [1]
 LDCM0345  AC8 HEK-293T C1119(1.04)  LDD1569  [1]
 LDCM0356  AKOS034007680 HEK-293T C156(0.92)  LDD1570  [1]
 LDCM0275  AKOS034007705 HEK-293T C1119(1.12)  LDD1514  [1]
 LDCM0371  CL102 HEK-293T C1119(0.82)  LDD1575  [1]
 LDCM0375  CL106 HEK-293T C1119(0.64)  LDD1579  [1]
 LDCM0380  CL110 HEK-293T C1119(0.94)  LDD1584  [1]
 LDCM0384  CL114 HEK-293T C1119(0.69)  LDD1588  [1]
 LDCM0388  CL118 HEK-293T C1119(0.97)  LDD1592  [1]
 LDCM0390  CL12 HEK-293T C1119(1.00)  LDD1594  [1]
 LDCM0393  CL122 HEK-293T C1119(0.72)  LDD1597  [1]
 LDCM0397  CL126 HEK-293T C1119(0.67)  LDD1601  [1]
 LDCM0401  CL14 HEK-293T C1119(0.83)  LDD1605  [1]
 LDCM0404  CL17 HEK-293T C156(1.06)  LDD1608  [1]
 LDCM0407  CL2 HEK-293T C1119(1.03)  LDD1611  [1]
 LDCM0412  CL24 HEK-293T C1119(0.93)  LDD1616  [1]
 LDCM0414  CL26 HEK-293T C1119(0.90)  LDD1618  [1]
 LDCM0417  CL29 HEK-293T C156(0.93)  LDD1621  [1]
 LDCM0425  CL36 HEK-293T C1119(1.05)  LDD1629  [1]
 LDCM0431  CL41 HEK-293T C156(0.81)  LDD1635  [1]
 LDCM0438  CL48 HEK-293T C1119(1.19)  LDD1642  [1]
 LDCM0440  CL5 HEK-293T C156(0.97)  LDD1644  [1]
 LDCM0441  CL50 HEK-293T C1119(0.82)  LDD1645  [1]
 LDCM0444  CL53 HEK-293T C156(0.92)  LDD1647  [1]
 LDCM0452  CL60 HEK-293T C1119(0.94)  LDD1655  [1]
 LDCM0454  CL62 HEK-293T C1119(0.79)  LDD1657  [1]
 LDCM0457  CL65 HEK-293T C156(1.48)  LDD1660  [1]
 LDCM0465  CL72 HEK-293T C1119(1.49)  LDD1668  [1]
 LDCM0467  CL74 HEK-293T C1119(0.89)  LDD1670  [1]
 LDCM0470  CL77 HEK-293T C156(0.87)  LDD1673  [1]
 LDCM0478  CL84 HEK-293T C1119(0.96)  LDD1681  [1]
 LDCM0480  CL86 HEK-293T C1119(0.81)  LDD1683  [1]
 LDCM0483  CL89 HEK-293T C156(0.94)  LDD1686  [1]
 LDCM0491  CL96 HEK-293T C1119(0.78)  LDD1694  [1]
 LDCM0493  CL98 HEK-293T C1119(0.82)  LDD1696  [1]
 LDCM0427  Fragment51 HEK-293T C1119(1.00)  LDD1631  [1]
 LDCM0022  KB02 HEK-293T C1119(1.03)  LDD1492  [1]
 LDCM0023  KB03 HEK-293T C1119(1.37)  LDD1497  [1]
 LDCM0024  KB05 HEK-293T C1119(1.05)  LDD1502  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
NAD-dependent protein deacetylase sirtuin-1 (SIRT1) Sirtuin family Q96EB6
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Chloride intracellular channel protein 3 (CLIC3) Chloride channel CLIC family O95833
Wolframin (WFS1) . O76024
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein c-Fos (FOS) BZIP family P01100
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock protein beta-1 (HSPB1) Small heat shock protein (HSP20) family P04792
Protein UXT (UXT) UXT family Q9UBK9
Histone-binding protein RBBP4 (RBBP4) WD repeat RBAP46/RBAP48/MSI1 family Q09028
RING finger protein 11 (RNF11) . Q9Y3C5

References

1 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
2 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004