Details of the Target

General Information of Target

Target ID LDTP03983
Target Name Protein AF-9 (MLLT3)
Gene Name MLLT3
Gene ID 4300
Synonyms
AF9; YEATS3; Protein AF-9; ALL1-fused gene from chromosome 9 protein; Myeloid/lymphoid or mixed-lineage leukemia translocated to chromosome 3 protein; YEATS domain-containing protein 3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASSCAVQVKLELGHRAQVRKKPTVEGFTHDWMVFVRGPEHSNIQHFVEKVVFHLHESFP
RPKRVCKDPPYKVEESGYAGFILPIEVYFKNKEEPRKVRFDYDLFLHLEGHPPVNHLRCE
KLTFNNPTEDFRRKLLKAGGDPNRSIHTSSSSSSSSSSSSSSSSSSSSSSSSSSSSSSSS
SSSSSSSSSSTSFSKPHKLMKEHKEKPSKDSREHKSAFKEPSRDHNKSSKESSKKPKENK
PLKEEKIVPKMAFKEPKPMSKEPKPDSNLLTITSGQDKKAPSKRPPISDSEELSAKKRKK
SSSEALFKSFSSAPPLILTCSADKKQIKDKSHVKMGKVKIESETSEKKKSTLPPFDDIVD
PNDSDVEENISSKSDSEQPSPASSSSSSSSSFTPSQTRQQGPLRSIMKDLHSDDNEEESD
EVEDNDNDSEMERPVNRGGSRSRRVSLSDGSDSESSSASSPLHHEPPPPLLKTNNNQILE
VKSPIKQSKSDKQIKNGECDKAYLDELVELHRRLMTLRERHILQQIVNLIEETGHFHITN
TTFDFDLCSLDKTTVRKLQSYLETSGTS
Target Bioclass
Other
Subcellular location
Nucleus
Function
Chromatin reader component of the super elongation complex (SEC), a complex required to increase the catalytic rate of RNA polymerase II transcription by suppressing transient pausing by the polymerase at multiple sites along the DNA. Specifically recognizes and binds acylated histone H3, with a preference for histone H3 that is crotonylated. Crotonylation marks active promoters and enhancers and confers resistance to transcriptional repressors. Recognizes and binds histone H3 crotonylated at 'Lys-9' (H3K9cr), and with slightly lower affinity histone H3 crotonylated at 'Lys-18' (H3K18cr). Also recognizes and binds histone H3 acetylated and butyrylated at 'Lys-9' (H3K9ac and H3K9bu, respectively), but with lower affinity than crotonylated histone H3. In the SEC complex, MLLT3 is required to recruit the complex to crotonylated histones. Recruitment of the SEC complex to crotonylated histones promotes recruitment of DOT1L on active chromatin to deposit histone H3 'Lys-79' methylation (H3K79me). Plays a key role in hematopoietic stem cell (HSC) maintenance by preserving, rather than conferring, HSC stemness. Acts by binding to the transcription start site of active genes in HSCs and sustaining level of H3K79me2, probably by recruiting DOT1L.
Uniprot ID
P42568
Ensemble ID
ENST00000380338.9
HGNC ID
HGNC:7136
ChEMBL ID
CHEMBL4295761

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.E40D .
MINO SNV: p.D357V .
MOLT4 Deletion: p.K325NfsTer3 .
NCIH1703 SNV: p.K257E .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C320(1.02)  LDD1492  [1]
NAIA_5
 Probe Info  		N.A.  LDD2224  [2]
IPM
 Probe Info  		C499(0.00); C320(0.00); C5(0.00)  LDD0147  [3]
TFBX
 Probe Info  		N.A.  LDD0148  [3]
VSF
 Probe Info  		N.A.  LDD0007  [4]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [5]
AOyne
 Probe Info  		13.50  LDD0443  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C320(1.02)  LDD1507  [1]
 LDCM0215  AC10 HEK-293T C320(1.08)  LDD1508  [1]
 LDCM0226  AC11 HEK-293T C320(1.02)  LDD1509  [1]
 LDCM0237  AC12 HEK-293T C320(1.14)  LDD1510  [1]
 LDCM0259  AC14 HEK-293T C320(0.99)  LDD1512  [1]
 LDCM0276  AC17 HEK-293T C320(1.16)  LDD1515  [1]
 LDCM0277  AC18 HEK-293T C320(0.99)  LDD1516  [1]
 LDCM0278  AC19 HEK-293T C320(0.96)  LDD1517  [1]
 LDCM0279  AC2 HEK-293T C320(0.96)  LDD1518  [1]
 LDCM0280  AC20 HEK-293T C320(1.15)  LDD1519  [1]
 LDCM0281  AC21 HEK-293T C320(0.93)  LDD1520  [1]
 LDCM0282  AC22 HEK-293T C320(1.09)  LDD1521  [1]
 LDCM0285  AC25 HEK-293T C320(1.05)  LDD1524  [1]
 LDCM0286  AC26 HEK-293T C320(1.01)  LDD1525  [1]
 LDCM0287  AC27 HEK-293T C320(1.01)  LDD1526  [1]
 LDCM0288  AC28 HEK-293T C320(1.06)  LDD1527  [1]
 LDCM0289  AC29 HEK-293T C320(1.14)  LDD1528  [1]
 LDCM0290  AC3 HEK-293T C320(0.90)  LDD1529  [1]
 LDCM0291  AC30 HEK-293T C320(1.14)  LDD1530  [1]
 LDCM0294  AC33 HEK-293T C320(0.95)  LDD1533  [1]
 LDCM0295  AC34 HEK-293T C320(1.09)  LDD1534  [1]
 LDCM0296  AC35 HEK-293T C320(0.92)  LDD1535  [1]
 LDCM0297  AC36 HEK-293T C320(1.27)  LDD1536  [1]
 LDCM0298  AC37 HEK-293T C320(0.93)  LDD1537  [1]
 LDCM0299  AC38 HEK-293T C320(1.01)  LDD1538  [1]
 LDCM0301  AC4 HEK-293T C320(1.07)  LDD1540  [1]
 LDCM0303  AC41 HEK-293T C320(1.21)  LDD1542  [1]
 LDCM0304  AC42 HEK-293T C320(1.15)  LDD1543  [1]
 LDCM0305  AC43 HEK-293T C320(0.88)  LDD1544  [1]
 LDCM0306  AC44 HEK-293T C320(1.19)  LDD1545  [1]
 LDCM0307  AC45 HEK-293T C320(1.16)  LDD1546  [1]
 LDCM0308  AC46 HEK-293T C320(0.97)  LDD1547  [1]
 LDCM0311  AC49 HEK-293T C320(0.94)  LDD1550  [1]
 LDCM0312  AC5 HEK-293T C320(1.19)  LDD1551  [1]
 LDCM0313  AC50 HEK-293T C320(1.04)  LDD1552  [1]
 LDCM0314  AC51 HEK-293T C320(1.03)  LDD1553  [1]
 LDCM0315  AC52 HEK-293T C320(1.08)  LDD1554  [1]
 LDCM0316  AC53 HEK-293T C320(0.89)  LDD1555  [1]
 LDCM0317  AC54 HEK-293T C320(1.34)  LDD1556  [1]
 LDCM0320  AC57 HEK-293T C320(1.01)  LDD1559  [1]
 LDCM0321  AC58 HEK-293T C320(1.00)  LDD1560  [1]
 LDCM0322  AC59 HEK-293T C320(1.10)  LDD1561  [1]
 LDCM0323  AC6 HEK-293T C320(1.34)  LDD1562  [1]
 LDCM0324  AC60 HEK-293T C320(1.29)  LDD1563  [1]
 LDCM0325  AC61 HEK-293T C320(1.26)  LDD1564  [1]
 LDCM0326  AC62 HEK-293T C320(1.59)  LDD1565  [1]
 LDCM0248  AKOS034007472 HEK-293T C320(1.05)  LDD1511  [1]
 LDCM0356  AKOS034007680 HEK-293T C320(1.05)  LDD1570  [1]
 LDCM0632  CL-Sc Hep-G2 C5(0.88)  LDD2227  [2]
 LDCM0367  CL1 HEK-293T C320(1.02)  LDD1571  [1]
 LDCM0368  CL10 HEK-293T C320(0.89)  LDD1572  [1]
 LDCM0370  CL101 HEK-293T C320(0.97)  LDD1574  [1]
 LDCM0372  CL103 HEK-293T C320(1.20)  LDD1576  [1]
 LDCM0374  CL105 HEK-293T C320(0.99)  LDD1578  [1]
 LDCM0376  CL107 HEK-293T C320(1.18)  LDD1580  [1]
 LDCM0378  CL109 HEK-293T C320(1.04)  LDD1582  [1]
 LDCM0381  CL111 HEK-293T C320(1.42)  LDD1585  [1]
 LDCM0383  CL113 HEK-293T C320(1.11)  LDD1587  [1]
 LDCM0385  CL115 HEK-293T C320(1.49)  LDD1589  [1]
 LDCM0387  CL117 HEK-293T C320(1.04)  LDD1591  [1]
 LDCM0389  CL119 HEK-293T C320(1.20)  LDD1593  [1]
 LDCM0392  CL121 HEK-293T C320(0.99)  LDD1596  [1]
 LDCM0394  CL123 HEK-293T C320(0.97)  LDD1598  [1]
 LDCM0396  CL125 HEK-293T C320(1.06)  LDD1600  [1]
 LDCM0398  CL127 HEK-293T C320(2.01)  LDD1602  [1]
 LDCM0400  CL13 HEK-293T C320(1.14)  LDD1604  [1]
 LDCM0402  CL15 HEK-293T C320(0.88)  LDD1606  [1]
 LDCM0404  CL17 HEK-293T C320(1.06)  LDD1608  [1]
 LDCM0405  CL18 HEK-293T C320(1.20)  LDD1609  [1]
 LDCM0406  CL19 HEK-293T C320(1.29)  LDD1610  [1]
 LDCM0408  CL20 HEK-293T C320(1.04)  LDD1612  [1]
 LDCM0409  CL21 HEK-293T C320(0.66)  LDD1613  [1]
 LDCM0410  CL22 HEK-293T C320(0.58)  LDD1614  [1]
 LDCM0413  CL25 HEK-293T C320(0.94)  LDD1617  [1]
 LDCM0415  CL27 HEK-293T C320(1.19)  LDD1619  [1]
 LDCM0417  CL29 HEK-293T C320(1.25)  LDD1621  [1]
 LDCM0418  CL3 HEK-293T C320(1.48)  LDD1622  [1]
 LDCM0419  CL30 HEK-293T C320(1.18)  LDD1623  [1]
 LDCM0420  CL31 HEK-293T C320(1.06)  LDD1624  [1]
 LDCM0421  CL32 HEK-293T C320(1.08)  LDD1625  [1]
 LDCM0422  CL33 HEK-293T C320(0.63)  LDD1626  [1]
 LDCM0423  CL34 HEK-293T C320(0.50)  LDD1627  [1]
 LDCM0426  CL37 HEK-293T C320(0.95)  LDD1630  [1]
 LDCM0428  CL39 HEK-293T C320(0.98)  LDD1632  [1]
 LDCM0431  CL41 HEK-293T C320(1.02)  LDD1635  [1]
 LDCM0432  CL42 HEK-293T C320(1.07)  LDD1636  [1]
 LDCM0433  CL43 HEK-293T C320(1.16)  LDD1637  [1]
 LDCM0434  CL44 HEK-293T C320(1.14)  LDD1638  [1]
 LDCM0435  CL45 HEK-293T C320(0.67)  LDD1639  [1]
 LDCM0436  CL46 HEK-293T C320(0.68)  LDD1640  [1]
 LDCM0439  CL49 HEK-293T C320(1.10)  LDD1643  [1]
 LDCM0440  CL5 HEK-293T C320(1.19)  LDD1644  [1]
 LDCM0444  CL53 HEK-293T C320(1.17)  LDD1647  [1]
 LDCM0445  CL54 HEK-293T C320(1.06)  LDD1648  [1]
 LDCM0446  CL55 HEK-293T C320(1.13)  LDD1649  [1]
 LDCM0447  CL56 HEK-293T C320(1.16)  LDD1650  [1]
 LDCM0448  CL57 HEK-293T C320(0.67)  LDD1651  [1]
 LDCM0449  CL58 HEK-293T C320(0.66)  LDD1652  [1]
 LDCM0451  CL6 HEK-293T C320(1.05)  LDD1654  [1]
 LDCM0453  CL61 HEK-293T C320(1.02)  LDD1656  [1]
 LDCM0455  CL63 HEK-293T C320(1.23)  LDD1658  [1]
 LDCM0457  CL65 HEK-293T C320(1.08)  LDD1660  [1]
 LDCM0458  CL66 HEK-293T C320(1.24)  LDD1661  [1]
 LDCM0459  CL67 HEK-293T C320(1.00)  LDD1662  [1]
 LDCM0460  CL68 HEK-293T C320(1.04)  LDD1663  [1]
 LDCM0461  CL69 HEK-293T C320(0.66)  LDD1664  [1]
 LDCM0462  CL7 HEK-293T C320(1.01)  LDD1665  [1]
 LDCM0463  CL70 HEK-293T C320(0.61)  LDD1666  [1]
 LDCM0466  CL73 HEK-293T C320(1.02)  LDD1669  [1]
 LDCM0470  CL77 HEK-293T C320(0.94)  LDD1673  [1]
 LDCM0471  CL78 HEK-293T C320(1.08)  LDD1674  [1]
 LDCM0472  CL79 HEK-293T C320(1.16)  LDD1675  [1]
 LDCM0473  CL8 HEK-293T C320(0.96)  LDD1676  [1]
 LDCM0474  CL80 HEK-293T C320(1.20)  LDD1677  [1]
 LDCM0475  CL81 HEK-293T C320(0.72)  LDD1678  [1]
 LDCM0476  CL82 HEK-293T C320(0.76)  LDD1679  [1]
 LDCM0479  CL85 HEK-293T C320(1.05)  LDD1682  [1]
 LDCM0481  CL87 HEK-293T C320(1.58)  LDD1684  [1]
 LDCM0483  CL89 HEK-293T C320(1.05)  LDD1686  [1]
 LDCM0484  CL9 HEK-293T C320(0.71)  LDD1687  [1]
 LDCM0485  CL90 HEK-293T C320(0.95)  LDD1688  [1]
 LDCM0486  CL91 HEK-293T C320(1.13)  LDD1689  [1]
 LDCM0487  CL92 HEK-293T C320(1.17)  LDD1690  [1]
 LDCM0488  CL93 HEK-293T C320(0.76)  LDD1691  [1]
 LDCM0489  CL94 HEK-293T C320(0.88)  LDD1692  [1]
 LDCM0492  CL97 HEK-293T C320(0.97)  LDD1695  [1]
 LDCM0494  CL99 HEK-293T C320(1.46)  LDD1697  [1]
 LDCM0495  E2913 HEK-293T C320(1.28)  LDD1698  [1]
 LDCM0468  Fragment33 HEK-293T C320(1.26)  LDD1671  [1]
 LDCM0022  KB02 HEK-293T C320(1.02)  LDD1492  [1]
 LDCM0023  KB03 HEK-293T C320(1.05)  LDD1497  [1]
 LDCM0024  KB05 HEK-293T C320(1.00)  LDD1502  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Alpha-ketoglutarate-dependent dioxygenase alkB homolog 4 (ALKBH4) AlkB family Q9NXW9
Histone-lysine N-methyltransferase, H3 lysine-79 specific (DOT1L) DOT1 family Q8TEK3
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
AF4/FMR2 family member 1 (AFF1) AF4 family P51825
AF4/FMR2 family member 4 (AFF4) AF4 family Q9UHB7
Zinc finger protein 572 (ZNF572) Krueppel C2H2-type zinc-finger protein family Q7Z3I7
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein FAM9A (FAM9A) FAM9 family Q8IZU1
Amyloid protein-binding protein 2 (APPBP2) . Q92624
Chromobox protein homolog 8 (CBX8) . Q9HC52
Migration and invasion-inhibitory protein (MIIP) . Q5JXC2

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 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
3 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
4 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
5 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
6 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.