Target Information
| Target General Information | Top | |||||
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| Target ID |
T33931
(Former ID: TTDI03345)
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| Target Name |
Lethal(3)malignant brain tumor-like 3 (L3MBTL3)
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| Synonyms |
MBT1; MBT-1; Lethal(3)malignant brain tumor-like protein 3; L(3)mbt-like protein 3; KIAA1798; H-l(3)mbt-like protein 3
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| Gene Name |
L3MBTL3
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Putative Polycomb group (PcG) protein. PcG proteins maintain the transcriptionally repressive state of genes, probably via a modification of chromatin, rendering it heritably changed in its expressibility. Required for normal maturation of myeloid progenitor cells (By similarity).
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| UniProt ID | ||||||
| Sequence |
MTESASSTSGQEFDVFSVMDWKDGVGTLPGSDLKFRVNEFGALEVITDENEMENVKKATA
TTTWMVPTAQEAPTSPPSSRPVFPPAYWTSPPGCPTVFSEKTGMPFRLKDPVKVEGLQFC ENCCQYGNVDECLSGGNYCSQNCARHIKDKDQKEERDVEEDNEEEDPKCSRKKKPKLSLK ADTKEDGEERDDEMENKQDVRILRGSQRARRKRRGDSAVLKQGLPPKGKKAWCWASYLEE EKAVAVPAKLFKEHQSFPYNKNGFKVGMKLEGVDPEHQSVYCVLTVAEVCGYRIKLHFDG YSDCYDFWVNADALDIHPVGWCEKTGHKLHPPKGYKEEEFNWQTYLKTCKAQAAPKSLFE NQNITVIPSGFRVGMKLEAVDKKNPSFICVATVTDMVDNRFLVHFDNWDESYDYWCEASS PHIHPVGWCKEHRRTLITPPGYPNVKHFSWDKYLEETNSLPAPARAFKVKPPHGFQKKMK LEVVDKRNPMFIRVATVADTDDHRVKVHFDGWNNCYDYWIDADSPDIHPVGWCSKTGHPL QPPLSPLELMEASEHGGCSTPGCKGIGHFKRARHLGPHSAANCPYSEINLNKDRIFPDRL SGEMPPASPSFPRNKRTDANESSSSPEIRDQHADDVKEDFEERTESEMRTSHEARGAREE PTVQQAQRRSAVFLSFKSPIPCLPLRWEQQSKLLPTVAGIPASKVSKWSTDEVSEFIQSL PGCEEHGKVFKDEQIDGEAFLLMTQTDIVKIMSIKLGPALKIFNSILMFKAAEKNSHNEL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: UNC1215 | Ligand Info | |||||
| Structure Description | Crystal structure of the complex of the 3-MBT repeat domain of L3MBTL3 and UNC1215 | PDB:4FL6 | ||||
| Method | X-ray diffraction | Resolution | 2.55 Å | Mutation | No | [1] |
| PDB Sequence |
AWCWASYLEE
240 EKAVAVPAKL250 FKEHQSFPYN260 KNGFKVGMKL270 EGVDPEHQSV280 YCVLTVAEVC 290 GYRIKLHFDG300 YSDCYDFWVN310 ADALDIHPVG320 WCEKTGHKLH330 PPKGYKEEEF 340 NWQTYLKTCK350 AQAAPKSLFE360 VIPSGFRVGM375 KLEAVDKKNP385 SFICVATVTD 395 MVDNRFLVHF405 DNWDESYDYW415 CEASSPHIHP425 VGWCKEHRRT435 LITPPGYPNV 445 KHFSWDKYLE455 ETNSLPAPAR465 AFKVKPPHGF475 QKKMKLEVVD485 KRNPMFIRVA 495 TVADTDDHRV505 KVHFDGWNNC515 YDYWIDADSP525 DIHPVGWCSK535 TGHPLQPPL |
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ASP274
3.015
HIS277
3.235
SER279
4.112
VAL280
3.893
CYS282
4.512
PHE298
3.631
TYR301
3.603
TYR305
3.476
HIS330
3.460
ASP381
2.625
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| Ligand Name: 4-(Pyrrolidin-1-Yl)-1-{4-[2-(Pyrrolidin-1-Yl)ethyl]phenyl}piperidine | Ligand Info | |||||
| Structure Description | Crystal structure of the 3-MBT repeat domain of L3MBTL3 and UNC2533 complex | PDB:4L59 | ||||
| Method | X-ray diffraction | Resolution | 2.29 Å | Mutation | No | [2] |
| PDB Sequence |
WCWASYLEEE
241 KAVAVPAKLF251 KEHQSFPYNK261 NGFKVGMKLE271 GVDPEHQSVY281 CVLTVAEVCG 291 YRIKLHFDGY301 SDCYDFWVNA311 DALDIHPVGW321 CEKTGHKLHP331 PKGYKEEEFN 341 WQTYLKTCKA351 QAAPKSLFEV366 IPSGFRVGMK376 LEAVDKKNPS386 FICVATVTDM 396 VDNRFLVHFD406 NWDESYDYWC416 EASSPHIHPV426 GWCKEHRRTL436 ITPPGYNVKH 447 FSWDKYLEET457 NSLPAPARAF467 KVKPPHGFQK477 KMKLEVVDKR487 NPMFIRVATV 497 ADTDDHRVKV507 HFDGWNNCYD517 YWIDADSPDI527 HPVGWCSKTG537 HPLQPPL |
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Similarity Proteins
Human Tissue Distribution
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| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
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| Sterile alpha motif domain-containing protein 11 (SAMD11) | 43.548 (27/62) | 3.35E-11 |
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Chemical Structure based Activity Landscape of Target | Top |
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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol. 2013 Mar;9(3):184-91. | |||||
| REF 2 | The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface. Medchemcomm. 2013 Nov;4(11):1501-1507. | |||||
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