Target Information
Target General Information | Top | |||||
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Target ID |
T95761
(Former ID: TTDR00920)
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Target Name |
Cell surface antigen MS2 (ADAM8)
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Synonyms |
CD156a antigen; CD156; ADAM8; A disintegrin and metalloproteinase domain 8
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Gene Name |
ADAM8
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Target Type |
Literature-reported target
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[1] | ||||
Function |
Possible involvement in extravasation of leukocytes.
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BioChemical Class |
Peptidase
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UniProt ID | ||||||
EC Number |
EC 3.4.24.-
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Sequence |
MRGLGLWLLGAMMLPAIAPSRPWALMEQYEVVLPWRLPGPRVRRALPSHLGLHPERVSYV
LGATGHNFTLHLRKNRDLLGSGYTETYTAANGSEVTEQPRGQDHCFYQGHVEGYPDSAAS LSTCAGLRGFFQVGSDLHLIEPLDEGGEGGRHAVYQAEHLLQTAGTCGVSDDSLGSLLGP RTAAVFRPRPGDSLPSRETRYVELYVVVDNAEFQMLGSEAAVRHRVLEVVNHVDKLYQKL NFRVVLVGLEIWNSQDRFHVSPDPSVTLENLLTWQARQRTRRHLHDNVQLITGVDFTGTT VGFARVSAMCSHSSGAVNQDHSKNPVGVACTMAHEMGHNLGMDHDENVQGCRCQERFEAG RCIMAGSIGSSFPRMFSDCSQAYLESFLERPQSVCLANAPDLSHLVGGPVCGNLFVERGE QCDCGPPEDCRNRCCNSTTCQLAEGAQCAHGTCCQECKVKPAGELCRPKKDMCDLEEFCD GRHPECPEDAFQENGTPCSGGYCYNGACPTLAQQCQAFWGPGGQAAEESCFSYDILPGCK ASRYRADMCGVLQCKGGQQPLGRAICIVDVCHALTTEDGTAYEPVPEGTRCGPEKVCWKG RCQDLHVYRSSNCSAQCHNHGVCNHKQECHCHAGWAPPHCAKLLTEVHAASGSLPVFVVV VLVLLAVVLVTLAGIIVYRKARSRILSRNVAPKTTMGRSNPLFHQAASRVPAKGGAPAPS RGPQELVPTTHPGQPARHPASSVALKRPPPAPPVTVSSPPFPVPVYTRQAPKQVIKPTFA PPVPPVKPGAGAANPGPAEGAVGPKVALKPPIQRKQGAGAPTAP 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: Batimastat | Ligand Info | |||||
Structure Description | ADAM-8 metalloproteinase domain with bound batimastat | PDB:4DD8 | ||||
Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | No | [2] |
PDB Sequence |
RETRYVELYV
206 VVDNAEFQML216 GSEAAVRHRV226 LEVVNHVDKL236 YQKLNFRVVL246 VGLEIWNSQD 256 RFHVSPDPSV266 TLENLLTWQA276 RRHLHDNVQL290 ITGVDFTGTT300 VGFARVSAMC 310 SHSSGAVNQD320 HSKNPVGVAC330 TMAHEMGHNL340 GMDHDENVQG350 CRCQERFEAG 360 RCIMAGSIGS370 SFPRMFSDCS380 QAYLESFLER390 PQSVCLANAP400 D |
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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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Microtubule-actin cross-linking factor 1, isoforms 6/7 (MACF1) | 29.545 (39/132) | 1.65E-04 | |
Teneurin-3 (TENM3) | 32.710 (35/107) | 1.00E-03 |
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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References | Top | |||||
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REF 1 | Catalytic activity of ADAM8, ADAM15, and MDC-L (ADAM28) on synthetic peptide substrates and in ectodomain cleavage of CD23. J Biol Chem. 2003 Aug 15;278(33):30469-77. | |||||
REF 2 | Structure of human ADAM-8 catalytic domain complexed with batimastat. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Jun 1;68(Pt 6):616-21. |
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