Target General Infomation
Target ID
T77997
Former ID
TTDR01342
Target Name
mRNA of Human ADAM10
Gene Name
ADAM10
Synonyms
ADAM 10 (mRNA); ADAM10 (mRNA); CD156c (mRNA); CDw156 (mRNA); Disintegrin and metalloproteinase domaincontaining protein 10 (mRNA); Kuzbanian protein homolog (mRNA); Mammalian disintegrinmetalloprotease (mRNA); ADAM10
Target Type
Research
Function
Cleaves the membrane-bound precursor of TNF-alpha at '76-Ala-|-Val-77' to its mature soluble form. Responsible for the proteolytical release of soluble JAM3 from endothelial cells surface. Responsible for the proteolytic release of several other cell-surface proteins, including heparin-binding epidermal growth- like factor, ephrin-A2 and for constitutive and regulated alpha- secretase cleavage of amyloid precursor protein (APP). Contributes tothe normal cleavage of the cellular prion protein. Involved in the cleavage of the adhesion molecule L1 at the cell surface and in released membrane vesicles, suggesting a vesicle-based protease activity. Controls also the proteolytic processing of Notch and mediates lateral inhibition during neurogenesis. Responsible for the FasL ectodomain shedding and for the generation of the remnant ADAM10-processed FasL (FasL APL) transmembrane form. Also cleaves the ectodomain of the integral membrane proteins CORIN and ITM2B. May regulate the EFNA5-EPHA3 signaling.
BioChemical Class
Peptidase
Target Validation
T77997
UniProt ID
EC Number
EC 3.4.24.81
Sequence
MVLLRVLILLLSWAAGMGGQYGNPLNKYIRHYEGLSYNVDSLHQKHQRAKRAVSHEDQFL
RLDFHAHGRHFNLRMKRDTSLFSDEFKVETSNKVLDYDTSHIYTGHIYGEEGSFSHGSVI
DGRFEGFIQTRGGTFYVEPAERYIKDRTLPFHSVIYHEDDINYPHKYGPQGGCADHSVFE
RMRKYQMTGVEEVTQIPQEEHAANGPELLRKKRTTSAEKNTCQLYIQTDHLFFKYYGTRE
AVIAQISSHVKAIDTIYQTTDFSGIRNISFMVKRIRINTTADEKDPTNPFRFPNIGVEKF
LELNSEQNHDDYCLAYVFTDRDFDDGVLGLAWVGAPSGSSGGICEKSKLYSDGKKKSLNT
GIITVQNYGSHVPPKVSHITFAHEVGHNFGSPHDSGTECTPGESKNLGQKENGNYIMYAR
ATSGDKLNNNKFSLCSIRNISQVLEKKRNNCFVESGQPICGNGMVEQGEECDCGYSDQCK
DECCFDANQPEGRKCKLKPGKQCSPSQGPCCTAQCAFKSKSEKCRDDSDCAREGICNGFT
ALCPASDPKPNFTDCNRHTQVCINGQCAGSICEKYGLEECTCASSDGKDDKELCHVCCMK
KMDPSTCASTGSVQWSRHFSGRTITLQPGSPCNDFRGYCDVFMRCRLVDADGPLARLKKA
IFSPELYENIAEWIVAHWWAVLLMGIALIMLMAGFIKICSVHTPSSNPKLPPPKPLPGTL
KRRRPPQPIQQPQRQRPRESYQMGHMRR
Inhibitor compound 25 Drug Info [529206]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Alzheimer&#039
s disease
Epithelial cell signaling in Helicobacter pylori infection
NetPath Pathway RANKL Signaling Pathway
PANTHER Pathway Alzheimer disease-amyloid secretase pathway
Pathway Interaction Database Notch signaling pathway
Presenilin action in Notch and Wnt signaling
Posttranslational regulation of adherens junction stability and dissassembly
Reactome Collagen degradation
Degradation of the extracellular matrix
Activated NOTCH1 Transmits Signal to the Nucleus
Constitutive Signaling by NOTCH1 PEST Domain Mutants
Constitutive Signaling by NOTCH1 t(7
M1580_K2555) Translocation Mutant
Constitutive Signaling by NOTCH1 HD Domain Mutants
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
NOTCH2 Activation and Transmission of Signal to the Nucleus
EPH-ephrin mediated repulsion of cells
WikiPathways Hypertrophy Model
Copper homeostasis
Signaling by NOTCH3
Signaling by NOTCH4
Signaling by NOTCH2
Alzheimers Disease
Signaling by EGFR
References
Ref 529206Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations. Bioorg Med Chem Lett. 2008 Jan 15;18(2):560-4. Epub 2007 Nov28.
Ref 549627US patent application no. 6,228,648, Antisense modulation of ADAM10 expression.

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