Target Information
Target General Information | Top | |||||
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Target ID |
T92463
(Former ID: TTDR01346)
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Target Name |
RIP2 messenger RNA (RIP2 mRNA)
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Synonyms |
UNQ277/PRO314/PRO34092 (mRNA); Tyrosine-protein kinase RIPK2 (mRNA); Receptor-interacting serine/threonine-protein kinase 2 (mRNA); Receptor-interacting protein 2 (mRNA); RIP2 (mRNA); RIP-like-interacting CLARP kinase (mRNA); RIP-2 (mRNA); RICK (mRNA); CARDIAK (mRNA); CARD-containing interleukin-1 beta-converting enzyme-associated kinase (mRNA); CARD-containing IL-1 beta ICE-kinase (mRNA)
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Gene Name |
RIPK2
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Target Type |
Clinical trial target
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[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Cardiovascular disease [ICD-11: BA00-BE2Z] | |||||
2 | Postoperative inflammation [ICD-11: 1A00-CA43] | |||||
Function |
Upon stimulation by bacterial peptidoglycans, NOD1 and NOD2 are activated, oligomerize and recruit RIPK2 through CARD-CARD domains. Contributes to the tyrosine phosphorylation of the guanine exchange factor ARHGEF2 through Src tyrosine kinase leading to NF-kappaB activation by NOD2. Once recruited, RIPK2 autophosphorylates and undergoes 'Lys-63'-linked polyubiquitination by E3 ubiquitin ligases XIAP, BIRC2 and BIRC3. The polyubiquitinated protein mediates the recruitment of MAP3K7/TAK1 to IKBKG/NEMO and induces 'Lys-63'-linked polyubiquitination of IKBKG/NEMO and subsequent activation of IKBKB/IKKB. In turn, NF-kappa-B is released from NF-kappa-B inhibitors and translocates into the nucleus where it activates the transcription of hundreds of genes involved in immune response, growth control, or protection against apoptosis. Plays also a role during engagement of the T-cell receptor (TCR) in promoting BCL10 phosphorylation and subsequent NF-kappa-B activation. Serine/threonine/tyrosine kinase that plays an essential role in modulation of innate and adaptive immune responses.
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BioChemical Class |
mRNA target
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UniProt ID | ||||||
EC Number |
EC 2.7.11.1
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Sequence |
MNGEAICSALPTIPYHKLADLRYLSRGASGTVSSARHADWRVQVAVKHLHIHTPLLDSER
KDVLREAEILHKARFSYILPILGICNEPEFLGIVTEYMPNGSLNELLHRKTEYPDVAWPL RFRILHEIALGVNYLHNMTPPLLHHDLKTQNILLDNEFHVKIADFGLSKWRMMSLSQSRS SKSAPEGGTIIYMPPENYEPGQKSRASIKHDIYSYAVITWEVLSRKQPFEDVTNPLQIMY SVSQGHRPVINEESLPYDIPHRARMISLIESGWAQNPDERPSFLKCLIELEPVLRTFEEI TFLEAVIQLKKTKLQSVSSAIHLCDKKKMELSLNIPVNHGPQEESCGSSQLHENSGSPET SRSLPAPQDNDFLSRKAQDCYFMKLHHCPGNHSWDSTISGSQRAAFCDHKTTPCSSAIIN PLSTAGNSERLQPGIAQQWIQSKREDIVNQMTEACLNQSLDALLSRDLIMKEDYELVSTK PTRTSKVRQLLDTTDIQGEEFAKVIVQKLKDNKQMGLQPYPEILVVSRSPSLNLLQNKSM Click to Show/Hide
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HIT2.0 ID | T02AK2 |
Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
1 | ISIS-CRP | Drug Info | Phase 1 | Inflammation | [2] | |
Mode of Action | [+] 1 Modes of Action | + | ||||
Inhibitor | [+] 3 Inhibitor drugs | + | ||||
1 | ISIS-CRP | Drug Info | [1] | |||
2 | NM-PP1 | Drug Info | [1] | |||
3 | Src kinase inhibitor I | Drug Info | [1] |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. | |||||
REF 2 | Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011). | |||||
REF 3 | US patent application no. 6,426,221, Antisense modulation of RIP2 expression. |
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