靶点信息58(本栏目收费,不能显示细节,电话13136136841)
靶点信息
标题
内容
相关药物
状态
TARGETID
T62841
FORMERID
TTDR00109
UNIPROID
PAR2_HUMAN
TARGNAME
Proteinase activated receptor 2 (PAR2)
GENENAME
F2RL1
TARGTYPE
Patented-recorded target
SYNONYMS
Thrombin receptor-like 1; Proteinase-activated receptor-2; Proteinase-activated receptor 2; Protease activated receptor 2; PAR-2; GPR11; G-protein coupled receptor 11; Coagulation factor II receptor-like 1
FUNCTION
Its function is mediated through the activation of several signaling pathways including phospholipase C (PLC), intracellular calcium, mitogen-activated protein kinase (MAPK), I-kappaB kinase/NF-kappaB and Rho. Can also be transactivated by cleaved F2R/PAR1. Involved in modulation of inflammatory responses and regulation of innate and adaptive immunity, and acts as a sensor for proteolytic enzymes generated during infection. Generally is promoting inflammation. Can signal synergistically with TLR4 and probably TLR2 in inflammatory responses and modulates TLR3 signaling. Has a protective role in establishing the endothelial barrier; the activity involves coagulation factor X. Regulates endothelial cell barrier integrity during neutrophil extravasation, probably following proteolytic cleavage by PRTN3. Proposed to have a bronchoprotective role in airway epithelium, but also shown to compromise the airway epithelial barrier by interrupting E-cadherin adhesion. Involved in the regulation of vascular tone; activation results in hypotension presumably mediated by vasodilation. Associates with a subset of G proteins alpha subunits such as GNAQ, GNA11, GNA14, GNA12 and GNA13, but probably not with G(o) alpha, G(i) subunit alpha-1 and G(i) subunit alpha-2. However, according to can signal through G(i) subunit alpha. Believed to be a class B receptor which internalizes as a complex with arrestin and traffic with it to endosomal vesicles, presumably as desensitized receptor, for extended periods of time. Mediates inhibition of TNF-alpha stimulated JNK phosphorylation via coupling to GNAQ and GNA11; the function involves dissociation of RIPK1 and TRADD from TNFR1. Mediates phosphorylation of nuclear factor NF-kappa-B RELA subunit at 'Ser-536'; the function involves IKBKB and is predominantly independent of G proteins. Involved in cellular migration. Involved in cytoskeletal rearrangement and chemotaxis through beta-arrestin-promoted scaffolds; the function is independent of GNAQ and GNA11 and involves promotion of cofilin dephosphorylation and actin filament severing. Induces redistribution of COPS5 from the plasma membrane to the cytosol and activation of the JNK cascade is mediated by COPS5. Involved in the recruitment of leukocytes to the sites of inflammation and is the major PAR receptor capable of modulating eosinophil function such as proinflammatory cytokine secretion, superoxide production and degranulation. During inflammation promotes dendritic cell maturation, trafficking to the lymph nodes and subsequent T-cell activation. Involved in antimicrobial response of innate immnune cells; activation enhances phagocytosis of Gram-positive and killing of Gram-negative bacteria. Acts synergistically with interferon-gamma in enhancing antiviral responses. Implicated in a number of acute and chronic inflammatory diseases such as of the joints, lungs, brain, gastrointestinal tract, periodontium, skin, and vascular systems, and in autoimmune disorders. Receptor for trypsin and trypsin-like enzymes coupled to G proteins.
PDBSTRUC
5NJ6; 5NDZ; 5NDD
BIOCLASS
GPCR rhodopsin
SEQUENCE
MRSPSAAWLLGAAILLAASLSCSGTIQGTNRSSKGRSLIGKVDGTSHVTGKGVTVETVFSVDEFSASVLTGKLTTVFLPIVYTIVFVVGLPSNGMALWVFLFRTKKKHPAVIYMANLALADLLSVIWFPLKIAYHIHGNNWIYGEALCNVLIGFFYGNMYCSILFMTCLSVQRYWVIVNPMGHSRKKANIAIGISLAIWLLILLVTIPLYVVKQTIFIPALNITTCHDVLPEQLLVGDMFNYFLSLAIGVFLFPAFLTASAYVLMIRMLRSSAMDENSEKKRKRAIKLIVTVLAMYLICFTPSNLLLVVHYFLIKSQGQSHVYALYIVALCLSTLNSCIDPFVYYFVSHDFRDHAKNALLCRSVRTVKQMQVSLTSKKHSRKSSSYSSSSTTVKTSY
DRUGINFO
Amidine compound 1
DRUGINFO
Amidine compound 2
DRUGINFO
Amidine compound 3
DRUGINFO
Amidine compound 4
DRUGINFO
Amidine compound 5
DRUGINFO
Amidine compound 6
DRUGINFO
Benzimidazole derivative 10
DRUGINFO
Benzimidazole derivative 8
DRUGINFO
Benzimidazole derivative 9
目标的 KEGG 通路数据
标题内容
hsa04080
hsa04750
hsa05143
目标的 Wiki 路径数据
标题内容
WP455
WP2664
WP1825
WP1824
目标的蛋白质ID
标题内容
TARGETID
UNIPROID
TARGNAME
TARGTYPE
目标的序列数据
标题内容
Proteinase activated receptor 2 (PAR2)
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