Target Information
Target General Information | Top | |||||
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Target ID |
T85228
(Former ID: TTDI02253)
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Target Name |
CCR3 messenger RNA (CCR3 mRNA)
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Synonyms |
Eosinophil eotaxin receptor (mRNA); Chemokine receptor CCR3 (mRNA); CMKBR3 (mRNA); CKR3 (mRNA); CD193 (mRNA); CCR-3 (mRNA); CC-CKR-3 (mRNA); C-C chemokine receptor type 3 (mRNA); C-C CKR-3 (mRNA)
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Gene Name |
CCR3
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Target Type |
Clinical trial target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Asthma [ICD-11: CA23] | |||||
Function |
Binds to eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES and MIP-1 delta. Subsequently transduces a signal by increasing the intracellular calcium ions level. Alternative coreceptor with CD4 for HIV-1 infection. Receptor for a C-C type chemokine.
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BioChemical Class |
mRNA target
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UniProt ID | ||||||
Sequence |
MTTSLDTVETFGTTSYYDDVGLLCEKADTRALMAQFVPPLYSLVFTVGLLGNVVVVMILI
KYRRLRIMTNIYLLNLAISDLLFLVTLPFWIHYVRGHNWVFGHGMCKLLSGFYHTGLYSE IFFIILLTIDRYLAIVHAVFALRARTVTFGVITSIVTWGLAVLAALPEFIFYETEELFEE TLCSALYPEDTVYSWRHFHTLRMTIFCLVLPLLVMAICYTGIIKTLLRCPSKKKYKAIRL IFVIMAVFFIFWTPYNVAILLSSYQSILFGNDCERSKHLDLVMLVTEVIAYSHCCMNPVI YAFVGERFRKYLRHFFHRHLLMHLGRYIPFLPSEKLERTSSVSPSTAEPELSIVF Click to Show/Hide
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Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
1 | ASM8 | Drug Info | Phase 2 | Allergic asthma | [2] | |
Mode of Action | [+] 1 Modes of Action | + | ||||
Antagonist | [+] 5 Antagonist drugs | + | ||||
1 | banyu (I) | Drug Info | [3] | |||
2 | RO116-4875/608 | Drug Info | [4] | |||
3 | RO116-9132/238 | Drug Info | [4] | |||
4 | RO320-2947/001 | Drug Info | [4] | |||
5 | RO330-0802/001 | Drug Info | [4] |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
1 | IL3 Signaling Pathway | |||||
Panther Pathway | [+] 1 Panther Pathways | + | ||||
1 | Inflammation mediated by chemokine and cytokine signaling pathway |
References | Top | |||||
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REF 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 60). | |||||
REF 2 | ClinicalTrials.gov (NCT01380236) A Single Blind Study to Evaluate the Safety, Tolerability and Explore the Efficacy of 8.0 mg ASM8 Inhaled Daily for 14 Days in Severe Asthma. U.S. National Institutesof Health. | |||||
REF 3 | Identification of full, partial and inverse CC chemokine receptor 3 agonists using [35S]GTPgammaS binding. Eur J Pharmacol. 2002 Dec 5;456(1-3):1-10. | |||||
REF 4 | Responses of leukocytes to chemokines in whole blood and their antagonism by novel CC-chemokine receptor 3 antagonists. Am J Respir Crit Care Med. 2002 Jun 15;165(12):1602-9. |
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