Target Information
| Target General Information | Top | |||||
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| Target ID |
T57011
(Former ID: TTDC00192)
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| Target Name |
ICAM1 messenger RNA (ICAM1 mRNA)
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| Synonyms |
Major group rhinovirus receptor (mRNA); Intercellular adhesion molecule 1 (mRNA); ICAM-1 (mRNA); CD54 (mRNA)
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| Gene Name |
ICAM1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Infectious gastroenteritis/colitis [ICD-11: 1A40] | |||||
| Function |
During leukocyte trans-endothelial migration, ICAM1 engagement promotes the assembly of endothelial apical cups through ARHGEF26/SGEF and RHOG activation. ICAM proteins are ligands for the leukocyte adhesion protein LFA-1 (integrin alpha-L/beta-2).
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| BioChemical Class |
mRNA target
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| UniProt ID | ||||||
| Sequence |
MAPSSPRPALPALLVLLGALFPGPGNAQTSVSPSKVILPRGGSVLVTCSTSCDQPKLLGI
ETPLPKKELLLPGNNRKVYELSNVQEDSQPMCYSNCPDGQSTAKTFLTVYWTPERVELAP LPSWQPVGKNLTLRCQVEGGAPRANLTVVLLRGEKELKREPAVGEPAEVTTTVLVRRDHH GANFSCRTELDLRPQGLELFENTSAPYQLQTFVLPATPPQLVSPRVLEVDTQGTVVCSLD GLFPVSEAQVHLALGDQRLNPTVTYGNDSFSAKASVSVTAEDEGTQRLTCAVILGNQSQE TLQTVTIYSFPAPNVILTKPEVSEGTEVTVKCEAHPRAKVTLNGVPAQPLGPRAQLLLKA TPEDNGRSFSCSATLEVAGQLIHKNQTRELRVLYGPRLDERDCPGNWTWPENSQQTPMCQ AWGNPLPELKCLKDGTFPLPIGESVTVTRDLEGTYLCRARSTQGEVTRKVTVNVLSPRYE IVIITVVAAAVIMGTAGLSTYLYNRQRKIKKYRLQQAQKGTPMKPNTQATPP Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | ISIS 1570 | Drug Info | Approved | Lleum inflammation | [2] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | Alicaforsen | Drug Info | Phase 3 | Lleum inflammation | [3] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | INXC-ICAM1 | Drug Info | Terminated | Transplant rejection | [4] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 5 Inhibitor drugs | + | ||||
| 1 | A-286982 | Drug Info | [7] | |||
| 2 | Dehydropipernonaline | Drug Info | [8] | |||
| 3 | Pellitorin | Drug Info | [8] | |||
| 4 | PIPERNONALINE | Drug Info | [8] | |||
| 5 | PIPERROLEIN B | Drug Info | [8] | |||
| 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-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | US patent application no. 6,300,491, Oligonucleotide inhibition of cell adhesion. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 4 | ISIS 2302. INXC ICAM1, Oligo-TCS. Drugs R D. 1999 Jan;1(1):85-6. | |||||
| REF 5 | Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2009). | |||||
| REF 6 | Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011). | |||||
| REF 7 | Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5269-73. | |||||
| REF 8 | Alkamides from the fruits of Piper longum and Piper nigrum displaying potent cell adhesion inhibition. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4544-6. | |||||
| REF 9 | US patent application no. 5,789,573, Antisense inhibition of ICAM-1, E-selectin, and CMV IE1/IE2. | |||||
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