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Colitis

Disease ID:232
Name:Colitis
Associated with:3 targets
1 immuno-relevant target
5 immuno-relevant ligands

Targets

5-HT1A receptor
Comments:  Serotonin acting via 5-HT1A receptors plays a key role in the pathogenesis of experimental colitis
NK1 receptor
Role:  Colonic inflammation, colonic fibrosis, colitis induced transformation
References:  1-2,4,6-8
NLRP6

Ligands

Key to terms and symbols Click ligand name to view ligand summary Click column headers to sort
Ligand References Clinical and Disease comments
triamcinolone
Immuno Disease Comments: Glucocorticoid drug used to treat many inflammatory condtions including colitis.
Clinical Use: Triamcinolone is used for its antiinflammatory or immunosuppressive actions in many conditions. For example, oral triamcinolone is used to treat conditions such as allergic disorders, skin conditions, ulcerative colitis, arthritis, lupus, psoriasis, and breathing disorders. This drug is also used topically as an anti-inflammatory and anti-pruritic agent. Injectable forms of the drug may be used to reduce intra-articular joint pain, stiffness and swelling associated with rheumatoid and osteoarthritic arthritis, bursitis, epicondylitis, and tenosynovitis. | View clinical data
methylprednisolone
Immuno Disease Comments: A corticosteroid used to treat colitis.
Clinical Use: Methylprednisolone is used to treat numerous inflammatory conditions including arthritis, lupus, psoriasis, ulcerative colitis and allergic disorders. The drug is also used to treat glucocorticoid-responsive conditions of the skin, eyes, lungs, stomach, nervous system and blood cells, and some endocrine conditions. | View clinical data
bihelical apoA-I mimetic peptide 5A
Immuno Disease Comments: Experimental compound with predicted application in colitis.
Bioactivity Comments: In vitro, the 5A peptide was able to solubilize phospholipid vesicles and stimulated cholesterol and phospholipid efflux by the ABCA1 transporter with high specificity but no affinity data has yet been reported [9]. | View biological activity
compound 24 [PMID: 26987013 ]
Immuno Disease Comments: Experimental compound with predicted application in inflammatory bowel disease.
Bioactivity Comments: In vivo, compound 24 dose-dependently reduced the disease activity index in a mouse model of inflammatory bowel disease (the acute dextran sulfate sodium (DSS)-induced colitis model) [5]. | View biological activity
PRN694
Immuno Disease Comments: Probe compound for experimental use.
Bioactivity Comments: In a kinase screening panel of 250 kinases ITK, TXK, BTK and BMX (all TEC family), and CLK2, CLK4, BLK, JAK3 and YES were the only enzymes inhibited by more than 90% at 1 μm PRN694 [10]. | View biological activity

References

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1. Dai L, Perera DS, King DW, Southwell BR, Burcher E, Liu L. (2012) Hemokinin-1 stimulates prostaglandin E₂ production in human colon through activation of cyclooxygenase-2 and inhibition of 15-hydroxyprostaglandin dehydrogenase. J. Pharmacol. Exp. Ther., 340 (1): 27-36. [PMID:21957267]

2. Engel MA, Becker C, Reeh PW, Neurath MF. (2011) Role of sensory neurons in colitis: increasing evidence for a neuroimmune link in the gut. Inflamm. Bowel Dis., 17 (4): 1030-3. [PMID:20722067]

3. Ghia JE, Li N, Wang H, Collins M, Deng Y, El-Sharkawy RT, Côté F, Mallet J, Khan WI. (2009) Serotonin has a key role in pathogenesis of experimental colitis. Gastroenterology, 137 (5): 1649-60. [PMID:19706294]

4. Gillespie E, Leeman SE, Watts LA, Coukos JA, O'Brien MJ, Cerda SR, Farraye FA, Stucchi AF, Becker JM. (2011) Truncated neurokinin-1 receptor is increased in colonic epithelial cells from patients with colitis-associated cancer. Proc. Natl. Acad. Sci. U.S.A., 108 (42): 17420-5. [PMID:21969570]

5. Kalindjian SB, Kadnur SV, Hewson CA, Venkateshappa C, Juluri S, Kristam R, Kulkarni B, Mohammed Z, Saxena R, Viswanadhan VN et al.. (2016) A New Series of Orally Bioavailable Chemokine Receptor 9 (CCR9) Antagonists; Possible Agents for the Treatment of Inflammatory Bowel Disease. J. Med. Chem., 59 (7): 3098-111. [PMID:26987013]

6. Koon HW, Shih D, Karagiannides I, Zhao D, Fazelbhoy Z, Hing T, Xu H, Lu B, Gerard N, Pothoulakis C. (2010) Substance P modulates colitis-associated fibrosis. Am. J. Pathol., 177 (5): 2300-9. [PMID:20889569]

7. Liu L, Markus I, Saghire HE, Perera DS, King DW, Burcher E. (2011) Distinct differences in tachykinin gene expression in ulcerative colitis, Crohn's disease and diverticular disease: a role for hemokinin-1?. Neurogastroenterol. Motil., 23 (5): 475-83, e179-80. [PMID:21342363]

8. Pagán B, Isidro AA, Coppola D, Chen Z, Ren Y, Wu J, Appleyard CB. (2010) Effect of a neurokinin-1 receptor antagonist in a rat model of colitis-associated colon cancer. Anticancer Res., 30 (9): 3345-53. [PMID:20944107]

9. Tabet F, Remaley AT, Segaliny AI, Millet J, Yan L, Nakhla S, Barter PJ, Rye KA, Lambert G. (2010) The 5A apolipoprotein A-I mimetic peptide displays antiinflammatory and antioxidant properties in vivo and in vitro. Arterioscler. Thromb. Vasc. Biol., 30 (2): 246-52. [PMID:19965776]

10. Zhong Y, Dong S, Strattan E, Ren L, Butchar JP, Thornton K, Mishra A, Porcu P, Bradshaw JM, Bisconte A et al.. (2015) Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694. J. Biol. Chem., 290 (10): 5960-78. [PMID:25593320]