Target Information
| Target General Information | Top | |||||
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| Target ID |
T22658
(Former ID: TTDR00205)
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| Target Name |
Interleukin-8 (IL8)
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| Synonyms |
T-cell chemotactic factor; Protein 3-10C; Neutrophil-activating protein 1; NAP-1; Monocyte-derived neutrophil-activating peptide; Monocyte-derived neutrophil chemotactic factor; MONAP; MDNCF; IL8; IL-8; Granulocyte chemotactic protein 1; GCP-1; Emoctakin; Chemokine (C-X-C motif) ligand 8; C-X-C motif chemokine 8
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| Gene Name |
CXCL8
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Pain [ICD-11: MG30-MG3Z] | |||||
| Function |
IL-8 is a chemotactic factor that attracts neutrophils, basophils, and T-cells, but not monocytes. It is also involved in neutrophil activation. It is released from several cell types in response to an inflammatory stimulus. IL-8(6-77) has a 5-10-fold higher activity on neutrophil activation, IL-8(5-77) has increased activity on neutrophil activation and IL-8(7-77) has a higher affinity to receptors CXCR1 and CXCR2 as compared to IL-8(1-77), respectively.
Click to Show/Hide
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| BioChemical Class |
Cytokine: interleukin
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| UniProt ID | ||||||
| Sequence |
MTSKLAVALLAAFLISAALCEGAVLPRSAKELRCQCIKTYSKPFHPKFIKELRVIESGPH
CANTEIIVKLSDGRELCLDPKENWVQRVVEKFLKRAENS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A00975 ; BADD_A05823 ; BADD_A05962 | |||||
| HIT2.0 ID | T54CIF | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Ibuprofen | Drug Info | Approved | Pain | [2], [3] | |
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | ABX-IL8 | Drug Info | Phase 2 | Melanoma | [4] | |
| 2 | BMS-986253 | Drug Info | Phase 2 | Coronavirus Disease 2019 (COVID-19) | [5] | |
| 3 | MDX-018 | Drug Info | Phase 1 | Autoimmune diabetes | [6] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 8 Inhibitor drugs | + | ||||
| 1 | Ibuprofen | Drug Info | [1] | |||
| 2 | BMS-986253 | Drug Info | [8] | |||
| 3 | R-ketoprofen | Drug Info | [1] | |||
| 4 | 2-(2-(2,5-dichlorophenylamino)phenyl)acetic acid | Drug Info | [1] | |||
| 5 | 2-(2-(2-chlorophenoxy)phenyl)acetic acid | Drug Info | [1] | |||
| 6 | 2-(2-(2-chlorophenylamino)phenyl)acetic acid | Drug Info | [1] | |||
| 7 | 2-(2-(2-fluorophenoxy)phenyl)acetic acid | Drug Info | [1] | |||
| 8 | 2-(2-(2-fluorophenylamino)phenyl)acetic acid | Drug Info | [1] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | MDX-018 | Drug Info | [9] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| 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 | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| 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 | Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4026-30. | |||||
| REF 2 | 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. (Ligand id: 2713). | |||||
| REF 3 | New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. | |||||
| REF 4 | ClinicalTrials.gov (NCT00035828) A Blinded Study Comparing the Safety and Efficacy of a Fully Human Anti-IL8 Monoclonal Antibody (ABX-IL8) to Placebo in Patients With Chronic Bronchitis and COPD. U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT04347226) Anti-Interleukin-8 (Anti-IL-8) for Patients With COVID-19. U.S. National Institutes of Health. | |||||
| REF 6 | Clinical pipeline report, company report or official report of Genmab. | |||||
| REF 7 | Fully humanized neutralizing antibodies to interleukin-8 (ABX-IL8) inhibit angiogenesis, tumor growth, and metastasis of human melanoma. Am J Pathol. 2002 Jul;161(1):125-34. | |||||
| REF 8 | Phase I trial of HuMax-IL8 (BMS-986253), an anti-IL-8 monoclonal antibody, in patients with metastatic or unresectable solid tumors. J Immunother Cancer. 2019 Sep 5;7(1):240. | |||||
| REF 9 | Company report (Genmab) | |||||
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