Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T78981
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| Former ID |
TTDS00435
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| Target Name |
Complement C5
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| Gene Name |
C5
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| Synonyms |
C3 and PZPlike alpha2macroglobulin domaincontaining protein 4; Complement C5 alpha' chain; C5
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| Target Type |
Clinical Trial
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| Disease | Autoimmune diabetes [ICD10: E08-E13] | ||||
| Cardiovascular disorder [ICD10: I00-I99] | |||||
| Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
| Glomerulonephritis [ICD9: 580-582; ICD10: N00, N01, N03, N18] | |||||
| Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
| Macular degeneration [ICD9: 362.5; ICD10: H35.3] | |||||
| Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
| Function |
Derived from proteolytic degradation of complement C5, C5 anaphylatoxin is a mediator of local inflammatory process. Binding to the receptor C5AR1 induces a variety of responses including intracellular calcium release, contraction of smooth muscle, increased vascular permeability, and histamine release from mast cells and basophilic leukocytes (PubMed:8182049). C5a is also a potent chemokine which stimulates the locomotion of polymorphonuclear leukocytes and directs their migration toward sites of inflammation.
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| BioChemical Class |
Complement system
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| Target Validation |
T78981
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| UniProt ID | |||||
| Sequence |
MGLLGILCFLIFLGKTWGQEQTYVISAPKIFRVGASENIVIQVYGYTEAFDATISIKSYP
DKKFSYSSGHVHLSSENKFQNSAILTIQPKQLPGGQNPVSYVYLEVVSKHFSKSKRMPIT YDNGFLFIHTDKPVYTPDQSVKVRVYSLNDDLKPAKRETVLTFIDPEGSEVDMVEEIDHI GIISFPDFKIPSNPRYGMWTIKAKYKEDFSTTGTAYFEVKEYVLPHFSVSIEPEYNFIGY KNFKNFEITIKARYFYNKVVTEADVYITFGIREDLKDDQKEMMQTAMQNTMLINGIAQVT FDSETAVKELSYYSLEDLNNKYLYIAVTVIESTGGFSEEAEIPGIKYVLSPYKLNLVATP LFLKPGIPYPIKVQVKDSLDQLVGGVPVTLNAQTIDVNQETSDLDPSKSVTRVDDGVASF VLNLPSGVTVLEFNVKTDAPDLPEENQAREGYRAIAYSSLSQSYLYIDWTDNHKALLVGE HLNIIVTPKSPYIDKITHYNYLILSKGKIIHFGTREKFSDASYQSINIPVTQNMVPSSRL LVYYIVTGEQTAELVSDSVWLNIEEKCGNQLQVHLSPDADAYSPGQTVSLNMATGMDSWV ALAAVDSAVYGVQRGAKKPLERVFQFLEKSDLGCGAGGGLNNANVFHLAGLTFLTNANAD DSQENDEPCKEILRPRRTLQKKIEEIAAKYKHSVVKKCCYDGACVNNDETCEQRAARISL GPRCIKAFTECCVVASQLRANISHKDMQLGRLHMKTLLPVSKPEIRSYFPESWLWEVHLV PRRKQLQFALPDSLTTWEIQGVGISNTGICVADTVKAKVFKDVFLEMNIPYSVVRGEQIQ LKGTVYNYRTSGMQFCVKMSAVEGICTSESPVIDHQGTKSSKCVRQKVEGSSSHLVTFTV LPLEIGLHNINFSLETWFGKEILVKTLRVVPEGVKRESYSGVTLDPRGIYGTISRRKEFP YRIPLDLVPKTEIKRILSVKGLLVGEILSAVLSQEGINILTHLPKGSAEAELMSVVPVFY VFHYLETGNHWNIFHSDPLIEKQKLKKKLKEGMLSIMSYRNADYSYSVWKGGSASTWLTA FALRVLGQVNKYVEQNQNSICNSLLWLVENYQLDNGSFKENSQYQPIKLQGTLPVEAREN SLYLTAFTVIGIRKAFDICPLVKIDTALIKADNFLLENTLPAQSTFTLAISAYALSLGDK THPQFRSIVSALKREALVKGNPPIYRFWKDNLQHKDSSVPNTGTARMVETTAYALLTSLN LKDINYVNPVIKWLSEEQRYGGGFYSTQDTINAIEGLTEYSLLVKQLRLSMDIDVSYKHK GALHNYKMTDKNFLGRPVEVLLNDDLIVSTGFGSGLATVHVTTVVHKTSTSEEVCSFYLK IDTQDIEASHYRGYGNSDYKRIVACASYKPSREESSSGSSHAVMDISLPTGISANEEDLK ALVEGVDQLFTDYQIKDGHVILQLNSIPSSDFLCVRFRIFELFEVGFLSPATFTVYEYHR PDKQCTMFYSTSNIKIQKVCEGAACKCVEADCGQMQEELDLTISAETRKQTACKPEIAYA YKVSITSITVENVFVKYKATLLDIYKTGEAVAEKDSEITFIKKVTCTNAELVKGRQYLIM GKEALQIKYNFSFRYIYPLDSLTWIEYWPRDTTCSSCQAFLANLDEFAEDIFLNGC |
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| Structure |
1CFA; 1KJS; 1XWE; 3CU7; 3HQA; 3HQB; 3KLS; 3KM9; 3PRX;3PVM; 4A5W; 4E0S; 4P39; 1CFA; 1KJS; 1XWE; 3CU7; 3HQA; 3HQB; 3KLS; 3KM9; 3PRX; 3PVM; 4A5W; 4E0S; 4P39
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| Drugs and Mode of Action | |||||
| Drug(s) | LFG-316 | Drug Info | Phase 2 | Macular degeneration | [1] |
| NNC-0151-0000-0000 | Drug Info | Phase 2 | Rheumatoid arthritis | [2] | |
| ARC-1905 | Drug Info | Phase 1 | Macular degeneration | [3] | |
| MEDI7814 | Drug Info | Phase 1 | Chronic obstructive pulmonary disease | [4] | |
| REV-576 | Drug Info | Phase 1 | Autoimmune diabetes | [5] | |
| SAND-5 | Drug Info | Preclinical | Glomerulonephritis | [6] | |
| Pexelizumab | Drug Info | Discontinued in Phase 3 | Cardiovascular disorder | [7] | |
| MP-435 | Drug Info | Discontinued in Phase 2 | Rheumatoid arthritis | [8] | |
| CGS-32359 | Drug Info | Terminated | Inflammatory disease | [9] | |
| Inhibitor | CGS-32359 | Drug Info | [10] | ||
| REV-576 | Drug Info | [11] | |||
| SAND-5 | Drug Info | [12] | |||
| Modulator | MEDI7814 | Drug Info | [13] | ||
| Antagonist | MP-435 | Drug Info | [14] | ||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Complement and coagulation cascades | ||||
| Prion diseases | |||||
| Pertussis | |||||
| Staphylococcus aureus infection | |||||
| Herpes simplex infection | |||||
| Systemic lupus erythematosus | |||||
| Reactome | Activation of C3 and C5 | ||||
| Peptide ligand-binding receptors | |||||
| G alpha (i) signalling events | |||||
| Regulation of Complement cascade | |||||
| WikiPathways | Complement Activation, Classical Pathway | ||||
| Human Complement System | |||||
| Spinal Cord Injury | |||||
| Allograft Rejection | |||||
| GPCR ligand binding | |||||
| GPCR downstream signaling | |||||
| Complement cascade | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT01527500) Intravitreal LFG316 in Patients With Age-related Macular Degeneration (AMD). U.S. National Institutes of Health. | ||||
| REF 2 | Complement-targeted therapeutics. Nat Biotechnol. 2007 Nov;25(11):1265-75. | ||||
| REF 3 | ClinicalTrials.gov (NCT00950638) A Study of ARC1905 (Anti-C5 Aptamer) in Subjects With Dry Age-related Macular Degeneration. U.S. National Institutes of Health. | ||||
| REF 4 | ClinicalTrials.gov (NCT01544361) A Phase 1 Study to Evaluate the Safety of MEDI7814 in Adult Volunteers. U.S. National Institutes of Health. | ||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800042907) | ||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032848) | ||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010238) | ||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027730) | ||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010131) | ||||
| REF 10 | Anticomplement therapy. Biologics. 2008 December; 2(4): 671-685. | ||||
| REF 11 | Complement C5-inhibitor rEV576 (coversin) ameliorates in-vivo effects of antiphospholipid antibodies. Lupus. 2014 Oct;23(12):1324-6. | ||||
| REF 12 | Progress and Trends in Complement Therapeutics. Adv Exp Med Biol. 2013; 734: 1-22. | ||||
| REF 13 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | ||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027730) | ||||
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