Target Information

Target General Infomation
Target ID
T78981
Former ID
TTDS00435
Target Name
Complement C5
Gene Name
C5
Synonyms
C3 and PZPlike alpha2macroglobulin domaincontaining protein 4; Complement C5 alpha' chain; C5
Target Type
Clinical Trial
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.
BioChemical Class
Complement system
Target Validation
T78981
UniProt ID
P01031
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
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
Drugs and Mode of Action
Drug(s) LFG-316 Drug Info Phase 2 Macular degeneration [523790]
NNC-0151-0000-0000 Drug Info Phase 2 Rheumatoid arthritis [529141]
ARC-1905 Drug Info Phase 1 Macular degeneration [522747]
MEDI7814 Drug Info Phase 1 Chronic obstructive pulmonary disease [523815]
REV-576 Drug Info Phase 1 Autoimmune diabetes [549591]
SAND-5 Drug Info Preclinical Glomerulonephritis [549143]
Pexelizumab Drug Info Discontinued in Phase 3 Cardiovascular disorder [546778]
MP-435 Drug Info Discontinued in Phase 2 Rheumatoid arthritis [548692]
CGS-32359 Drug Info Terminated Inflammatory disease [546756]
Inhibitor CGS-32359 Drug Info [544090]
REV-576 Drug Info [532962]
SAND-5 Drug Info [544286]
Modulator MEDI7814 Drug Info [1572591]
Antagonist MP-435 Drug Info [548693]
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 522747ClinicalTrials.gov (NCT00950638) A Study of ARC1905 (Anti-C5 Aptamer) in Subjects With Dry Age-related Macular Degeneration. U.S. National Institutes of Health.
Ref 523790ClinicalTrials.gov (NCT01527500) Intravitreal LFG316 in Patients With Age-related Macular Degeneration (AMD). U.S. National Institutes of Health.
Ref 523815ClinicalTrials.gov (NCT01544361) A Phase 1 Study to Evaluate the Safety of MEDI7814 in Adult Volunteers. U.S. National Institutes of Health.
Ref 529141Complement-targeted therapeutics. Nat Biotechnol. 2007 Nov;25(11):1265-75.
Ref 546756Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010131)
Ref 546778Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010238)
Ref 548692Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027730)
Ref 549143Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032848)
Ref 549591Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800042907)
Ref
Ref 522747ClinicalTrials.gov (NCT00950638) A Study of ARC1905 (Anti-C5 Aptamer) in Subjects With Dry Age-related Macular Degeneration. U.S. National Institutes of Health.
Ref 528331Pexelizumab reduces death and myocardial infarction in higher risk cardiac surgical patients. Ann Thorac Surg. 2006 Aug;82(2):486-92.
Ref 529141Complement-targeted therapeutics. Nat Biotechnol. 2007 Nov;25(11):1265-75.
Ref 532962Complement C5-inhibitor rEV576 (coversin) ameliorates in-vivo effects of antiphospholipid antibodies. Lupus. 2014 Oct;23(12):1324-6.
Ref 544090Anticomplement therapy. Biologics. 2008 December; 2(4): 671-685.
Ref 544286Progress and Trends in Complement Therapeutics. Adv Exp Med Biol. 2013; 734: 1-22.
Ref 544404Advances in the management of macular degeneration. F1000Prime Rep. 2014; 6: 29.
Ref 548693Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027730)
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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