Target General Infomation
Target ID
T08856
Former ID
TTDR01266
Target Name
Neutrophil collagenase
Gene Name
MMP8
Synonyms
MMP-8; Matrix metalloproteinase-8; PMNL collagenase; PMNL-CL; MMP8
Target Type
Clinical Trial
Disease Multiple scierosis [ICD9: 340; ICD10: G35]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Function
Can degrade fibrillar type I, II, and III collagens.
BioChemical Class
Peptidase
Target Validation
T08856
UniProt ID
EC Number
EC 3.4.24.34
Sequence
MFSLKTLPFLLLLHVQISKAFPVSSKEKNTKTVQDYLEKFYQLPSNQYQSTRKNGTNVIV
EKLKEMQRFFGLNVTGKPNEETLDMMKKPRCGVPDSGGFMLTPGNPKWERTNLTYRIRNY
TPQLSEAEVERAIKDAFELWSVASPLIFTRISQGEADINIAFYQRDHGDNSPFDGPNGIL
AHAFQPGQGIGGDAHFDAEETWTNTSANYNLFLVAAHEFGHSLGLAHSSDPGALMYPNYA
FRETSNYSLPQDDIDGIQAIYGLSSNPIQPTGPSTPKPCDPSLTFDAITTLRGEILFFKD
RYFWRRHPQLQRVEMNFISLFWPSLPTGIQAAYEDFDRDLIFLFKGNQYWALSGYDILQG
YPKDISNYGFPSSVQAIDAAVFYRSKTYFFVNDQFWRYDNQRQFMEPGYPKSISGAFPGI
ESKVDAVFQQEHFFHVFSGPRYYAFDLIAQRVTRVARGNKWLNCRYG
Drugs and Mode of Action
Drug(s) CIPEMASTAT Drug Info Phase 3 Rheumatoid arthritis [532656], [541601]
ILOMASTAT Drug Info Preclinical Discovery agent [542432], [544872]
BB-1101 Drug Info Terminated Multiple scierosis [546101]
SC-44463 Drug Info Terminated Discovery agent [546364]
Inhibitor 1-Hydroxyamine-2-Isobutylmalonic Acid Drug Info [551393]
2-(biphenyl-4-ylsulfonamido)pentanedioic acid Drug Info [529392]
2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Drug Info [530402]
2-HYDROXYCARBAMOYL-4-METHYL-PENTANOIC ACID Drug Info [551374]
2-Thiomethyl-3-Phenylpropanoic Acid Drug Info [551393]
3-(4-Methoxy-benzenesulfonyl)-cyclohexanethiol Drug Info [525535]
3-(4-Methoxy-benzenesulfonyl)-propane-1-thiol Drug Info [525535]
3-(4-Phenoxy-benzenesulfonyl)-cyclohexanethiol Drug Info [525535]
3-(4-Phenoxy-benzenesulfonyl)-propane-1-thiol Drug Info [525535]
3-AMINO-AZACYCLOTRIDECAN-2-ONE Drug Info [551374]
4-amino-3-(4-(hexyloxy)phenyl)-4-oxobutanoic acid Drug Info [529392]
BB-1101 Drug Info [525644]
Glycinamid Drug Info [551393]
IK-682 Drug Info [526446]
ILOMASTAT Drug Info [551294]
METHYLAMINO-PHENYLALANYL-LEUCYL-HYDROXAMIC ACID Drug Info [551374]
MMI270 Drug Info [525642]
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide Drug Info [530402]
Ro-37-9790 Drug Info [551326]
SC-44463 Drug Info [526154]
SL422 Drug Info [526113]
[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid Drug Info [530402]
Modulator CIPEMASTAT Drug Info [532656]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
PANTHER Pathway Alzheimer disease-presenilin pathway
Reactome Collagen degradation
Degradation of the extracellular matrix
Activation of Matrix Metalloproteinases
WikiPathways Activation of Matrix Metalloproteinases
Matrix Metalloproteinases
References
Ref 532656Matrix metalloproteinase inhibition lowers mortality and brain injury in experimental pneumococcal meningitis. Infect Immun. 2014 Apr;82(4):1710-8.
Ref 541601(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: 6466).
Ref 542432(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: 7409).
Ref 544872Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001387)
Ref 546101Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006361)
Ref 546364Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007717)
Ref 525535Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors.
Ref 525642J Med Chem. 1999 Nov 4;42(22):4547-62.Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.
Ref 525644J Med Chem. 1999 Nov 18;42(23):4890-908.New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
Ref 526113Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo. J Med Chem. 2001 Aug 2;44(16):2636-60.
Ref 526154J Med Chem. 2001 Oct 11;44(21):3347-50.Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.
Ref 526446J Med Chem. 2002 Nov 7;45(23):4954-7.Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Ref 529392Bioorg Med Chem. 2009 Feb 1;17(3):1101-8. Epub 2008 Mar 8.Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.
Ref 530402J Med Chem. 2009 Oct 22;52(20):6347-61.Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
Ref 532656Matrix metalloproteinase inhibition lowers mortality and brain injury in experimental pneumococcal meningitis. Infect Immun. 2014 Apr;82(4):1710-8.
Ref 551294Hydroxamate inhibitors of human gelatinase B (92 kDa), Bioorg. Med. Chem. Lett. 5(4):349-352 (1995).
Ref 55132611,21-Bisphenyl-19-norpregnane derivatives are selective antiglucocorticoids, Bioorg. Med. Chem. Lett. 7(17):2299-2302 (1997).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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