Target Information
Target General Infomation | |||||
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Target ID |
T08856
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Former ID |
TTDR01266
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Target Name |
Neutrophil collagenase
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Gene Name |
MMP8
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Synonyms |
MMP-8; Matrix metalloproteinase-8; PMNL collagenase; PMNL-CL; MMP8
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Target Type |
Clinical Trial
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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.
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BioChemical Class |
Peptidase
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Target Validation |
T08856
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UniProt ID | |||||
EC Number |
EC 3.4.24.34
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Sequence |
MFSLKTLPFLLLLHVQISKAFPVSSKEKNTKTVQDYLEKFYQLPSNQYQSTRKNGTNVIV
EKLKEMQRFFGLNVTGKPNEETLDMMKKPRCGVPDSGGFMLTPGNPKWERTNLTYRIRNY TPQLSEAEVERAIKDAFELWSVASPLIFTRISQGEADINIAFYQRDHGDNSPFDGPNGIL AHAFQPGQGIGGDAHFDAEETWTNTSANYNLFLVAAHEFGHSLGLAHSSDPGALMYPNYA FRETSNYSLPQDDIDGIQAIYGLSSNPIQPTGPSTPKPCDPSLTFDAITTLRGEILFFKD RYFWRRHPQLQRVEMNFISLFWPSLPTGIQAAYEDFDRDLIFLFKGNQYWALSGYDILQG YPKDISNYGFPSSVQAIDAAVFYRSKTYFFVNDQFWRYDNQRQFMEPGYPKSISGAFPGI ESKVDAVFQQEHFFHVFSGPRYYAFDLIAQRVTRVARGNKWLNCRYG |
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Drugs and Mode of Action | |||||
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 | |||||
References | |||||
Ref 532656 | Matrix 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 544872 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001387) | ||||
Ref 525535 | Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. | ||||
Ref 525642 | J Med Chem. 1999 Nov 4;42(22):4547-62.Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors. | ||||
Ref 525644 | J Med Chem. 1999 Nov 18;42(23):4890-908.New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. | ||||
Ref 526113 | Design, 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 526154 | J 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 526446 | J 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 529392 | Bioorg 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 530402 | J 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 532656 | Matrix metalloproteinase inhibition lowers mortality and brain injury in experimental pneumococcal meningitis. Infect Immun. 2014 Apr;82(4):1710-8. | ||||
Ref 551294 | Hydroxamate inhibitors of human gelatinase B (92 kDa), Bioorg. Med. Chem. Lett. 5(4):349-352 (1995). |
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