Target Information
Target General Infomation | |||||
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Target ID |
T86702
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Former ID |
TTDC00105
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Target Name |
Stromelysin-1
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Gene Name |
MMP3
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Synonyms |
MMP-3; Matrix metalloproteinase 3; Matrix metalloproteinase-3; SL-1; Transin-1; MMP3
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Target Type |
Research
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Disease | Corneal ulcers [ICD9: 370; ICD10: H16.0] | ||||
HCV infection [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2] | |||||
Ischemic stroke [ICD9: 434.91; ICD10: I61-I63] | |||||
Multiple scierosis [ICD9: 340; ICD10: G35] | |||||
Osteoarthritis; Myocardial infarction [ICD9: 410, 715; ICD10: I21, I22, M15-M19, M47] | |||||
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
Function |
Can degrade fibronectin, laminin, gelatins of type I, III, IV, and V; collagens III, IV, X, and IX, and cartilage proteoglycans. Activates procollagenase.
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BioChemical Class |
Peptidase
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Target Validation |
T86702
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UniProt ID | |||||
EC Number |
EC 3.4.24.17
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Sequence |
MKSLPILLLLCVAVCSAYPLDGAARGEDTSMNLVQKYLENYYDLKKDVKQFVRRKDSGPV
VKKIREMQKFLGLEVTGKLDSDTLEVMRKPRCGVPDVGHFRTFPGIPKWRKTHLTYRIVN YTPDLPKDAVDSAVEKALKVWEEVTPLTFSRLYEGEADIMISFAVREHGDFYPFDGPGNV LAHAYAPGPGINGDAHFDDDEQWTKDTTGTNLFLVAAHEIGHSLGLFHSANTEALMYPLY HSLTDLTRFRLSQDDINGIQSLYGPPPDSPETPLVPTEPVPPEPGTPANCDPALSFDAVS TLRGEILIFKDRHFWRKSLRKLEPELHLISSFWPSLPSGVDAAYEVTSKDLVFIFKGNQF WAIRGNEVRAGYPRGIHTLGFPPTVRKIDAAISDKEKNKTYFFVEDKYWRFDEKRNSMEP GFPKQIAEDFPGIDSKIDAVFEEFGFFYFFTGSSQLEFDPNAKKVTHTLKSNSWLNC |
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Drugs and Mode of Action | |||||
Drug(s) | ILOMASTAT | Drug Info | Preclinical | Discovery agent | [542432], [544872] |
Batimastat | Drug Info | Discontinued in Phase 3 | Ischemic stroke | [468208], [545311] | |
Galardin | Drug Info | Discontinued in Phase 2 | Corneal ulcers | [544872] | |
PG-530742 | Drug Info | Discontinued in Phase 2 | Osteoarthritis; Myocardial infarction | [536172] | |
RS-130830 | Drug Info | Discontinued in Phase 2 | HCV infection | [546851] | |
BB-1101 | Drug Info | Terminated | Multiple scierosis | [546101] | |
L-696418 | Drug Info | Terminated | Discovery agent | [546087] | |
RO-319790 | Drug Info | Terminated | Rheumatoid arthritis | [545173] | |
SC-44463 | Drug Info | Terminated | Discovery agent | [546364] | |
Inhibitor | 1-Methyloxy-4-Sulfone-Benzene | Drug Info | [551393] | ||
3-Methylpyridine | Drug Info | [551393] | |||
5-Biphenyl-4-yl-5-ethyl-pyrimidine-2,4,6-trione | Drug Info | [526040] | |||
8-chloro-quinoline-3-carbonitrile | Drug Info | [529035] | |||
AM-2S | Drug Info | [529997] | |||
BB-1101 | Drug Info | [534793] | |||
CM-352 | Drug Info | [533140] | |||
FUTOENONE | Drug Info | [551279] | |||
Galardin | Drug Info | [528485], [529239] | |||
Hydroxyaminovaline | Drug Info | [551393] | |||
IK-682 | Drug Info | [526446] | |||
ILOMASTAT | Drug Info | [529683] | |||
L-696418 | Drug Info | [551297] | |||
MMI270 | Drug Info | [535550] | |||
PD-169469 | Drug Info | [527998] | |||
PG-530742 | Drug Info | [528049], [536172] | |||
PKF-242-484 | Drug Info | [528065] | |||
PNU-107859 | Drug Info | [527091] | |||
PNU-142372 | Drug Info | [526419] | |||
RO-319790 | Drug Info | [534791] | |||
Ro-37-9790 | Drug Info | [551326] | |||
RS-130830 | Drug Info | [527412] | |||
RS-39066 | Drug Info | [551301] | |||
SC-44463 | Drug Info | [551328] | |||
UK-356618 | Drug Info | [526680] | |||
Modulator | Batimastat | Drug Info | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | TNF signaling pathway | ||||
Transcriptional misregulation in cancer | |||||
Rheumatoid arthritis | |||||
NetPath Pathway | IL1 Signaling Pathway | ||||
IL4 Signaling Pathway | |||||
PANTHER Pathway | Plasminogen activating cascade | ||||
CCKR signaling map ST | |||||
Pathway Interaction Database | Posttranslational regulation of adherens junction stability and dissassembly | ||||
p75(NTR)-mediated signaling | |||||
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling | |||||
Reactome | Collagen degradation | ||||
Degradation of the extracellular matrix | |||||
Activation of Matrix Metalloproteinases | |||||
Assembly of collagen fibrils and other multimeric structures | |||||
EGFR Transactivation by Gastrin | |||||
WikiPathways | Activation of Matrix Metalloproteinases | ||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Oncostatin M Signaling Pathway | |||||
Matrix Metalloproteinases | |||||
References | |||||
Ref 468208 | (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: 5145). | ||||
Ref 536172 | Selective matrix metalloproteinase inhibition attenuates progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Am J Physiol Heart Circ Physiol. 2006 Jun;290(6):H2522-7. Epub 2006 Jan 20. | ||||
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 545173 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002350) | ||||
Ref 545311 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002787) | ||||
Ref 546087 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006282) | ||||
Ref 546101 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006361) | ||||
Ref 526040 | Bioorg Med Chem Lett. 2001 Apr 23;11(8):969-72.Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors. | ||||
Ref 526419 | Bioorg Med Chem Lett. 2002 Oct 7;12(19):2667-72.Protease inhibitors: synthesis of matrix metalloproteinase and bacterial collagenase inhibitors incorporating 5-amino-2-mercapto-1,3,4-thiadiazole zincbinding functions. | ||||
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 526680 | J Med Chem. 2003 Jul 31;46(16):3514-25.A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. | ||||
Ref 527091 | J Med Chem. 2004 Jun 3;47(12):3065-74.A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics simulations. | ||||
Ref 527412 | Bioorg Med Chem Lett. 2005 Feb 15;15(4):1101-6.Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). | ||||
Ref 527998 | J Med Chem. 2006 Feb 9;49(3):923-31.Structural insight into the stereoselective inhibition of MMP-8 by enantiomeric sulfonamide phosphonates. | ||||
Ref 528049 | Tumour microenvironment - opinion: validating matrix metalloproteinases as drug targets and anti-targets for cancer therapy. Nat Rev Cancer. 2006 Mar;6(3):227-39. | ||||
Ref 528065 | Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6. Epub 2006 Mar 3.A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. | ||||
Ref 528485 | Blockade of tumor necrosis factor-alpha-converting enzyme improves experimental small intestinal damage by decreasing matrix metalloproteinase-3 production in rats. Scand J Gastroenterol. 2006 Nov;41(11):1320-9. | ||||
Ref 529035 | J Biol Chem. 2007 Nov 16;282(46):33295-304. Epub 2007 Sep 11.Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood. | ||||
Ref 529239 | Novel transcription-factor-like function of human matrix metalloproteinase 3 regulating the CTGF/CCN2 gene. Mol Cell Biol. 2008 Apr;28(7):2391-413. | ||||
Ref 529683 | Bioorg Med Chem. 2008 Sep 15;16(18):8745-59. Epub 2008 Jul 20.Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity. | ||||
Ref 529997 | Bioorg Med Chem Lett. 2009 Apr 1;19(7):1970-6. Epub 2009 Feb 14.Synthesis of hydroxypyrone- and hydroxythiopyrone-based matrix metalloproteinase inhibitors: developing a structure-activity relationship. | ||||
Ref 533140 | Discovery and safety profiling of a potent preclinical candidate, (4-[4-[[(3R)-3-(hydroxycarbamoyl)-8-azaspiro[4.5]decan-3-yl]sulfonyl]phenoxy]-N-methylbenzamide) (CM-352), for the prevention and treatment of hemorrhage. J Med Chem. 2015 Apr 9;58(7):2941-57. | ||||
Ref 534791 | Bioorg Med Chem Lett. 1998 May 19;8(10):1163-8.The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases. | ||||
Ref 534793 | Bioorg Med Chem Lett. 1998 Jun 16;8(12):1443-8.Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution. | ||||
Ref 535550 | Strategies for MMP inhibition in cancer: innovations for the post-trial era. Nat Rev Cancer. 2002 Sep;2(9):657-72. | ||||
Ref 536172 | Selective matrix metalloproteinase inhibition attenuates progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Am J Physiol Heart Circ Physiol. 2006 Jun;290(6):H2522-7. Epub 2006 Jan 20. | ||||
Ref 551279 | Inhibition of metalloproteinase by futoenone derivatives, Bioorg. Med. Chem. Lett. 5(15):1637-1642 (1995). | ||||
Ref 551297 | Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides containing extended alkyl residues At P1', Bioorg. Med. Chem. Lett. 5(6):539-542 (1995). | ||||
Ref 551301 | Design, synthesis, activity, and structure of a novel class of matrix metalloproteinase inhibitors containing a heterocyclic P2??P3?? Bioorg. Med. Chem. Lett. 6(13):1541-1542 (1996). | ||||
Ref 551326 | 11,21-Bisphenyl-19-norpregnane derivatives are selective antiglucocorticoids, Bioorg. Med. Chem. Lett. 7(17):2299-2302 (1997). |
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