Target Validation Information
Target ID T86702
Target Name Stromelysin-1
Target Type
Research
Drug Potency against Target Tanomastat Drug Info Ki = 134 nM [552207]
L-696418 Drug Info Ki = 470 nM
PNU-107859 Drug Info Ki = 710 nM [527091]
RS-130830 Drug Info Ki = 9.3 nM [527412]
CIPEMASTAT Drug Info Ki = 56 nM [528065]
IK-682 Drug Info Ki = 141 nM [526446]
FUTOENONE Drug Info IC50 < 1000 nM
SC-44463 Drug Info Ki < 10 nM
BB-3644 Drug Info IC50 = 30 nM [552497]
Prinomastat Drug Info IC50 = 0.27 nM [552497]
Ro-37-9790 Drug Info IC50 = 160 nM
BB-1101 Drug Info IC50 = 12 nM [534793]
UK-356618 Drug Info IC50 = 5.9 nM [526680]
5-Biphenyl-4-yl-5-ethyl-pyrimidine-2,4,6-trione Drug Info IC50 = 9000 nM [526040]
BMS 275291 Drug Info IC50 = 157 nM [552278]
8-chloro-quinoline-3-carbonitrile Drug Info IC50 = 2300 nM [529035]
PD-169469 Drug Info Ki = 4.4 nM [527998]
ILOMASTAT Drug Info IC50 = 26 nM [529683]
PKF-242-484 Drug Info Ki = 0.9 nM [528065]
PG-530742 Drug Info Complete Inhibition = 150 ng/mL [536172]
CIPEMASTAT Drug Info IC50 = 527 nM
MMI270 Drug Info IC50 = 22 nM [527431]
RS-39066 Drug Info IC50 = 0.8 nM
AM-2S Drug Info IC50 = 5600 nM [529997]
RO-319790 Drug Info IC50 = 470 nM [534791]
Action against Disease Model Prinomastat Treatment of MT1-MMP-transfected MDA-MB-231 cells with AG3340 (Prinomastat) directly affected the processing a multitude of matrix metalloproteinase substrates, and indirectly altered the expression of an array of other proteins with diverse functions. In this h uMan breast cancer cell line, secreted substrates acc uMulated uncleaved in the conditioned medi uM and plasma membrane protein substrates were retained on the cell surface, due to reduced processing and shedding of these proteins (cell surface receptors, growth factors and bioactive molecules) to the medi uM in the presence of the matrix metalloproteinase inhibitor. [552679] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Decreased immune-complex-induced lung injury and neutrophil counts; Protection and reduced hepatocyte apoptosis and necrosis in TNF-induced hepatitis [552207]
References
Ref 552207BAY 12-9566, a novel inhibitor of matrix metalloproteinases with antiangiogenic activity. Clin Cancer Res. 1999 Nov;5(11):3603-7.
Ref 552679Proteomic validation of protease drug targets: pharmacoproteomics of matrix metalloproteinase inhibitor drugs using isotope-coded affinity tag labelling and tandem mass spectrometry. Curr Pharm Des. 2007;13(3):263-70.
Ref 527091J 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 527412Bioorg Med Chem Lett. 2005 Feb 15;15(4):1101-6.Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
Ref 528065Bioorg 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 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 552497Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322.
Ref 552497Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322.
Ref 534793Bioorg 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 526680J 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 526040Bioorg Med Chem Lett. 2001 Apr 23;11(8):969-72.Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors.
Ref 552278Inhibition of angiogenesis and metastasis in two murine models by the matrix metalloproteinase inhibitor, BMS-275291. Cancer Res. 2001 Dec 1;61(23):8480-5.
Ref 529035J 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 527998J Med Chem. 2006 Feb 9;49(3):923-31.Structural insight into the stereoselective inhibition of MMP-8 by enantiomeric sulfonamide phosphonates.
Ref 529683Bioorg 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 528065Bioorg 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 536172Selective 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 527431Bioorg Med Chem Lett. 2005 Mar 1;15(5):1321-6.N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.
Ref 529997Bioorg 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 534791Bioorg 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.

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