| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T86702 | ||||
| Target Name | Matrix metalloproteinase-3 (MMP-3) | ||||
| Type of Target |
Patented-recorded |
||||
| Drug Potency against Target | BB-3644 | Drug Info | IC50 = 30 nM | [17] | |
| BMS 275291 | Drug Info | IC50 = 157 nM | [16] | ||
| PG-530742 | Drug Info | Complete Inhibition = 150 ng/mL | [14] | ||
| Prinomastat | Drug Info | IC50 = 0.27 nM | [17] | ||
| Tanomastat | Drug Info | Ki = 134 nM | [15] | ||
| 5-Biphenyl-4-yl-5-ethyl-pyrimidine-2,4,6-trione | Drug Info | IC50 = 9000 nM | [1] | ||
| 8-chloro-quinoline-3-carbonitrile | Drug Info | IC50 = 2300 nM | [9] | ||
| AM-2S | Drug Info | IC50 = 5600 nM | [11] | ||
| BB-1101 | Drug Info | IC50 = 12 nM | [13] | ||
| CIPEMASTAT | Drug Info | Ki = 56 nM | [8] | ||
| CIPEMASTAT | Drug Info | IC50 = 527 nM | |||
| FUTOENONE | Drug Info | IC50 < 1000 nM | |||
| GM6001 | Drug Info | IC50 = 26 nM | [10] | ||
| IK-862 | Drug Info | Ki = 141 nM | [2] | ||
| L-696418 | Drug Info | Ki = 470 nM | |||
| MMI270 | Drug Info | IC50 = 22 nM | [6] | ||
| PD-169469 | Drug Info | Ki = 4.4 nM | [7] | ||
| PKF-242-484 | Drug Info | Ki = 0.9 nM | [8] | ||
| PNU-107859 | Drug Info | Ki = 710 nM | [4] | ||
| RO-319790 | Drug Info | IC50 = 470 nM | [12] | ||
| Ro-37-9790 | Drug Info | IC50 = 160 nM | |||
| RS-130830 | Drug Info | Ki = 9.3 nM | [5] | ||
| RS-39066 | Drug Info | IC50 = 0.8 nM | |||
| SC-44463 | Drug Info | Ki < 10 nM | |||
| UK-356618 | Drug Info | IC50 = 5.9 nM | [3] | ||
| Action against Disease Model | Prinomastat | Drug Info | 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. | [18] | |
| References | |||||
| REF 1 | Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors. Bioorg Med Chem Lett. 2001 Apr 23;11(8):969-72. | ||||
| REF 2 | Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structu... J Med Chem. 2002 Nov 7;45(23):4954-7. | ||||
| REF 3 | A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J Med Chem. 2003 Jul 31;46(16):3514-25. | ||||
| REF 4 | A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics s... J Med Chem. 2004 Jun 3;47(12):3065-74. | ||||
| REF 5 | Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). Bioorg Med Chem Lett. 2005 Feb 15;15(4):1101-6. | ||||
| REF 6 | N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1321-6. | ||||
| REF 7 | Structural insight into the stereoselective inhibition of MMP-8 by enantiomeric sulfonamide phosphonates. J Med Chem. 2006 Feb 9;49(3):923-31. | ||||
| REF 8 | A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6. | ||||
| REF 9 | Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood. J Biol Chem. 2007 Nov 16;282(46):33295-304. | ||||
| REF 10 | Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with i... Bioorg Med Chem. 2008 Sep 15;16(18):8745-59. | ||||
| REF 11 | Synthesis of hydroxypyrone- and hydroxythiopyrone-based matrix metalloproteinase inhibitors: developing a structure-activity relationship. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1970-6. | ||||
| REF 12 | The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases. Bioorg Med Chem Lett. 1998 May 19;8(10):1163-8. | ||||
| REF 13 | Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution. Bioorg Med Chem Lett. 1998 Jun 16;8(12):1443-8. | ||||
| REF 14 | Selective matrix metalloproteinase inhibition attenuates progression of left ventricular dysfunction and remodeling in dogs with chronic heart fail... Am J Physiol Heart Circ Physiol. 2006 Jun;290(6):H2522-7. | ||||
| REF 15 | BAY 12-9566, a novel inhibitor of matrix metalloproteinases with antiangiogenic activity. Clin Cancer Res. 1999 Nov;5(11):3603-7. | ||||
| REF 16 | Inhibition 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 17 | Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322. | ||||
| REF 18 | Proteomic 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. | ||||
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