Drug General Information |
Drug ID |
D0H2PA
|
Former ID |
DNC003860
|
Drug Name |
PKF-242-484
|
Synonyms |
TNF-484
|
Drug Type |
Small molecular drug
|
Indication |
Discovery agent
|
Investigative |
[1]
|
Structure |
|
Download
2D MOL
3D MOL
|
Formula |
C19H29N3O6
|
Canonical SMILES |
CC(C)(C)C(C(=O)NC)NC(=O)C(C1=CC=C(C=C1)OC)C(CO)C(=O)NO
|
InChI |
1S/C19H29N3O6/c1-19(2,3)15(18(26)20-4)21-17(25)14(13(10-23)16(24)22-27)11-6-8-12(28-5)9-7-11/h6-9,13-15,23,27H,10H2,1-5H3,(H,20,26)(H,21,25)(H,22,24)/t13-,14+,15+/m0/s1
|
InChIKey |
IOLRUMINDIUCLJ-RRFJBIMHSA-N
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PubChem Compound ID |
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Target and Pathway |
Target(s) |
ADAM 17 |
Target Info |
Inhibitor |
[2]
|
Collagenase 3 |
Target Info |
Inhibitor |
[1]
|
Stromelysin-1 |
Target Info |
Inhibitor |
[1]
|
Tumor necrosis factor |
Target Info |
Inhibitor |
[3]
|
Interstitial collagenase |
Target Info |
Inhibitor |
[1]
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KEGG Pathway
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Notch signaling pathway
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Alzheimer's disease
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Epithelial cell signaling in Helicobacter pylori infectionhsa04668:TNF signaling pathway
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Transcriptional misregulation in cancer
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Rheumatoid arthritishsa04010:MAPK signaling pathway
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Cytokine-cytokine receptor interaction
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NF-kappa B signaling pathway
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Sphingolipid signaling pathway
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mTOR signaling pathway
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Apoptosis
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TGF-beta signaling pathway
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Osteoclast differentiation
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Antigen processing and presentation
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Toll-like receptor signaling pathway
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NOD-like receptor signaling pathway
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RIG-I-like receptor signaling pathway
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Hematopoietic cell lineage
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Natural killer cell mediated cytotoxicity
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T cell receptor signaling pathway
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Fc epsilon RI signaling pathway
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TNF signaling pathway
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Adipocytokine signaling pathway
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Type II diabetes mellitus
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Non-alcoholic fatty liver disease (NAFLD)
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Type I diabetes mellitus
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Amyotrophic lateral sclerosis (ALS)
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Pertussis
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Legionellosis
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Leishmaniasis
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Chagas disease (American trypanosomiasis)
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African trypanosomiasis
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Malaria
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Toxoplasmosis
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Amoebiasis
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Tuberculosis
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Hepatitis C
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Hepatitis B
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Influenza A
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HTLV-I infection
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Herpes simplex infection
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Proteoglycans in cancer
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Asthma
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Inflammatory bowel disease (IBD)
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Systemic lupus erythematosus
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Rheumatoid arthritis
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Allograft rejection
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Graft-versus-host disease
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Hypertrophic cardiomyopathy (HCM)
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Dilated cardiomyopathyhsa03320:PPAR signaling pathway
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Pathways in cancer
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Bladder cancer
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NetPath Pathway
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IL1 Signaling PathwayNetPath_13:IL1 Signaling Pathway
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IL4 Signaling PathwayNetPath_11:TCR Signaling Pathway
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IL2 Signaling Pathway
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IL3 Signaling Pathway
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IL4 Signaling Pathway
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Leptin Signaling Pathway
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RANKL Signaling Pathway
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EGFR1 Signaling Pathway
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TWEAK Signaling Pathway
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Wnt Signaling Pathway
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PANTHER Pathway
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Alzheimer disease-amyloid secretase pathway
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Alzheimer disease-presenilin pathway
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Notch signaling pathwayP00004:Alzheimer disease-presenilin pathway
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Plasminogen activating cascadeP00050:Plasminogen activating cascade
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CCKR signaling map STP00006:Apoptosis signaling pathway
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Wnt signaling pathwayP00004:Alzheimer disease-presenilin pathway
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Plasminogen activating cascade
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Pathway Interaction Database
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ErbB4 signaling events
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TNF receptor signaling pathway
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p75(NTR)-mediated signalingupa_upar_pathway:Urokinase-type plasminogen activator (uPA) and uPAR-mediated signalingajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly
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p75(NTR)-mediated signaling
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Urokinase-type plasminogen activator (uPA) and uPAR-mediated signalingil27pathway:IL27-mediated signaling events
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Canonical NF-kappaB pathway
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Calcineurin-regulated NFAT-dependent transcription in lymphocytes
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Angiopoietin receptor Tie2-mediated signaling
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Signaling events mediated by HDAC Class I
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Ceramide signaling pathway
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amb2 Integrin signaling
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RXR and RAR heterodimerization with other nuclear receptor
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IL23-mediated signaling events
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HIV-1 Nef: Negative effector of Fas and TNF-alpha
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Caspase Cascade in Apoptosis
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Cellular roles of Anthrax toxin
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Downstream signaling in naï
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Endothelins
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Validated transcriptional targets of AP1 family members Fra1 and Fra2
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Glucocorticoid receptor regulatory network
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AP-1 transcription factor network
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Syndecan-1-mediated signaling events
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PathWhiz Pathway
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Fc Epsilon Receptor I Signaling in Mast Cells
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Reactome
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Nuclear signaling by ERBB4
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Collagen degradation
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Regulated proteolysis of p75NTR
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Activated NOTCH1 Transmits Signal to the Nucleus
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Constitutive Signaling by NOTCH1 PEST Domain Mutants
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Constitutive Signaling by NOTCH1 t(7
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M1580_K2555) Translocation Mutant
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Constitutive Signaling by NOTCH1 HD Domain Mutants
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Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
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TNF signaling
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Growth hormone receptor signalingR-HSA-1442490:Collagen degradation
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Degradation of the extracellular matrix
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Activation of Matrix Metalloproteinases
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Assembly of collagen fibrils and other multimeric structuresR-HSA-1442490:Collagen degradation
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Assembly of collagen fibrils and other multimeric structures
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EGFR Transactivation by GastrinR-HSA-381340:Transcriptional regulation of white adipocyte differentiation
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TNFR1-induced proapoptotic signaling
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Regulation of TNFR1 signaling
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TNFR1-induced NFkappaB signaling pathway
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TNFR1-mediated ceramide production
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TNFR2 non-canonical NF-kB pathway
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TNF signalingR-HSA-1442490:Collagen degradation
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Basigin interactions
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Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
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WikiPathways
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Notch Signaling Pathway
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Copper homeostasis
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Notch Signaling Pathway
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Growth hormone receptor signaling
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BDNF signaling pathway
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Alzheimers Disease
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Signalling by NGF
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Extrinsic Pathway for ApoptosisWP474:Endochondral Ossification
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Activation of Matrix Metalloproteinases
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Oncostatin M Signaling Pathway
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AGE/RAGE pathway
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Matrix MetalloproteinasesWP2769:Activation of Matrix Metalloproteinases
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Gastrin-CREB signalling pathway via PKC and MAPK
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Matrix MetalloproteinasesWP75:Toll-like receptor signaling pathway
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Monoamine Transport
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SIDS Susceptibility Pathways
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TGF Beta Signaling Pathway
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Cytokines and Inflammatory Response
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MAPK Signaling Pathway
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EV release from cardiac cells and their functional effects
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FAS pathway and Stress induction of HSP regulation
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Apoptosis-related network due to altered Notch3 in ovarian cancer
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Cardiac Hypertrophic Response
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Transcriptional Regulation of White Adipocyte Differentiation
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Aryl Hydrocarbon Receptor
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Apoptosis
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Nanoparticle triggered regulated necrosis
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Amyotrophic lateral sclerosis (ALS)
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Adipogenesis
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Allograft Rejection
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TNF alpha Signaling Pathway
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TWEAK Signaling Pathway
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Extrinsic Pathway for Apoptosis
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Folate Metabolism
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MicroRNAs in cardiomyocyte hypertrophy
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Vitamin B12 Metabolism
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Selenium Micronutrient Network
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Regulation of toll-like receptor signaling pathway
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Matrix MetalloproteinasesWP366:TGF beta Signaling Pathway
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Bladder Cancer
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Degradation of collagen
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Quercetin and Nf-kB/ AP-1 Induced Cell Apoptosis
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Prostate Cancer
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Integrated Breast Cancer Pathway
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Integrated Cancer pathway
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Cell surface interactions at the vascular wall
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Matrix Metalloproteinases
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References |
REF 1 | 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. |
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REF 2 | Bioorg Med Chem. 2009 Jan 15;17(2):444-59. Epub 2008 Dec 3.Current perspective of TACE inhibitors: a review. |
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REF 3 | J Med Chem. 2002 May 23;45(11):2289-93.Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme. |