Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T68251 | Target Info | |||
Target Name | Matrix metalloproteinase-2 (MMP-2) | ||||
Synonyms |
TBE-1; Matrix metalloproteinase 2; CLG4A; 72 kDa type IV collagenase; 72 kDa gelatinase
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Target Type | Successful Target | ||||
Gene Name | MMP2 | ||||
Biochemical Class | Peptidase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Matrix metalloproteinase-1 (MMP-1) | Successful Target | ||||
UniProt ID | MMP1_HUMAN | |||||
Gene Name | MMP1 | |||||
Synonyms |
Interstitial collagenase; Fibroblast collagenase; CLG
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Representative Drug(s) | Marimastat | Drug Info | Ki = 0.7 nM | Click to Show More | [1] | |
2 | Prinomastat | Drug Info | IC50 = 4.9 nM | [3] | ||
Co-Target Name | Matrix metalloproteinase-7 (MMP-7) | Successful Target | ||||
UniProt ID | MMP7_HUMAN | |||||
Gene Name | MMP7 | |||||
Synonyms |
Uterine metalloproteinase; Pump-1 protease; PUMP1; Matrin; Matrilysin; MPSL1
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Representative Drug(s) | Marimastat | Drug Info | IC50 = 4.1 nM | Click to Show More | [2] | |
2 | Prinomastat | Drug Info | IC50 = 54 nM | [5] | ||
Co-Target Name | Plasmodium Enoyl-ACP reductase (Malaria fabI) | Successful Target | ||||
UniProt ID | Q965D5_PLAFA | |||||
Gene Name | Malaria fabI | |||||
Synonyms |
fabI; NADH-dependent enoyl-ACP reductase; Enoyl-acyl-carrier protein reductase; Enoyl-acyl carrier reductase; Enoyl-acyl carrier protein reductase; Enoyl-ACP reductase FabI
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | Ki = 8 nM | [4] | ||
Co-Target Name | Multidrug resistance protein 1 (ABCB1) | Clinical trial Target | ||||
UniProt ID | MDR1_HUMAN | |||||
Gene Name | ABCB1 | |||||
Synonyms |
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 122.6 nM | [6] | ||
Co-Target Name | Apoptosis regulator Bcl-2 (BCL-2) | Successful Target | ||||
UniProt ID | BCL2_HUMAN | |||||
Gene Name | BCL2 | |||||
Synonyms |
Bcl-2
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | Ki = 234.42 nM | [7] | ||
Co-Target Name | Amyloid beta A4 protein (APP) | Successful Target | ||||
UniProt ID | A4_HUMAN | |||||
Gene Name | APP | |||||
Synonyms |
Protease nexin-II; PreA4; PN-II; Cerebral vascular amyloid peptide; CVAP; Amyloid-beta precursor protein; Amyloid-beta A4 protein; Alzheimer disease amyloid protein; APPI; APP; AD1; ABPP; A4
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 500 nM | [8] | ||
Co-Target Name | Phosphogluconate dehydrogenase (PGD) | Successful Target | ||||
UniProt ID | 6PGD_HUMAN | |||||
Gene Name | PGD | |||||
Synonyms |
PGDH; 6PGDH; 6-phosphogluconate dehydrogenase, decarboxylating; 6-phosphogluconate dehydrogenase
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 720 nM | [9] | ||
Co-Target Name | Human immunodeficiency virus Reverse transcriptase (HIV RT) | Successful Target | ||||
UniProt ID | POL_HV1B1 | |||||
Gene Name | HIV RT | |||||
Synonyms |
HIV p66 RT; HIV Exoribonuclease H
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 730 nM | [10] | ||
Co-Target Name | Plasmodium Beta-hydroxyacyl-ACP dehydratase (Malaria FabZ) | Clinical trial Target | ||||
UniProt ID | Q965D7_PLAFA | |||||
Gene Name | Malaria FabZ | |||||
Synonyms |
fabZ; Fatty acid synthesis protein; Beta-hydroxyacyl-ACP dehydratase; 17 kDa actomyosin component; (3R)-hydroxymyristoyl-[acyl-carrier-protein] dehydratase; (3R)-hydroxymyristoyl-ACP dehydrase
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 0.03 ug.mL-1 | [11] | ||
Co-Target Name | Matrix metalloproteinase-13 (MMP-13) | Clinical trial Target | ||||
UniProt ID | MMP13_HUMAN | |||||
Gene Name | MMP13 | |||||
Synonyms |
Matrix metalloproteinase 13; Collagenase-3; Collagenase 3
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Representative Drug(s) | Prinomastat | Drug Info | Ki = 0.038 nM | Click to Show More | [12] | |
2 | Marimastat | Drug Info | IC50 = 1.2 nM | [2] | ||
Co-Target Name | Matrix metalloproteinase-9 (MMP-9) | Clinical trial Target | ||||
UniProt ID | MMP9_HUMAN | |||||
Gene Name | MMP9 | |||||
Synonyms |
Matrix metalloproteinase 9; GELB; CLG4B; 92 kDa type IV collagenase; 92 kDa gelatinase
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Representative Drug(s) | Prinomastat | Drug Info | IC50 = 0.048 nM | Click to Show More | [2] | |
2 | Marimastat | Drug Info | IC50 = 0.79 nM | [2] | ||
Co-Target Name | Matrix metalloproteinase-14 (MMP-14) | Clinical trial Target | ||||
UniProt ID | MMP14_HUMAN | |||||
Gene Name | MMP14 | |||||
Synonyms |
Membrane-type-1 matrix metalloproteinase; Membrane-type matrix metalloproteinase 1; MTMMP1; MT1MMP; MT1-MMP; MT-MMP 1; MMP-X1
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Representative Drug(s) | Prinomastat | Drug Info | IC50 = 0.3 nM | Click to Show More | [5] | |
2 | Marimastat | Drug Info | IC50 = 1.82 nM | [14] | ||
Co-Target Name | Plasmodium Oxoacyl-[acyl-carrier protein] reductase (Malaria fabG) | Clinical trial Target | ||||
UniProt ID | Q965D6_PLAFA | |||||
Gene Name | Malaria fabG | |||||
Synonyms |
3-oxoacyl-acyl-carrier protein reductase
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 0.32 ug.mL-1 | [11] | ||
Co-Target Name | Matrix metalloproteinase-8 (MMP-8) | Clinical trial Target | ||||
UniProt ID | MMP8_HUMAN | |||||
Gene Name | MMP8 | |||||
Synonyms |
PMNL-CL; PMNL collagenase; Neutrophil collagenase; CLG1
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Representative Drug(s) | Prinomastat | Drug Info | IC50 < 0.4 nM | Click to Show More | [3] | |
2 | Marimastat | Drug Info | IC50 = 0.47 nM | [2] | ||
Co-Target Name | TNF alpha converting enzyme (ADAM17) | Clinical trial Target | ||||
UniProt ID | ADA17_HUMAN | |||||
Gene Name | ADAM17 | |||||
Synonyms |
TNFalpha converting enzyme; TNF-alpha-converting enzyme; TNF-alpha converting enzyme; TNF-alpha convertase; TACE; Snake venom-like protease; Disintegrin and metalloproteinase domain-containing protein 17; CSVP; CD156b antigen; CD156b; ADAM 17; A disintegrin and metalloproteinase domain 17
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Representative Drug(s) | Marimastat | Drug Info | Ki = 0.4 nM | Click to Show More | [13] | |
2 | Prinomastat | Drug Info | IC50 = 5.5 nM | [15] | ||
Co-Target Name | DNA [cytosine-5]-methyltransferase 1 (DNMT1) | Clinical trial Target | ||||
UniProt ID | DNMT1_HUMAN | |||||
Gene Name | DNMT1 | |||||
Synonyms |
MCMT; M.HsaI; Dnmt1; DNMT; DNA methyltransferase HsaI; DNA MTase HsaI; DNA (cytosine5)methyltransferase 1; DNA (cytosine-5)-methyltransferase 1; CXXCtype zinc finger protein 9; CXXC9; CXXC-type zinc finger protein 9; AIM
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 500 nM | [16] | ||
Co-Target Name | Beta-secretase 1 (BACE1) | Clinical trial Target | ||||
UniProt ID | BACE1_HUMAN | |||||
Gene Name | BACE1 | |||||
Synonyms |
Membrane-associated aspartic protease 2; Memapsin-2; KIAA1149; Beta-site amyloid precursor protein cleaving enzyme 1; Beta-site APP cleaving enzyme 1; BACE; Aspartyl protease 2; Asp 2; ASP2
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 757 nM | [17] | ||
Co-Target Name | Telomerase reverse transcriptase (TERT) | Clinical trial Target | ||||
UniProt ID | TERT_HUMAN | |||||
Gene Name | TERT | |||||
Synonyms |
Telomerase-associated protein 2; Telomerase catalytic subunit; TRT; TP2; TCS1; HEST2; EST2
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 1000 nM | [18] | ||
Co-Target Name | Matrix metalloproteinase-3 (MMP-3) | Patented-recorded Target | ||||
UniProt ID | MMP3_HUMAN | |||||
Gene Name | MMP3 | |||||
Synonyms |
Transin-1; Stromelysin-1; STMY1; SL-1; MMP-3
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Representative Drug(s) | Prinomastat | Drug Info | IC50 = 0.23 nM | Click to Show More | [5] | |
2 | Marimastat | Drug Info | Ki = 2.4 nM | [19] | ||
Co-Target Name | Proteasome beta-5 (PS beta-5) | Patented-recorded Target | ||||
UniProt ID | PSB5_HUMAN | |||||
Gene Name | PSMB5 | |||||
Synonyms |
Proteasome subunit beta type-5; Proteasome subunit X; Proteasome subunit MB1; Proteasome epsilon chain; Proteasome chain 6; Multicatalytic endopeptidase complex epsilon chain; Macropain epsilon chain; MB1; LMPX
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 86 nM | [20] | ||
Co-Target Name | Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A) | Patented-recorded Target | ||||
UniProt ID | DYR1A_HUMAN | |||||
Gene Name | DYRK1A | |||||
Synonyms |
hMNB; Protein kinase minibrain homolog; MNBH; MNB; HP86; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; Dual specificity YAK1-related kinase; DYRK
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 330 nM | [21] | ||
Co-Target Name | MAPK-activated protein kinase 5 (MAPKAPK5) | Discontinued Target | ||||
UniProt ID | MAPK5_HUMAN | |||||
Gene Name | MAPKAPK5 | |||||
Synonyms |
p38regulated/activated protein kinase; p38-regulated/activated protein kinase; PRAK; MK5; MK-5; MAPKactivated protein kinase 5; MAPKAPK-5; MAPKAP-K5; MAPKAP kinase 5; MAP kinaseactivated protein kinase 5; MAP kinase-activated protein kinase 5
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 1000 nM | [22] | ||
Co-Target Name | Phosphoglycerate mutase 1 (PGAM1) | Co-Target | ||||
UniProt ID | PGAM1_HUMAN | |||||
Gene Name | PGAM1 | |||||
Synonyms |
BPG-dependent PGAM 1; Phosphoglycerate mutase isozyme B; PGAM-B
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Representative Drug(s) | Epigallocatechin gallate | Drug Info | IC50 = 490 nM | [23] |
References | Top | ||||
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REF 1 | Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme. J Med Chem. 2002 May 23;45(11):2289-93. | ||||
REF 2 | Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors. J Med Chem. 2002 Jan 3;45(1):219-32. | ||||
REF 3 | Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors. J Med Chem. 1999 Nov 4;42(22):4547-62. | ||||
REF 4 | Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR). J Med Chem. 2007 Feb 22;50(4):765-75. | ||||
REF 5 | 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 6 | Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives. J Med Chem. 2015 Jun 11;58(11):4529-49. | ||||
REF 7 | Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. | ||||
REF 8 | Nodulisporiviridins A-H, Bioactive Viridins from Nodulisporium sp. J Nat Prod. 2015 Jun 26;78(6):1221-30. | ||||
REF 9 | Catechin gallates are NADP+-competitive inhibitors of glucose-6-phosphate dehydrogenase and other enzymes that employ NADP+ as a coenzyme. Bioorg Med Chem. 2008 Apr 1;16(7):3580-6. | ||||
REF 10 | Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2763-7. | ||||
REF 11 | 2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections. Bioorg Med Chem. 2010 Nov 1;18(21):7475-85. | ||||
REF 12 | Protease inhibitors: current status and future prospects. J Med Chem. 2000 Feb 10;43(3):305-41. | ||||
REF 13 | Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors. Bioorg Med Chem Lett. 2003 Aug 18;13(16):2741-4. | ||||
REF 14 | Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket. J Med Chem. 1998 Apr 9;41(8):1209-17. | ||||
REF 15 | New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. J Med Chem. 1999 Nov 18;42(23):4890-908. | ||||
REF 16 | Targeting DNA methylation with small molecules: what's next?. J Med Chem. 2015 Mar 26;58(6):2569-83. | ||||
REF 17 | The green tea polyphenol (2)-epigallocatechin-3-gallate (EGCG) is not a beta-secretase inhibitor. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1408-14. | ||||
REF 18 | Natural products targeting telomere maintenance. Medchemcomm. 2011;2:229-45. | ||||
REF 19 | 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 20 | Another look at phenolic compounds in cancer therapy the effect of polyphenols on ubiquitin-proteasome system. Eur J Med Chem. 2019 Apr 1;167:291-311. | ||||
REF 21 | Development of DANDYs, new 3,5-diaryl-7-azaindoles demonstrating potent DYRK1A kinase inhibitory activity. J Med Chem. 2013 Dec 12;56(23):9569-85. | ||||
REF 22 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. J Med Chem. 2018 Nov 21;61(22):9791-9810. | ||||
REF 23 | Xanthone derivatives as phosphoglycerate mutase 1 inhibitors: Design, synthesis, and biological evaluation. Bioorg Med Chem. 2018 May 1;26(8):1961-1970. |
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