Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T40332 Target Info
Target Name Neutrophil elastase (NE)
Synonyms
PMN elastase; Medullasin; Human leukocyte elastase; HLE; Elastase-2; ELA2; Bone marrow serine protease
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Target Type Clinical trial Target
Gene Name ELANE
Biochemical Class Peptidase
UniProt ID
ELNE_HUMAN
Co-Targets of This Target  Top
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 [1]
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 [2]
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 [3]
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 [4]
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 [5]
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 [6]
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 [7]
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 [7]
Co-Target Name Leukocyte proteinase-3 (PRTN3) Clinical trial Target
UniProt ID PRTN3_HUMAN
Gene Name PRTN3
Synonyms
Wegener autoantigen; PR3; PR-3; P29; Neutrophil proteinase 4; NP4; NP-4; Myeloblastin; MBN; Leukocyte proteinase 3; CANCA antigen; C-ANCA antigen; AGP7
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Representative Drug(s) Sivelestat Drug Info IC50 = 340 nM [8]
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 [9]
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 [10]
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 [11]
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 [12]
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 [13]
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 [14]
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 [15]
References  Top
REF 1 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 2 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 3 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 4 Nodulisporiviridins A-H, Bioactive Viridins from Nodulisporium sp. J Nat Prod. 2015 Jun 26;78(6):1221-30.
REF 5 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 6 Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2763-7.
REF 7 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 8 Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3. Bioorg Med Chem. 2015 Mar 1;23(5):1123-34.
REF 9 Targeting DNA methylation with small molecules: what's next?. J Med Chem. 2015 Mar 26;58(6):2569-83.
REF 10 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 11 Natural products targeting telomere maintenance. Medchemcomm. 2011;2:229-45.
REF 12 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 13 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 14 Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. J Med Chem. 2018 Nov 21;61(22):9791-9810.
REF 15 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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