Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T14342 | Target Info | |||
Target Name | Human immunodeficiency virus Reverse transcriptase (HIV RT) | ||||
Synonyms |
HIV p66 RT; HIV Exoribonuclease H
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Target Type | Successful Target | ||||
Gene Name | HIV RT | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Platelet-activating factor receptor (PTAFR) | Successful Target | ||||
UniProt ID | PTAFR_HUMAN | |||||
Gene Name | PTAFR | |||||
Synonyms |
PTAFR; PAF-R
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Representative Drug(s) | Lexipafant | Drug Info | Ki = 0.38 nM | [1] | ||
Co-Target Name | Human immunodeficiency virus Protease (HIV PR) | Successful Target | ||||
UniProt ID | POL_HV1B1 | |||||
Gene Name | HIV PR | |||||
Synonyms |
HIV Retropepsin; HIV PR
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Representative Drug(s) | Zidovudine | Drug Info | IC50 = 6 nM | Click to Show More | [2] | |
2 | L-697,661 | Drug Info | IC50 = 36 nM | [4] | ||
3 | Nevirapine | Drug Info | IC50 = 101 nM | [4] | ||
4 | CALANOLIDE A | Drug Info | IC50 = 320 nM | [8] | ||
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 | [3] | ||
Co-Target Name | C-X-C chemokine receptor type 4 (CXCR4) | Successful Target | ||||
UniProt ID | CXCR4_HUMAN | |||||
Gene Name | CXCR4 | |||||
Synonyms |
Stromal cell-derived factor 1 receptor; SDF-1 receptor; NPYRL; Lipopolysaccharide-associated protein 3; Leukocyte-derived seven transmembrane domain receptor; LPS-associated protein 3; LESTR; LCR1; LAP-3; HM89; Fusin; FB22; Chemokine receptor CXCR4; CXCR-4; CXC-R4; CD184 antigen; CD184
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Representative Drug(s) | Drug Info | EC50 = 88 nM | [5] | |||
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 | S-mephenytoin 4-hydroxylase (CYP2C9) | Successful Target | ||||
UniProt ID | CP2C9_HUMAN | |||||
Gene Name | CYP2C9 | |||||
Synonyms |
Cytochrome P450 PB-1; Cytochrome P450 MP-8; Cytochrome P450 MP-4; Cytochrome P450 2C9; Cytochrome P-450MP; Cholesterol 25-hydroxylase; CYPIIC9; CYP2C10; (S)-limonene 7-monooxygenase; (S)-limonene 6-monooxygenase; (R)-limonene 6-monooxygenase
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Representative Drug(s) | Rilpivirine | Drug Info | IC50 = 346 nM | [9] | ||
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 | [10] | ||
Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
UniProt ID | KCNH2_HUMAN | |||||
Gene Name | KCNH2 | |||||
Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) | Rilpivirine | Drug Info | IC50 = 500 nM | [9] | ||
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 | [11] | ||
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 | [12] | ||
Co-Target Name | Human immunodeficiency virus Envelope glycoprotein gp160 (HIV env) | Clinical trial Target | ||||
UniProt ID | ENV_HV1H2 | |||||
Gene Name | HIV env | |||||
Synonyms |
Envelope glycoprotein gp160; Env polyprotein
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Representative Drug(s) | Efavirenz | Drug Info | IC50 = 3.5 nM | [13] | ||
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 | [14] | ||
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 | [15] | ||
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 | [16] | ||
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 | [17] | ||
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 | [18] | ||
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 | [19] | ||
Co-Target Name | Cytochrome P450 2C19 (CYP2C19) | Co-Target | ||||
UniProt ID | CP2CJ_HUMAN | |||||
Gene Name | CYP2C19 | |||||
Synonyms |
Fenbendazole monooxygenase (4'-hydroxylating); (R)-limonene 6-monooxygenase; (S)-limonene 6-monooxygenase; (S)-limonene 7-monooxygenase; CYPIIC17; CYPIIC19; Cytochrome P450-11A; Cytochrome P450-254C; Mephenytoin 4-hydroxylase
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Representative Drug(s) | Rilpivirine | Drug Info | IC50 = 335 nM | [9] | ||
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 | [20] |
References | Top | ||||
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REF 1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. J Med Chem. 1998 Jan 1;41(1):74-95. | ||||
REF 2 | Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. J Med Chem. 1995 Jun 9;38(12):2038-40. | ||||
REF 3 | 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 4 | 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. J Med Chem. 1993 Apr 30;36(9):1291-4. | ||||
REF 5 | Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1897-902. | ||||
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 | Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. J Med Chem. 1996 Mar 15;39(6):1303-13. | ||||
REF 9 | Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties. J Med Chem. 2020 May 14;63(9):4837-4848. | ||||
REF 10 | Nodulisporiviridins A-H, Bioactive Viridins from Nodulisporium sp. J Nat Prod. 2015 Jun 26;78(6):1221-30. | ||||
REF 11 | 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 12 | 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 13 | Soluble-type small-molecule CD4 mimics as HIV entry inhibitors. Bioorg Med Chem Lett. 2019 Mar 1;29(5):719-723. | ||||
REF 14 | Targeting DNA methylation with small molecules: what's next?. J Med Chem. 2015 Mar 26;58(6):2569-83. | ||||
REF 15 | 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 16 | Natural products targeting telomere maintenance. Medchemcomm. 2011;2:229-45. | ||||
REF 17 | 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 18 | 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 19 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. J Med Chem. 2018 Nov 21;61(22):9791-9810. | ||||
REF 20 | 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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