Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T09826 Target Info
Target Name DNA topoisomerase I (TOP1)
Synonyms
DNA topoisomerase I
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Target Type Successful Target
Gene Name TOP1
Biochemical Class Topoisomerase
UniProt ID
TOP1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Prostaglandin G/H synthase 2 (COX-2) Successful Target
UniProt ID PGH2_HUMAN
Gene Name PTGS2
Synonyms
Prostaglandin-endoperoxide synthase 2; Prostaglandin H2 synthase 2; PHS II; PGHS-2; PGH synthase 2; Cyclooxygenase-2; COX2; COX-2
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Representative Drug(s) B-Lactams Drug Info IC50 = 2.5 ug.mL-1 [1]
Co-Target Name Influenza Neuraminidase (Influ NA) Successful Target
UniProt ID NRAM_I33A0
Gene Name Influ NA
Synonyms
STNA; NEU1; NANase; N-acylneuraminate glycohydrolase; Influ Sialidase
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Representative Drug(s) B-Lactams Drug Info IC50 = 9.65 ug.mL-1 [2]
Co-Target Name LCK tyrosine protein kinase (LCK) Successful Target
UniProt ID LCK_HUMAN
Gene Name LCK
Synonyms
p56-LCK; Tyrosine-protein kinase Lck; T cell-specific protein-tyrosine kinase; Proto-oncogene tyrosine-protein kinase LCK; Proto-oncogene Lck; Protein YT16; Lymphocyte cell-specific protein-tyrosine kinase; Leukocyte C-terminal Src kinase; LSK; LCK p59-Fyn; LCK Protooncogene Syn
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Representative Drug(s) B-Lactams Drug Info IC50 = 10 ug.mL-1 [3]
Co-Target Name Acetylcholinesterase (AChE) Successful Target
UniProt ID ACES_HUMAN
Gene Name ACHE
Synonyms
YT; N-ACHE; ARACHE
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Representative Drug(s) Irinotecan Drug Info Ki = 50.5 nM [4]
Co-Target Name Carbonic anhydrase XII (CA-XII) Successful Target
UniProt ID CAH12_HUMAN
Gene Name CA12
Synonyms
Tumor antigen HOM-RCC-3.1.3; Carbonic anhydrase 12; Carbonate dehydratase XII
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Representative Drug(s) B-Lactams Drug Info Ki = 60.3 nM [5]
Co-Target Name Indoleamine 2,3-dioxygenase 1 (IDO1) Successful Target
UniProt ID I23O1_HUMAN
Gene Name IDO1
Synonyms
Indoleamine-pyrrole 2,3-dioxygenase; INDO; IDO-1; IDO
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Representative Drug(s) Beta-Lapachone Drug Info Ki = 100 nM [6]
Co-Target Name Dipeptidyl peptidase 4 (DPP-4) Successful Target
UniProt ID DPP4_HUMAN
Gene Name DPP4
Synonyms
Tcell activation antigen CD26; TP103; T-cell activation antigen CD26; Dipeptidyl peptidase IV; Dipeptidyl peptidase 4 soluble form; DPP-IV; DPP IV; DPP 4; CD26; Adenosine deaminase complexing protein-2; Adenosine deaminase complexing protein 2; ADCP2; ADCP-2; ADABP
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Representative Drug(s) B-Lactams Drug Info IC50 = 120 nM [7]
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) Camptothecin Drug Info IC50 ~ 200 ug.mL-1 [8]
Co-Target Name Carbonic anhydrase IV (CA-IV) Successful Target
UniProt ID CAH4_HUMAN
Gene Name CA4
Synonyms
Carbonic anhydrase 4; Carbonate dehydratase IV; CAIV
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Representative Drug(s) B-Lactams Drug Info Ki = 293 nM [5]
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) B-Lactams Drug Info IC50 = 450 nM [9]
Co-Target Name DNA topoisomerase II (TOP2) Successful Target
UniProt ID TOP2A_HUMAN; TOP2B_HUMAN
Gene Name TOP2A; TOP2B
Synonyms
TOP2; DNA topoisomerase 2
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Representative Drug(s) Topotecan Drug Info IC50 = 480 nM [10]
Co-Target Name Xanthine dehydrogenase/oxidase (XDH) Successful Target
UniProt ID XDH_HUMAN
Gene Name XDH
Synonyms
Xanthine oxidase; Xanthine dehydrogenase; XDHA
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Representative Drug(s) B-Lactams Drug Info IC50 = 550 nM [11]
Co-Target Name Aldose reductase (AKR1B1) Successful Target
UniProt ID ALDR_HUMAN
Gene Name AKR1B1
Synonyms
Aldehyde reductase; AKR1B1
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Representative Drug(s) B-Lactams Drug Info IC50 = 600 nM [12]
Co-Target Name Glycogen synthase kinase-3 alpha (GSK-3A) Successful Target
UniProt ID GSK3A_HUMAN
Gene Name GSK3A
Synonyms
Serine/threonineprotein kinase GSK3A; Serine/threonine-protein kinase GSK3A; Glycogen synthase kinase3 alpha; Glycogen synthase kinase 3; GSK3 alpha; GSK-3 alpha; GSK-3
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Representative Drug(s) B-Lactams Drug Info IC50 = 800 nM [13]
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
Synonyms
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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Representative Drug(s) B-Lactams Drug Info IC50 = 830 nM [14]
Co-Target Name Checkpoint kinase-1 (CHK1) Clinical trial Target
UniProt ID CHK1_HUMAN
Gene Name CHEK1
Synonyms
Serine/threonine-protein kinase Chk1; Chk1; Cell cycle checkpoint kinase; CHK1 checkpoint homolog
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Representative Drug(s) Camptothecin Drug Info EC50 = 2.1 nM [15]
Co-Target Name Somatostatin receptor (SSTR) Clinical trial Target
UniProt ID SSR1_HUMAN; SSR2_HUMAN; SSR3_HUMAN; SSR4_HUMAN
Gene Name NO-GeName
Representative Drug(s) Camptothecin Drug Info IC50 = 2.21 nM [16]
Co-Target Name Lysosomal alpha-glucosidase (GAA) Successful Target
UniProt ID LYAG_HUMAN
Gene Name GAA
Synonyms
GAA; Aglucosidase alfa; Acid maltase
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Representative Drug(s) B-Lactams Drug Info IC50 = 5.96 ug.mL-1 [17]
Co-Target Name Hypoxia-inducible factor 1 alpha (HIF-1A) Clinical trial Target
UniProt ID HIF1A_HUMAN
Gene Name HIF1A
Synonyms
bHLHe78; Transcription factor HIF-1; PASD8; PAS domain-containing protein 8; Member of PAS protein 1; MOP1; Hypoxia-inducible transcription factor (HIF)-1; Hypoxia-inducible factor 1-alpha; Hypoxia-inducible factor 1 A; Hypoxia inducible factor 1; HIF1-alpha; HIF1 alpha; HIF-1alpha; HIF-1-alpha; HIF-1 alpha; Class E basic helix-loop-helix protein 78; Basic-helix-loop-helix-PAS protein MOP1; ARNT-interacting protein; ARNT interacting protein
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Representative Drug(s) Topotecan Drug Info EC50 = 12 nM Click to Show More [18]
2 Topotecan Drug Info EC50 = 71.3 nM [20]
Co-Target Name Cytochrome P450 1B1 (CYP1B1) Clinical trial Target
UniProt ID CP1B1_HUMAN
Gene Name CYP1B1
Synonyms
CYPIB1
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Representative Drug(s) B-Lactams Drug Info Ki = 56 nM [19]
Co-Target Name Hypoxia-inducible factor 2 alpha (HIF-2A) Successful Target
UniProt ID EPAS1_HUMAN
Gene Name EPAS1
Synonyms
bHLHe73; PASD2; PAS domain-containing protein 2; Member of PAS protein 2; MOP2; Hypoxia-inducible factor 2-alpha; HLF; HIF2A; HIF2-alpha; HIF-2-alpha; HIF-1-alpha-like factor; Endothelial PAS domain-containing protein 1; EPAS-1; Class E basic helix-loop-helix protein 73; Basic-helix-loop-helix-PAS protein MOP2
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Representative Drug(s) Topotecan Drug Info EC50 = 71.3 nM [20]
Co-Target Name Casein kinase II (CSNK2) Clinical trial Target
UniProt ID CSK21_HUMAN; CSK22_HUMAN; CSK23_HUMAN; CSK2B_HUMAN
Gene Name NO-GeName
Representative Drug(s) B-Lactams Drug Info IC50 = 500 nM Click to Show More [21]
2 B-Lactams Drug Info IC50 < 1000 nM [25]
Co-Target Name Glycogen synthase kinase-3 beta (GSK-3B) Clinical trial Target
UniProt ID GSK3B_HUMAN
Gene Name GSK3B
Synonyms
Serine/threonine-protein kinase GSK3B; GSK-3 beta
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Representative Drug(s) B-Lactams Drug Info IC50 = 800 nM [13]
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) B-Lactams Drug Info Ki = 800 nM [22]
Co-Target Name NADPH oxidase 4 (NOX4) Clinical trial Target
UniProt ID NOX4_HUMAN
Gene Name NOX4
Synonyms
Renal NAD(P)Hoxidase; Renal NAD(P)H-oxidase; RENOX; Kidney superoxideproducing NADPH oxidase; Kidney superoxide-producing NADPH oxidase; Kidney oxidase1; Kidney oxidase-1; KOX1; KOX-1
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Representative Drug(s) B-Lactams Drug Info IC50 = 850 nM [23]
Co-Target Name Matrix metalloproteinase-12 (MMP-12) Clinical trial Target
UniProt ID MMP12_HUMAN
Gene Name MMP12
Synonyms
Macrophage metalloelastase; Macrophage elastase; MME; ME; HME
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Representative Drug(s) B-Lactams Drug Info IC50 = 980 nM [24]
Co-Target Name Carbonic anhydrase VII (CA-VII) Patented-recorded Target
UniProt ID CAH7_HUMAN
Gene Name CA7
Synonyms
Carbonic anhydrase 7; Carbonate dehydratase VII
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Representative Drug(s) B-Lactams Drug Info Ki = 4.7 nM [5]
Co-Target Name Tyrosyl-DNA phosphodiesterase 2 (TDP2) Literature-reported Target
UniProt ID TYDP2_HUMAN
Gene Name TDP2
Synonyms
hTDP2; VPg unlinkase; Tyrosyl-RNA phosphodiesterase; Tyr-DNA phosphodiesterase 2; TRAF and TNF receptor-associated protein; TDP2; ETS1-associated protein II; ETS1-associated protein 2; EAPII; 5'-tyrosyl-DNA phosphodiesterase; 5'-Tyr-DNA phosphodiesterase
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Representative Drug(s) Beta-Lapachone Drug Info IC50 = 970 nM [26]
Co-Target Name Carboxylesterase 2 (CES2) Co-Target
UniProt ID EST2_HUMAN
Gene Name CES2
Synonyms
Cocaine esterase; CE-2; hCE-2; Methylumbelliferyl-acetate deacetylase 2
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Representative Drug(s) Beta-Lapachone Drug Info Ki = 109 nM [27]
Co-Target Name Thiosulfate sulfurtransferase (TST) Co-Target
UniProt ID THTR_HUMAN
Gene Name TST
Synonyms
Rhodanese
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Representative Drug(s) Beta-Lapachone Drug Info IC50 = 120 nM [28]
Co-Target Name Cytochrome P450 1A1 (CYP1A1) Co-Target
UniProt ID CP1A1_HUMAN
Gene Name CYP1A1
Synonyms
CYPIA1; Hydroperoxy icosatetraenoate dehydratase; Cytochrome P450 form 6; Cytochrome P450-C; Cytochrome P450-P1
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Representative Drug(s) B-Lactams Drug Info Ki = 890 nM [19]
References  Top
REF 1 Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay. J Nat Prod. 2002 Nov;65(11):1517-21.
REF 2 QSAR study of flavonoids and biflavonoids as influenza H1N1 virus neuraminidase inhibitors. Eur J Med Chem. 2010 May;45(5):1724-30.
REF 3 Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents. J Nat Prod. 1992 Nov;55(11):1529-60.
REF 4 Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely... J Med Chem. 2008 Jun 12;51(11):3154-70.
REF 5 New natural product carbonic anhydrase inhibitors incorporating phenol moieties. Bioorg Med Chem. 2015 Nov 15;23(22):7219-25.
REF 6 Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors. J Med Chem. 2015 Dec 24;58(24):9421-37.
REF 7 Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. Eur J Med Chem. 2018 May 10;151:145-157.
REF 8 Evaluation of natural products as inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. J Nat Prod. 1991 Jan-Feb;54(1):143-54.
REF 9 Design and discovery of flavonoid-based HIV-1 integrase inhibitors targeting both the active site and the interaction with LEDGF/p75. Bioorg Med Chem. 2014 Jun 15;22(12):3146-58.
REF 10 Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives. Bioorg Med Chem. 2019 Oct 1;27(19):115026.
REF 11 Structure-activity relationship and classification of flavonoids as inhibitors of xanthine oxidase and superoxide scavengers. J Nat Prod. 1998 Jan;61(1):71-6.
REF 12 Synthesis of organic nitrates of luteolin as a novel class of potent aldose reductase inhibitors. Bioorg Med Chem. 2013 Jul 15;21(14):4301-10.
REF 13 Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. J Med Chem. 2005 Feb 10;48(3):737-43.
REF 14 Flavonoids as receptor tyrosine kinase FLT3 inhibitors. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1768-70.
REF 15 Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem. 2007 Apr 1;15(7):2759-67.
REF 16 An adjustable release rate linking strategy for cytotoxin-peptide conjugates. Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.
REF 17 Antioxidant and alpha-glucosidase inhibitory compounds from Pimpinella candolleana Wight et Arn. Med Chem Res. 2012 Jan 18;21:4324-9.
REF 18 Tetracycline analogues with a selective inhibitory effect on HIF-1alpha. Medchemcomm. 2014;5:923-6.
REF 19 Comparative CYP1A1 and CYP1B1 substrate and inhibitor profile of dietary flavonoids. Bioorg Med Chem. 2011 May 1;19(9):2842-9.
REF 20 Laurenditerpenol, a new diterpene from the tropical marine alga Laurenciaintricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells. J Nat Prod. 2004 Dec;67(12):2002-7.
REF 21 A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. Bioorg Med Chem. 2019 Mar 1;27(5):677-685.
REF 22 Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. J Med Chem. 2006 Jun 1;49(11):3345-53.
REF 23 Small-molecule inhibitors of NADPH oxidase 4. J Med Chem. 2010 Sep 23;53(18):6758-62.
REF 24 Natural products as a gold mine for selective matrix metalloproteinases inhibitors. Bioorg Med Chem. 2012 Jul 1;20(13):4164-71.
REF 25 Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids. J Med Chem. 2015 Sep 24;58(18):7400-8.
REF 26 Toxoflavins and deazaflavins as the first reported selective small molecule inhibitors of tyrosyl-DNA phosphodiesterase II. J Med Chem. 2013 Aug 22;56(16):6352-70.
REF 27 Selective Inhibitors of Human Liver Carboxylesterase Based on a beta-Lapachone Scaffold: Novel Reagents for Reaction Profiling. J Med Chem. 2017 Feb 23;60(4):1568-1579.
REF 28 HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. Bioorg Med Chem Lett. 2019 May 1;29(9):1106-1112.

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