Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T96144 Target Info
Target Name DNA topoisomerase II (TOP2)
Synonyms
TOP2; DNA topoisomerase 2
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Target Type Successful Target
Gene Name TOP2A; TOP2B
Biochemical Class ATP-hydrolyzing DNA topoisomerase
UniProt ID
TOP2A_HUMAN; TOP2B_HUMAN
Co-Targets of This Target  Top
Co-Target Name Glucocorticoid receptor (NR3C1) Successful Target
UniProt ID GCR_HUMAN
Gene Name NR3C1
Synonyms
Nuclear receptor subfamily 3 group C member 1; GRL; GR
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Representative Drug(s) Podofilox Drug Info IC50 = 14 nM [1]
Co-Target Name Histone deacetylase 1 (HDAC1) Successful Target
UniProt ID HDAC1_HUMAN
Gene Name HDAC1
Synonyms
RPD3L1; HD1
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Representative Drug(s) Etoposide Drug Info IC50 ~ 20 ug.mL-1 [2]
Co-Target Name Multidrug resistance-associated protein 1 (ABCC1) Successful Target
UniProt ID MRP1_HUMAN
Gene Name ABCC1
Synonyms
MRP1; MRP; Leukotriene C(4) transporter; LTC4 transporter; ATP-binding cassette sub-family C member 1
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Representative Drug(s) Mitoxantrone Drug Info IC50 = 27.5 nM [3]
Co-Target Name Carbonic anhydrase VI (CA-VI) Successful Target
UniProt ID CAH6_HUMAN
Gene Name CA6
Synonyms
Secreted carbonic anhydrase; Salivary carbonic anhydrase; Carbonic anhydrase 6; Carbonate dehydratase VI
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Representative Drug(s) Drug Info Ki = 33 nM [4]
Co-Target Name Carbonic anhydrase XIV (CA-XIV) Successful Target
UniProt ID CAH14_HUMAN
Gene Name CA14
Synonyms
UNQ690/PRO1335; Carbonic anhydrase 14; Carbonate dehydratase XIV
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Representative Drug(s) Drug Info Ki = 36 nM [4]
Co-Target Name DNA topoisomerase II beta (TOP2B) Successful Target
UniProt ID TOP2B_HUMAN
Gene Name TOP2B
Synonyms
Topo IIbeta; TOP2beta; TOP2B
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Representative Drug(s) Nalidixic Acid Drug Info IC50 = 52 ug.mL-1 Click to Show More [5]
2 Etoposide Drug Info IC50 = 69.8 nM [6]
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) Drug Info Ki = 93 nM [7]
Co-Target Name Solute carrier family 47 member 1 (SLC47A1) Successful Target
UniProt ID S47A1_HUMAN
Gene Name SLC47A1
Synonyms
hMATE-1; Multidrug and toxin extrusion protein 1; MATE1; MATE-1
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Representative Drug(s) Mitoxantrone Drug Info IC50 = 190 nM [8]
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) Amsacrine Drug Info IC50 = 208.93 nM Click to Show More [9]
2 GSK2140944 Drug Info IC50 = 588 ug.mL-1 [11]
Co-Target Name Tubulin (TUB) Successful Target
UniProt ID TBA1A_HUMAN; TBA1B_HUMAN; TBA1C_HUMAN; TBA3C_HUMAN; TBA3E_HUMAN; TBA4A_HUMAN; TBB1_HUMAN; TBB2A_HUMAN; TBB2B_HUMAN; TBB3_HUMAN; TBB4A_HUMAN; TBB4B_HUMAN; TBB5_HUMAN; TBB6_HUMAN; TBB8_HUMAN
Gene Name NO-GeName
Synonyms
Human tubulin
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Representative Drug(s) Podofilox Drug Info IC50 = 260 nM [10]
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) Drug Info Ki = 360 nM [4]
Co-Target Name ATP-binding cassette transporter G2 (ABCG2) Successful Target
UniProt ID ABCG2_HUMAN
Gene Name ABCG2
Synonyms
Urate exporter; Placenta-specific ATP-binding cassette transporter; Mitoxantrone resistance-associated protein; MXR; CDw338; CD338; Breast cancer resistance protein; BCRP1; BCRP; ABCP
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Representative Drug(s) Mitoxantrone Drug Info IC50 = 903.8 nM [3]
Co-Target Name Tyrosine-protein kinase BTK (ATK) Successful Target
UniProt ID BTK_HUMAN
Gene Name BTK
Synonyms
Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
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Representative Drug(s) Mitoxantrone Drug Info IC50 = 1000 nM [12]
Co-Target Name Aurora kinase A (AURKA) Clinical trial Target
UniProt ID AURKA_HUMAN
Gene Name AURKA
Synonyms
hARK1; Serine/threonine-protein kinase aurora-A; Serine/threonine-protein kinase 6; Serine/threonine-protein kinase 15; Serine/threonine kinase 15; STK6; STK15; IAK1; Breast tumor-amplified kinase; BTAK; Aurora/IPL1-related kinase 1; Aurora-related kinase 1; Aurora-A; Aurora 2; AYK1; AURA; ARK1; ARK-1; AIRK1; AIK
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Representative Drug(s) Doxorubicin Drug Info IC50 = 40 nM [13]
Co-Target Name Carbonic anhydrase IX (CA-IX) Clinical trial Target
UniProt ID CAH9_HUMAN
Gene Name CA9
Synonyms
Renal cell carcinoma-associated antigen G250; RCC-associated antigen G250; PMW1; P54/58N; Membrane antigen MN; MN; G250 antigen (MN/CA IX/G250); G250; Carbonic anhydrase 9; Carbonate dehydratase IX; CAIX
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Representative Drug(s) Drug Info Ki = 82 nM [4]
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) Doxorubicin Drug Info EC50 = 120 nM [14]
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) Doxorubicin Drug Info EC50 = 120 nM [14]
Co-Target Name DNA topoisomerase II alpha (TOP2A) Clinical trial Target
UniProt ID TOP2A_HUMAN
Gene Name TOP2A
Synonyms
DNA topoisomerase II, alpha isozyme; DNA topoisomerase 2alpha; DNA topoisomerase 2-alpha
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Representative Drug(s) Doxorubicin Drug Info IC50 = 600 nM [15]
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) Mitoxantrone Drug Info IC50 = 660 nM [12]
Co-Target Name Caspase-3 (CASP3) Clinical trial Target
UniProt ID CASP3_HUMAN
Gene Name CASP3
Synonyms
Yama protein; SREBP cleavage activity 1; SCA-1; Protein Yama; Cysteine protease CPP32; Caspase 3; CPP32; CPP-32; CASP-3; Apopain
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Representative Drug(s) Etoposide Drug Info IC50 < 1000 nM [16]
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) Drug Info Ki = 420 nM [4]
Co-Target Name Multidrug and toxin extrusion protein 2 (MATE2) Literature-reported Target
UniProt ID S47A2_HUMAN
Gene Name SLC47A2
Synonyms
hMATE-2; Solute carrier family 47 member 2; MATE2; MATE-2; Kidney-specific H(+)/organic cation antiporter
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Representative Drug(s) Mitoxantrone Drug Info IC50 = 530 nM [8]
Co-Target Name Carbonic anhydrase XIII (CA13) Co-Target
UniProt ID CAH13_HUMAN
Gene Name CA13
Synonyms
Carbonic anhydrase 13; Carbonate dehydratase XIII; CA-XIII
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Representative Drug(s) Drug Info Ki = 65 nM [4]
Co-Target Name Carbonic anhydrase VA (CA5A) Co-Target
UniProt ID CAH5A_HUMAN
Gene Name CA5A
Synonyms
Carbonic anhydrase 5A, mitochondrial; Carbonate dehydratase VA; CA-VA
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Representative Drug(s) Drug Info Ki = 410 nM [4]
Co-Target Name Carbonic anhydrase III (CA3) Co-Target
UniProt ID CAH3_HUMAN
Gene Name CA3
Synonyms
Carbonic anhydrase 3; Carbonate dehydratase III; CA-III
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Representative Drug(s) Drug Info Ki = 570 nM [4]
Co-Target Name Carbonic anhydrase VB (CA5B) Co-Target
UniProt ID CAH5B_HUMAN
Gene Name CA5B
Synonyms
Carbonic anhydrase 5B, mitochondrial; Carbonate dehydratase VB; Carbonic anhydrase VB; CA-VB
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Representative Drug(s) Drug Info Ki = 750 nM [4]
References  Top
REF 1 Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity. Antimicrob Agents Chemother. 2009 Jul;53(7):2824-33.
REF 2 The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase. Bioorg Med Chem. 2013 Nov 15;21(22):6981-95.
REF 3 Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors. J Med Chem. 2019 Sep 26;62(18):8578-8608.
REF 4 New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2182-5.
REF 5 DNA gyrase inhibitory and antimicrobial activities of some diphenic acid monohydroxamides. J Med Chem. 1997 Sep 26;40(20):3292-6.
REF 6 Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line. Eur J Med Chem. 2018 Aug 5;156:563-79.
REF 7 Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines. ACS Med Chem Lett. 2018 Aug 29;9(9):947-51.
REF 8 Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. J Med Chem. 2013 Feb 14;56(3):781-795.
REF 9 Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30.
REF 10 Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. Eur J Med Chem. 2017 Dec 1;141:460-72.
REF 11 Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety. Bioorg Med Chem Lett. 2018 Aug 1;28(14):2477-80.
REF 12 A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling. J Med Chem. 2013 Mar 28;56(6):2619-29.
REF 13 Single step synthesis of new fused pyrimidine derivatives and their evaluation as potent Aurora-A kinase inhibitors. Eur J Med Chem. 2011 Sep;46(9):3690-5.
REF 14 Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii. J Nat Prod. 2009 May 22;72(5):805-12.
REF 15 Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria. J Med Chem. 2019 Mar 28;62(6):2950-2973.
REF 16 Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50.

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