Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T20401 Target Info
Target Name Carbonic anhydrase II (CA-II)
Synonyms
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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Target Type Successful Target
Gene Name CA2
Biochemical Class Alpha-carbonic anhydrase
UniProt ID
CAH2_HUMAN
Co-Targets of This Target  Top
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 = 0.07 nM Click to Show More [1]
2 Dorzolamide Drug Info Ki = 10 nM [6]
3 Ethoxzolamide Drug Info Ki = 43 nM [1]
4 Dichlorphenamide Drug Info Ki = 79 nM [14]
5 SULTHIAME Drug Info Ki = 134 nM [16]
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) Sulfamylon Drug Info Ki = 0.3 nM Click to Show More [2]
2 Dorzolamide Drug Info Ki = 3 nM [4]
3 Ethoxzolamide Drug Info Ki = 22 nM [8]
4 Dichlorphenamide Drug Info Ki = 50 nM [13]
Co-Target Name Carbonic anhydrase I (CA-I) Successful Target
UniProt ID CAH1_HUMAN
Gene Name CA1
Synonyms
Carbonic anhydrase B; Carbonic anhydrase 1; Carbonate dehydratase I; CAB
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Representative Drug(s) Drug Info Ki = 0.31 nM Click to Show More [1]
2 Ethoxzolamide Drug Info IC50 = 15.71 nM [7]
3 Dichlorphenamide Drug Info Ki = 25 nM [9]
4 SULTHIAME Drug Info Ki = 374 nM [17]
5 Dorzolamide Drug Info Ki = 500 nM [18]
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) Ethoxzolamide Drug Info Ki = 2.5 nM Click to Show More [3]
2 Dorzolamide Drug Info Ki = 27 nM [10]
3 Dichlorphenamide Drug Info Ki = 345 nM [3]
Co-Target Name Steryl-sulfatase (STS) Successful Target
UniProt ID STS_HUMAN
Gene Name STS
Synonyms
Steryl-sulfate sulfohydrolase; Steroid sulfatase; STS; Estrone sulfatase; Arylsulfatase C; ASC
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Representative Drug(s) Drug Info IC50 = 10 uM tube-1 Click to Show More [5]
2 STX-140 Drug Info IC50 = 39 nM [11]
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) Dorzolamide Drug Info IC50 = 43 nM Click to Show More [12]
2 Ethoxzolamide Drug Info Ki = 93 nM [15]
3 Dichlorphenamide Drug Info Ki = 95 nM [10]
4 Drug Info Ki = 880 nM [21]
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) Curcumin Drug Info IC50 = 630 nM [19]
Co-Target Name Monoamine oxidase type A (MAO-A) Successful Target
UniProt ID AOFA_HUMAN
Gene Name MAOA
Synonyms
Monoamine oxidase A; Amine oxidase [flavin-containing] A
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Representative Drug(s) Curcumin Drug Info Ki = 710 nM [20]
Co-Target Name Glutamate receptor AMPA 1 (GRIA1) Successful Target
UniProt ID GRIA1_HUMAN
Gene Name GRIA1
Synonyms
Glutamate receptor ionotropic, AMPA 1; Glutamate receptor 1; GluR-K1; GluR-A; GluR-1; GluA1; GLUR1; GLUH1; AMPA-selective glutamate receptor 1
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Representative Drug(s) Cyclothiazide Drug Info EC50 = 1000 nM [22]
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) Ethoxzolamide Drug Info IC50 = 0.25 nM Click to Show More [23]
2 Dichlorphenamide Drug Info Ki = 34 nM [9]
3 SULTHIAME Drug Info Ki = 43 nM [16]
4 Dorzolamide Drug Info IC50 = 52 nM [26]
5 STX-140 Drug Info Ki = 70 nM [27]
6 Sulfamylon Drug Info Ki = 103 nM [28]
Co-Target Name Lactoylglutathione lyase (GLO1) Clinical trial Target
UniProt ID LGUL_HUMAN
Gene Name GLO1
Synonyms
S-D-lactoylglutathione methylglyoxal lyase; Methylglyoxalase; Ketone-aldehyde mutase; Glyoxalase I; GlxI; Glx I; GLO1; Aldoketomutase
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Representative Drug(s) Curcumin Drug Info Ki = 5 nM [24]
Co-Target Name Tissue factor (F3) Successful Target
UniProt ID TF_HUMAN
Gene Name F3
Synonyms
Thromboplastin; TF; F3; Coagulation factor III; CD142 antigen
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Representative Drug(s) Curcumin Drug Info IC50 = 13.16 nM [25]
Co-Target Name Prostaglandin E synthase (PTGES) Clinical trial Target
UniProt ID PTGES_HUMAN
Gene Name PTGES
Synonyms
p53-induced gene 12 protein; PIG12; PGES; PGE synthase; P53-induced apoptosis protein 12; Microsomal prostaglandin E synthase 1; Microsomal glutathione S-transferase 1-like 1; MPGES1; MPGES-1; MGST1L1; MGST1-L1
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Representative Drug(s) Curcumin Drug Info IC50 = 200 nM [29]
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) Ethoxzolamide Drug Info Ki = 0.78 nM Click to Show More [30]
2 Dorzolamide Drug Info Ki = 3.5 nM [31]
3 Dichlorphenamide Drug Info Ki = 6 nM [10]
4 Sulfamylon Drug Info Ki = 75 nM [30]
Co-Target Name Carbonic anhydrase V (CA5) Co-Target
UniProt ID CAH5A_HUMAN; CAH5B_HUMAN
Gene Name CA5A; CA5B
Synonyms
Carbonate dehydratase V; Carbonic anhydrase V; CA-V
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Representative Drug(s) Drug Info Ki = 0.84 nM Click to Show More [32]
2 Ethoxzolamide Drug Info Ki = 2 nM [33]
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) Dorzolamide Drug Info Ki = 18 nM Click to Show More [34]
2 Dichlorphenamide Drug Info Ki = 23 nM [36]
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) Ethoxzolamide Drug Info Ki = 19 nM Click to Show More [35]
2 Dichlorphenamide Drug Info Ki = 21 nM [35]
3 Dorzolamide Drug Info Ki = 33 nM [6]
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) Ethoxzolamide Drug Info Ki = 25 nM Click to Show More [37]
2 Dorzolamide Drug Info Ki = 42 nM [38]
3 Dichlorphenamide Drug Info Ki = 81 nM [10]
Co-Target Name CDGSH iron-sulfur domain-containing protein 1 (CISD1_HUMAN) Co-Target
UniProt ID CISD1_HUMAN
Gene Name CISD1
Synonyms
MitoNEET
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Representative Drug(s) Curcumin Drug Info Ki = 101 nM [39]
References  Top
REF 1 Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata. Bioorg Med Chem Lett. 2011 Jan 15;21(2):710-4.
REF 2 Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglauc... Bioorg Med Chem Lett. 2005 Feb 15;15(4):963-9.
REF 3 Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies. Bioorg Med Chem. 2011 May 15;19(10):3105-19.
REF 4 Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2377-81.
REF 5 Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES). Bioorg Med Chem Lett. 2002 May 20;12(10):1343-6.
REF 6 Carbonic anhydrases as targets for medicinal chemistry. Bioorg Med Chem. 2007 Jul 1;15(13):4336-50.
REF 7 Discovery of new potent inhibitors for carbonic anhydrase IX by structure-based virtual screening. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3496-9.
REF 8 Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties. Bioorg Med Chem. 2014 Mar 1;22(5):1586-95.
REF 9 Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic... Bioorg Med Chem Lett. 2005 Jan 17;15(2):367-72.
REF 10 Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2669-74.
REF 11 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity. J Med Chem. 2006 Dec 28;49(26):7683-96.
REF 12 Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation. Bioorg Med Chem. 2010 May 1;18(9):3307-19.
REF 13 Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies. Eur J Med Chem. 2018 Jan 1;143:1931-41.
REF 14 Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. J Med Chem. 2010 Aug 12;53(15):5511-22.
REF 15 Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mamm... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3601-5.
REF 16 Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. J Med Chem. 2009 Feb 12;52(3):646-54.
REF 17 Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis. J Med Chem. 2009 May 14;52(9):3116-20.
REF 18 Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2273-6.
REF 19 Neuritogenic activity of bi-functional bis-tryptoline triazole. Bioorg Med Chem. 2017 Feb 1;25(3):1195-1201.
REF 20 Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis. ACS Med Chem Lett. 2015 Dec 1;7(1):56-61.
REF 21 Carbonic anhydrase inhibitors: the membrane-associated isoform XV is highly inhibited by inorganic anions. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1155-8.
REF 22 Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands. Bioorg Med Chem. 2010 Feb 15;18(4):1381-7.
REF 23 Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies. Med. Chem. Commun. 2018; 9:2100-2105
REF 24 Recent advances in the discovery and development of glyoxalase I inhibitors. Bioorg Med Chem. 2020 Feb 15;28(4):115243.
REF 25 Microbial hydroxylation and glycosylation of pentacyclic triterpenes as inhibitors on tissue factor procoagulant activity. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1026-30.
REF 26 Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. J Med Chem. 2004 Jan 29;47(3):550-7.
REF 27 3,17beta-Bis-sulfamoyloxy-2-methoxyestra-1,3,5(10)-triene and Nonsteroidal Sulfamate Derivatives Inhibit Carbonic Anhydrase IX: Structure-Activity Optimization for Isoform Selectivity. J Med Chem. 2019 Feb 28;62(4):2202-2212.
REF 28 Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. J Med Chem. 2010 Apr 8;53(7):2913-26.
REF 29 Targeting microsomal prostaglandin E2 synthase-1 (mPGES-1): the development of inhibitors as an alternative to non-steroidal anti-inflammatory drugs (NSAIDs). Medchemcomm. 2015;6:2081-123.
REF 30 Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. Bioorg Med Chem Lett. 2005 Feb 15;15(4):971-6.
REF 31 Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety. Bioorg Med Chem. 2013 Sep 1;21(17):5168-74.
REF 32 Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5435-9.
REF 33 Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. Bioorg Med Chem Lett. 2005 May 2;15(9):2315-20.
REF 34 Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases. Bioorg Med Chem. 2013 Nov 15;21(22):7210-5.
REF 35 Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. J Med Chem. 2006 Nov 30;49(24):7024-31.
REF 36 Conformational variability of different sulfonamide inhibitors with thienyl-acetamido moieties attributes to differential binding in the active site of cytosolic human carbonic anhydrase isoforms. Bioorg Med Chem. 2011 Jun 15;19(12):3732-8.
REF 37 A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1371-5.
REF 38 Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors. J Med Chem. 2005 Dec 1;48(24):7860-6.
REF 39 Identification of small molecules that bind to the mitochondrial protein mitoNEET. Bioorg Med Chem Lett. 2016 Nov 1;26(21):5350-5353.

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