Co-Target(s) Information
Target General Information | Top | ||||
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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 |
Co-Targets of This Target | Top | |||||
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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) | SULFAMIDE | 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) | SULFAMIDE | 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) | Coumate | 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 | SULFAMIDE | 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) | SULFAMIDE | 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 | ||||
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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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