Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T13201 Target Info
Target Name Carbonic anhydrase I (CA-I)
Synonyms
Carbonic anhydrase B; Carbonic anhydrase 1; Carbonate dehydratase I; CAB
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Target Type Successful Target
Gene Name CA1
Biochemical Class Alpha-carbonic anhydrase
UniProt ID
CAH1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Carbonic anhydrase II (CA-II) Successful Target
UniProt ID CAH2_HUMAN
Gene Name CA2
Synonyms
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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Representative Drug(s) Acetazolamide Drug Info Ki = 0.012 nM Click to Show More [1]
2 Ethoxzolamide Drug Info IC50 = 0.3 nM [3]
3 Drug Info Ki = 1.13 nM [2]
4 Methazolamide Drug Info IC50 = 4.8 nM [7]
5 Dichlorphenamide Drug Info Ki = 8 nM [8]
6 Drug Info Ki = 25 nM [13]
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 [2]
2 Methazolamide Drug Info Ki = 10 nM [10]
3 Acetazolamide Drug Info Ki = 11 nM [12]
4 Ethoxzolamide Drug Info Ki = 43 nM [2]
5 Dichlorphenamide Drug Info Ki = 79 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) Acetazolamide Drug Info Ki = 2.5 nM Click to Show More [4]
2 Methazolamide Drug Info Ki = 3.4 nM [6]
3 Ethoxzolamide Drug Info Ki = 22 nM [6]
4 Dichlorphenamide Drug Info Ki = 50 nM [15]
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 [5]
2 Acetazolamide Drug Info Ki = 5.7 nM [1]
3 Methazolamide Drug Info Ki = 43 nM [14]
4 Dichlorphenamide Drug Info Ki = 345 nM [5]
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 [9]
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) Acetazolamide Drug Info Ki = 11 nM Click to Show More [11]
2 Ethoxzolamide Drug Info Ki = 93 nM [17]
3 Dichlorphenamide Drug Info Ki = 95 nM [10]
4 Methazolamide Drug Info Ki = 240 nM [18]
5 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 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) Acetazolamide Drug Info Ki = 0.06 nM Click to Show More [1]
2 Ethoxzolamide Drug Info IC50 = 0.25 nM [22]
3 Methazolamide Drug Info IC50 = 0.25 nM [7]
4 Dichlorphenamide Drug Info Ki = 34 nM [8]
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 [23]
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 [24]
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 [25]
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 [26]
2 Acetazolamide Drug Info Ki = 2 nM [27]
3 Methazolamide Drug Info Ki = 2.1 nM [28]
4 Dichlorphenamide Drug Info Ki = 6 nM [10]
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 [29]
2 Acetazolamide Drug Info Ki = 1.8 nM [30]
3 Ethoxzolamide Drug Info Ki = 2 nM [30]
4 Methazolamide Drug Info Ki = 2.5 nM [30]
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) Methazolamide Drug Info Ki = 1.1 nM Click to Show More [14]
2 Acetazolamide Drug Info Ki = 3.1 nM [14]
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) Acetazolamide Drug Info Ki = 5.7 nM Click to Show More [5]
2 Methazolamide Drug Info Ki = 19 nM [33]
3 Dichlorphenamide Drug Info Ki = 23 nM [33]
Co-Target Name Carbonic anhydrase-related protein 11 (CA11) Co-Target
UniProt ID CAH11_HUMAN
Gene Name CA11
Synonyms
CA-RP XI; CA-XI; CARP XI; Carbonic anhydrase-related protein 2; CA-RP II; CARP-2
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Representative Drug(s) Acetazolamide Drug Info Ki = 5.7 nM [31]
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 [32]
2 Dichlorphenamide Drug Info Ki = 21 nM [32]
3 Acetazolamide Drug Info Ki = 54 nM [34]
4 Methazolamide Drug Info Ki = 62 nM [28]
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 [28]
2 Acetazolamide Drug Info Ki = 60 nM [13]
3 Methazolamide Drug Info Ki = 65 nM [28]
4 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 [35]
References  Top
REF 1 Fluorescent sulfonamide carbonic anhydrase inhibitors incorporating 1,2,3-triazole moieties: Kinetic and X-ray crystallographic studies. Bioorg Med Chem. 2016 Jan 15;24(2):104-12.
REF 2 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 3 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 4 Coumarinyl-substituted sulfonamides strongly inhibit several human carbonic anhydrase isoforms: solution and crystallographic investigations. Bioorg Med Chem. 2010 Jul 15;18(14):4873-8.
REF 5 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 6 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 7 Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship. Eur J Med Chem. 2013 Apr;62:597-604.
REF 8 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 9 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 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 Carbonic anhydrase inhibitors: inhibition studies of a coral secretory isoform with inorganic anions. Bioorg Med Chem Lett. 2009 Feb 1;19(3):650-3.
REF 12 Inhibition studies of new ureido-substituted sulfonamides incorporating a GABA moiety against human carbonic anhydrase isoforms I-XIV. Bioorg Med Chem. 2014 Dec 15;22(24):6768-75.
REF 13 Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5192-6.
REF 14 Carbonic anhydrases as targets for medicinal chemistry. Bioorg Med Chem. 2007 Jul 1;15(13):4336-50.
REF 15 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 16 Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. J Med Chem. 2010 Aug 12;53(15):5511-22.
REF 17 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 18 Carbonic anhydrase inhibitors: synthesis of sulfonamides incorporating dtpa tails and of their zinc complexes with powerful topical antiglaucoma properties. Bioorg Med Chem Lett. 2001 Feb 26;11(4):575-82.
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 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 23 Recent advances in the discovery and development of glyoxalase I inhibitors. Bioorg Med Chem. 2020 Feb 15;28(4):115243.
REF 24 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 25 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 26 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 27 Bortezomib inhibits mammalian carbonic anhydrases. Bioorg Med Chem. 2017 Oct 1;25(19):5064-5067.
REF 28 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 29 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 30 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 31 Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases. Bioorg Med Chem. 2017 Jul 15;25(14):3714-3718.
REF 32 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 33 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 34 Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate. J Med Chem. 2009 Apr 23;52(8):2226-32.
REF 35 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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