Target Information

Target General Infomation
Target ID
T64567
Former ID
TTDR00211
Target Name
Carbonic anhydrase IX
Gene Name
CA9
Synonyms
CA-IX; CAIX; Carbonate dehydratase IX; G250 antigen (MN/CA IX/G250); Membrane antigen MN; P54/58N; PMW1; RCC-associated antigen G250; Renal cell carcinoma-associated antigen G250; CA9
Target Type
Clinical Trial
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Clear cell renal cell carcinoma [ICD9: 189; ICD10: C64]
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86]
Renal cancer [ICD9: 140-229, 189; ICD10: C64]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Reversible hydration of carbon dioxide. Participates in pH regulation. May be involved in the control of cell proliferation and transformation. Appears to be a novel specific biomarker for a cervical neoplasia.
BioChemical Class
Carbon-oxygen lyases
Target Validation
T64567
UniProt ID
Q16790
EC Number
EC 4.2.1.1
Sequence
MAPLCPSPWLPLLIPAPAPGLTVQLLLSLLLLVPVHPQRLPRMQEDSPLGGGSSGEDDPL
GEEDLPSEEDSPREEDPPGEEDLPGEEDLPGEEDLPEVKPKSEEEGSLKLEDLPTVEAPG
DPQEPQNNAHRDKEGDDQSHWRYGGDPPWPRVSPACAGRFQSPVDIRPQLAAFCPALRPL
ELLGFQLPPLPELRLRNNGHSVQLTLPPGLEMALGPGREYRALQLHLHWGAAGRPGSEHT
VEGHRFPAEIHVVHLSTAFARVDEALGRPGGLAVLAAFLEEGPEENSAYEQLLSRLEEIA
EEGSETQVPGLDISALLPSDFSRYFQYEGSLTTPPCAQGVIWTVFNQTVMLSAKQLHTLS
DTLWGPGDSRLQLNFRATQPLNGRVIEASFPAGVDSSPRAAEPVQLNSCLAAGDILALVF
GLLFAVTSVAFLVQMRRQHRRGTKGGVSYRPAEVAETGA
Drugs and Mode of Action
Drug(s) MAFENIDE Drug Info Approved Bacterial infection [530765]
Curcumin Drug Info Phase 3 Cancer [532348], [542031]
Girentuximab Drug Info Phase 3 Clear cell renal cell carcinoma [524178], [542901]
PARABEN Drug Info Phase 3 Discovery agent [524059]
PHENOL Drug Info Phase 2/3 Discovery agent [525296]
COUMATE Drug Info Phase 2 Breast cancer [531371]
Girentuximab I-124 Drug Info Phase 2 Renal cancer [522378]
INDISULAM Drug Info Phase 2 Lymphoma [521486], [542057]
90Y-cG250 Drug Info Phase 1 Cancer [521704]
BAY 79-4620 Drug Info Phase 1 Solid tumours [522886]
SULFAMIDE Drug Info Phase 1 Discovery agent [524873]
CA9-ADC Drug Info Discontinued in Phase 1 Solid tumours [549015]
SPERMINE Drug Info Terminated Discovery agent [542107], [546483]
Inhibitor (2-bromophenyl)difluoromethanesulfonamide Drug Info [527782]
(4-bromophenyl)difluoromethanesulfonamide Drug Info [527782]
(4-sulfamoylphenylethylthioureido)fluorescein Drug Info [529381]
1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide Drug Info [530978]
1,4-phenylene disulfamate Drug Info [529884]
1-(3,4-dichlorophenyl)-3-hydroxyurea Drug Info [528240]
1-acetamido-5-sulfonamidoindane Drug Info [528160]
1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide Drug Info [530978]
1-cyclohexylamido-5-sulfonamidoindane Drug Info [528160]
1-pentafluorophenylamido-5-sulfonamidoindane Drug Info [528160]
1-valproylamido-5-sulfonamidoindane Drug Info [528160]
2,2,2-Trifluoro-N-(4-sulfamoyl-phenyl)-acetamide Drug Info [527743]
2,2-Dimethyl-N-(4-sulfamoyl-phenyl)-propionamide Drug Info [527743]
2,4-Disulfamyltrifluoromethylaniline Drug Info [529948]
2-(4-chlorobenzyloxyamino)-N-hydroxyacetamide Drug Info [528653]
2-(4-chlorobenzyloxyamino)-N-hydroxyhexanamide Drug Info [528653]
2-(4-chlorobenzyloxyamino)-N-hydroxypropanamide Drug Info [528653]
2-(benzyloxyamino)-N-hydroxy-3-methylpentanamide Drug Info [528653]
2-(benzyloxyamino)-N-hydroxyacetamide Drug Info [528653]
2-(benzyloxyamino)-N-hydroxyhexanamide Drug Info [528653]
2-(N''-Acetyl-hydrazino)-benzenesulfonamide Drug Info [527482]
2-acetamido-5-sulfonamidoindane Drug Info [528160]
2-Amino-benzenesulfonamide Drug Info [529948]
2-butylamido-5-sulfonamidoindane Drug Info [528160]
2-cyclohexylamido-5-sulfonamidoindane Drug Info [528160]
2-ethylamido-5-sulfonamidoindane Drug Info [528160]
2-Hydrazinocarbonyl-benzenesulfonamide Drug Info [527482]
2-hydrazinylbenzenesulfonamide Drug Info [529948]
2-Mercapto-N-(4-sulfamoyl-phenyl)-benzamide Drug Info [529381]
2-Morpholin-4-yl-N-(4-sulfamoyl-phenyl)-acetamide Drug Info [527338]
2-nonylamido-5-sulfonamidoindane Drug Info [528160]
2-oxo-2H-chromene-3-carboxylic acid Drug Info [530514]
2-oxo-2H-thiochromene-3-carboxylic acid Drug Info [530514]
2-pentafluorophenylamido-5-sulfonamidoindane Drug Info [528160]
2-propylamido-5-sulfonamidoindane Drug Info [528160]
2-Sulfamoyl-benzoic acid methyl ester Drug Info [527482]
2-valproylamido-5-sulfonamidoindane Drug Info [528160]
3-((4-aminophenyl)diazenyl)benzenesulfonamide Drug Info [530399]
3-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Drug Info [530399]
3-(3-Phenyl-ureido)-benzenesulfonamide Drug Info [527743]
3-(4'-Hydroxyphenyl)diazenylbenzenesulfonamide Drug Info [530399]
3-Amino-benzenesulfonamide Drug Info [527654]
3-bromophenyl-difluoromethanesulfonamide Drug Info [527782]
3-Chloro-4-hydrazino-benzenesulfonamide Drug Info [527482]
3-Fluoro-4-hydrazino-benzenesulfonamide Drug Info [527482]
3-mercapto-N-(4-sulfamoyl-phenyl)-propionamide Drug Info [528406]
4,4'-thiodipyridine-3-sulfonamide Drug Info [530766]
4-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Drug Info [530399]
4-(2-Amino-ethyl)-benzenesulfonamide Drug Info [527645]
4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide Drug Info [529948]
4-(2-Hydroxy-ethyl)-benzenesulfonamide Drug Info [529948]
4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Drug Info [530766]
4-(2-Propynylthio)pyridine-3-sulfonamide Drug Info [530766]
4-(4'-N-Methylphenyl)diazenylbenzenesulfonamide Drug Info [530399]
4-(4-Cyanophenoxy)-3-pyridinesulfonamide Drug Info [530766]
4-(4-Fluorophenoxy)-3-pyridinesulfonamide Drug Info [530766]
4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Drug Info [530766]
4-(Allylamino)-3-pyridinesulfonamide Drug Info [530766]
4-(Carbamolymethylthio)pyridine-3-sulfonamide Drug Info [530766]
4-(Cyanomethylthio)pyridine-3-sulfonamide Drug Info [530766]
4-(hydroxymethyl)benzenesulfonamide Drug Info [529948]
4-(Methylhydrazino)-3-pyridinesulfonamide Drug Info [530766]
4-(N-Oxide-2-pyridylthio)pyridine-3-sulfonamide Drug Info [530766]
4-(Quinolinoxy)-3-pyridinesulfonamide Drug Info [530766]
4-Amino-3-bromo-benzenesulfonamide Drug Info [529948]
4-Amino-3-chloro-benzenesulfonamide Drug Info [529948]
4-Amino-3-fluoro-benzenesulfonamide Drug Info [529948]
4-Amino-3-iodo-benzenesulfonamide Drug Info [529948]
4-amino-6-chlorobenzene-1,3-disulfonamide Drug Info [529948]
4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide Drug Info [529948]
4-azidobenzenesulfonamide Drug Info [530020]
4-Benzenesulfonylamino-benzenesulfonamide Drug Info [527743]
4-Benzythiopyridine-3-sulfonamide Drug Info [530766]
4-Ethoxy-3-pyridinesulfonamide Drug Info [530766]
4-ethynyl benzene sulfonamide Drug Info [529344]
4-fluoro-N-(4-sulfamoylbenzyl)benzenesulfonamide Drug Info [529884]
4-Hydrazino-3-pyridinesulfonamide Drug Info [530766]
4-Hydrazino-benzenesulfonamide Drug Info [529948]
4-Hydrazinocarbonyl-benzenesulfonamide Drug Info [527482]
4-Methanesulfonylamino-benzenesulfonamide Drug Info [527743]
4-Methoxy-3-pyridinesulfonamide Drug Info [530766]
4-methylphenyl-difluoromethanesulfonamide Drug Info [527782]
4-Methylthiopyridine-3-sulfonamide Drug Info [530766]
4-nitrophenyl-difluoromethanesulfonamide Drug Info [527782]
4-[2-(3-Phenyl-ureido)-ethyl]-benzenesulfonamide Drug Info [527743]
5-amino-1,3,4-thiadiazole-2-sulfonamide Drug Info [531013]
5-Amino-[1,3,4]thiadiazole-2-thiol Drug Info [527519]
6-(aminomethyl)-2H-chromen-2-one Drug Info [530514]
6-(hydroxymethyl)-2H-chromen-2-one Drug Info [530514]
6-Acetyl-7-ethoxy-2H-chromen-2-one Drug Info [531259]
6-Acetyl-7-hydroxy-2H-chromen-2-one Drug Info [531259]
6-acetyl-7-methoxy-2H-chromen-2-one Drug Info [531259]
6-acetyl-7-propoxy-2H-chromen-2-one Drug Info [531259]
6-Hydroxy-benzothiazole-2-sulfonic acid amide Drug Info [529948]
6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info [530514]
6-methyl-2-oxo-2H-chromene-3-carboxylic acid Drug Info [530514]
7-(benzyloxy)-2H-chromen-2-one Drug Info [530514]
7-butoxy-2H-chromen-2-one Drug Info [530514]
7-ethoxy-8-propionyl-2H-chromen-2-one Drug Info [531259]
7-hydroxy-6-propionyl-2H-chromen-2-one Drug Info [531259]
7-hydroxy-8-propionyl-2H-chromen-2-one Drug Info [531259]
7-methoxy-2-oxo-2H-chromene-4-carboxylic acid Drug Info [530514]
7-methoxy-8-propionyl-2H-chromen-2-one Drug Info [531259]
7-phenethoxy-2H-chromen-2-one Drug Info [530514]
7-propoxy-2H-chromen-2-one Drug Info [530514]
8-acetyl-7-(benzyloxy)-2H-chromen-2-one Drug Info [531259]
8-acetyl-7-butoxy-2H-chromen-2-one Drug Info [531259]
8-acetyl-7-ethoxy-2H-chromen-2-one Drug Info [531259]
8-Acetyl-7-hydroxy-2H-chromen-2-one Drug Info [531259]
8-acetyl-7-methoxy-2H-chromen-2-one Drug Info [531259]
8-acetyl-7-propoxy-2H-chromen-2-one Drug Info [531259]
8-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info [530514]
8-Propionyl-7-propoxy-2H-chromen-2-one Drug Info [531259]
ACETYLSULFANILAMIDE Drug Info [527743]
Aminobenzolamide derivative Drug Info [527261]
Azide Drug Info [527260]
BENZOLAMIDE Drug Info [529948]
BICARBONATE Drug Info [527389]
Carzenide Drug Info [529948]
CATECHIN Drug Info [531068]
COUMARIN Drug Info [530514]
COUMATE Drug Info [529605]
Curcumin Drug Info [531068]
Decane-1,10-diyl disulfamate Drug Info [530359]
Decyl sulfamate Drug Info [530359]
ELLAGIC ACID Drug Info [530751]
ETHOXYCOUMARIN Drug Info [530514]
Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Drug Info [530514]
FERULIC ACID Drug Info [530751]
GALLICACID Drug Info [530751]
HERNIARIN Drug Info [530514]
Hexane-1,6-diamine Drug Info [530998]
HYDROSULFIDE Drug Info [527260]
MAFENIDE Drug Info [530765]
MMI270 Drug Info [528653]
N-(4-cyanophenyl)sulfamide Drug Info [527520]
N-(4-Sulfamoyl-phenyl)-benzamide Drug Info [527743]
N-(4-Sulfamoyl-phenyl)-butyramide Drug Info [527743]
N-(4-Sulfamoyl-phenyl)-isobutyramide Drug Info [527743]
N-(4-Sulfamoyl-phenyl)-propionamide Drug Info [527743]
N-(4-sulfamoylphenylethyl)-4-sulfamoylbenzamide Drug Info [551223]
N-(5-Mercapto-[1,3,4]thiadiazol-2-yl)-acetamide Drug Info [527519]
N-(pentafluorophenyl)sulfamide Drug Info [527520]
N-hydroxysulfamide Drug Info [530922]
N-propynyl amidebenzenesulphonide Drug Info [528491]
N1-(2-aminoethyl)ethane-1,2-diamine Drug Info [530998]
N1-(naphthalen-1-yl)ethane-1,2-diamine Drug Info [530998]
NSC-654077 Drug Info [529381]
Octane-1,8-diyl disulfamate Drug Info [530359]
Octyl sulfamate Drug Info [530359]
P-Coumaric Acid Drug Info [530751]
P-TOLUENESULFONAMIDE Drug Info [529948]
PARABEN Drug Info [530751]
Pentane-1,5-diamine Drug Info [530998]
Pentanoic acid (4-sulfamoyl-phenyl)-amide Drug Info [527743]
PHENOL Drug Info [531068]
PHENYLDIFLUOROMETHANESULFONAMIDE Drug Info [527782]
PHENYLMETHANESULFONAMIDE Drug Info [527782]
PHENYLSULFAMATE Drug Info [527782]
Prop-2-ynyl 4-sulfamoylbenzoate Drug Info [528491]
Quinoline-8-sulfonamide Drug Info [529884]
SACCHARIN Drug Info [529179]
Sodium N-methylphenylaminomethanesulfonate Drug Info [530399]
Sodium phenylaminomethanesulfonate Drug Info [530399]
SPERMINE Drug Info [530998]
SULFAMATE Drug Info [527389]
Sulfamic acid 12-sulfamoyloxy-dodecyl ester Drug Info [527391]
Sulfamic acid 16-sulfamoyloxy-hexadecyl ester Drug Info [527391]
Sulfamic acid 3-sulfamoyloxy-phenyl ester Drug Info [527391]
Sulfamic acid 4-sulfamoyloxy-butyl ester Drug Info [527391]
Sulfamic acid 4-sulfamoyloxymethyl-benzyl ester Drug Info [527391]
Sulfamic acid 6-sulfamoyloxy-hexyl ester Drug Info [527391]
Sulfamic acid 7-sulfamoyloxy-heptyl ester Drug Info [527391]
SULFAMIDE Drug Info [527389]
Sulfanilamide derivative Drug Info [527560]
Syringic Acid Drug Info [530751]
UMBELLIFERONE Drug Info [531259]
Enhancer Girentuximab I-124 Drug Info [532138], [532748]
Modulator INDISULAM Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Nitrogen metabolism
Pathway Interaction Database HIF-1-alpha transcription factor network
Reactome Regulation of gene expression by Hypoxia-inducible Factor
Reversible hydration of carbon dioxide
WikiPathways Vitamin D Receptor Pathway
Reversible Hydration of Carbon Dioxide
Regulation of Hypoxia-inducible Factor (HIF) by Oxygen
References
Ref 521486ClinicalTrials.gov (NCT00014625) E7070 in Treating Patients With Stage IV Melanoma. U.S. National Institutes of Health.
Ref 521704ClinicalTrials.gov (NCT00199875) Treatment of Patients With Advanced Renal Cancer With a Radio-labeled Antibody, Yttrium-90 Conjugated Chimeric G250. U.S. National Institutes of Health.
Ref 522378ClinicalTrials.gov (NCT00717587) Sunitinib Before and After Surgery in Treating Patients With Stage IV Kidney Cancer. U.S. National Institutes of Health.
Ref 522886ClinicalTrials.gov (NCT01028755) To Determine Maximum Tolerated Dose of BAY79-4620 in Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 524059ClinicalTrials.gov (NCT01688479) Trial Comparing Calendula Officinalis With Aqueous Cream "Essex" to Treat Skin Reactions From Radiotherapy of Breast Cancer. U.S. National Institutes of Health.
Ref 524178ClinicalTrials.gov (NCT01762592) REDECT 2: REnal Masses: Pivotal Trial to DEteCT Clear Cell Renal Cell Carcinoma With PET/CT. U.S. National Institutes of Health.
Ref 524873ClinicalTrials.gov (NCT02216669) Trial to Determine Optimal Phase II Dose of the Oral Dual CAIX Inhibitor/ Radiosensitizer. U.S. National Institutes of Health.
Ref 525296ClinicalTrials.gov (NCT02527187) Determination of the Sensitivity and Specificity of Prick Test Betula Verrucosa.
Ref 530765J Med Chem. 2010 Apr 8;53(7):2913-26.Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases.
Ref 531371Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer. Expert Rev Anticancer Ther. 2011 Feb;11(2):179-83.
Ref 532348Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68.
Ref 542031(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7000).
Ref 542057(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7046).
Ref 542107(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 710).
Ref 542901(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7987).
Ref 546483Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008464)
Ref 549015Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031507)
Ref 527260Bioorg Med Chem Lett. 2004 Dec 6;14(23):5769-73.Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions.
Ref 527261Bioorg Med Chem Lett. 2004 Dec 6;14(23):5775-80.Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide.
Ref 527338Bioorg Med Chem Lett. 2005 Jan 17;15(2):367-72.Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX.
Ref 527389Bioorg Med Chem Lett. 2005 Feb 1;15(3):567-71.Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate.
Ref 527391Bioorg Med Chem Lett. 2005 Feb 1;15(3):579-84.Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.
Ref 527482J Med Chem. 2005 Mar 24;48(6):2121-5.Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporatinghydrazino moieties.
Ref 527519Bioorg Med Chem Lett. 2005 May 2;15(9):2347-52.Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols.
Ref 527520Bioorg Med Chem Lett. 2005 May 2;15(9):2353-8.Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxysulfamides--a new zinc-binding function in the design of inhibitors.
Ref 527560Bioorg Med Chem Lett. 2005 Jun 15;15(12):3096-101.Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes.
Ref 527645J Med Chem. 2005 Jul 28;48(15):4834-41.Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors.
Ref 527654Bioorg Med Chem Lett. 2005 Sep 1;15(17):3828-33.Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides.
Ref 527743Bioorg Med Chem Lett. 2005 Nov 1;15(21):4862-6.Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides.
Ref 527782Bioorg Med Chem Lett. 2005 Dec 1;15(23):5192-6. Epub 2005 Oct 3.Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides.
Ref 528160J Med Chem. 2006 May 4;49(9):2743-9.Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX.
Ref 528240Bioorg Med Chem Lett. 2006 Aug 15;16(16):4316-20. Epub 2006 Jun 12.N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors.
Ref 528406J Med Chem. 2006 Sep 7;49(18):5544-51.Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.
Ref 528491J Med Chem. 2006 Nov 2;49(22):6539-48.A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
Ref 528653Bioorg Med Chem. 2007 Mar 15;15(6):2298-311. Epub 2007 Jan 19.Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I andII with sulfonylated hydroxamates.
Ref 529179Bioorg Med Chem Lett. 2008 Jan 15;18(2):836-41. Epub 2007 Nov 13.Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potentinhibitors of the tumor-associated isoforms IX and XII.
Ref 529344J Med Chem. 2008 Mar 27;51(6):1945-53. Epub 2008 Feb 29.Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides.
Ref 529381J Med Chem. 2008 Jun 12;51(11):3051-6. Epub 2008 Mar 19.Recent developments of carbonic anhydrase inhibitors as potential anticancer drugs.
Ref 529605Bioorg Med Chem Lett. 2008 Aug 1;18(15):4282-6. Epub 2008 Jul 5.Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
Ref 529884Bioorg Med Chem. 2009 Jan 15;17(2):553-7. Epub 2008 Dec 6.Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors.
Ref 529948J Med Chem. 2009 Feb 12;52(3):646-54.Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
Ref 530020Bioorg Med Chem Lett. 2009 Apr 15;19(8):2273-6. Epub 2009 Feb 26.Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties.
Ref 530359J Med Chem. 2009 Oct 8;52(19):5990-8.Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors.
Ref 530399Bioorg Med Chem. 2009 Oct 15;17(20):7093-9. Epub 2009 Sep 6.Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XIIover the cytosolic isoforms I and II.
Ref 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 530751Bioorg Med Chem. 2010 Mar 15;18(6):2159-64. Epub 2010 Feb 6.Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids.
Ref 530765J Med Chem. 2010 Apr 8;53(7):2913-26.Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases.
Ref 530766Eur J Med Chem. 2010 Jun;45(6):2396-404. Epub 2010 Feb 12.Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides.
Ref 530922Bioorg Med Chem Lett. 2010 Jun 15;20(12):3601-5. Epub 2010 Apr 28.Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV.
Ref 530978Eur J Med Chem. 2010 Sep;45(9):3656-61. Epub 2010 May 12.Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII.
Ref 530998J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule.
Ref 531013Bioorg Med Chem Lett. 2010 Aug 1;20(15):4376-81. Epub 2010 Jun 17.Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamideresides in a less utilized binding pocket than most hydrophobic inhibitors.
Ref 531068Bioorg Med Chem Lett. 2010 Sep 1;20(17):5050-3. Epub 2010 Jul 13.Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV.
Ref 531259Bioorg Med Chem Lett. 2010 Dec 15;20(24):7255-8. Epub 2010 Oct 25.7,8-disubstituted- but not 6,7-disubstituted coumarins selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic ones I and II in the low nanomolar/subnanomolar range.
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Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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