carbonic anhydrase ix

Summary

Summary: A carbonic anhydrase and transmembrane protein that consists of an N-terminal PROTEOGLYCAN-like domain, a catalytic region, a single-pass transmembrane domain, and a short intracellular tail. It functions as a dimer and is expressed primarily by cells of the GASTROINTESTINAL TRACT; BILE DUCT EPITHELIUM; and GALL BLADDER. It is expressed at high levels in many solid tumors, especially CLEAR CELL RENAL CARCINOMA, in response to CELL HYPOXIA.

Top Publications

  1. Kim S, Park W, Park E, Park B, Joo J, Joung J, et al. The prognostic value of BAP1, PBRM1, pS6, PTEN, TGase2, PD-L1, CA9, PSMA, and Ki-67 tissue markers in localized renal cell carcinoma: A retrospective study of tissue microarrays using immunohistochemistry. PLoS ONE. 2017;12:e0179610 pubmed publisher
    ..63) and RFS (HR, 8.51) in the multivariable model (p<0.05). pS6 and Ki-67 are significant prognostic factors of RCC; however, BAP1, PBRM1, TGase 2, PD-L1, CA9, PTEN loss, and PSMA markers did not show this association. ..
  2. Ramya P, Angapelly S, Angeli A, Digwal C, Arifuddin M, Babu B, et al. Discovery of curcumin inspired sulfonamide derivatives as a new class of carbonic anhydrase isoforms I, II, IX, and XII inhibitors. J Enzyme Inhib Med Chem. 2017;32:1274-1281 pubmed publisher
    ..89?nM) over hCA IX and hCA XII, whereas 5e was 3 and 70 times more selective against hCA II (KI =?0.75?nM) over hCA IX and hCA XII, respectively. ..
  3. Kumar R, Sharma V, Bua S, Supuran C, Sharma P. Synthesis and biological evaluation of benzenesulphonamide-bearing 1,4,5-trisubstituted-1,2,3-triazoles possessing human carbonic anhydrase I, II, IV, and IX inhibitory activity. J Enzyme Inhib Med Chem. 2017;32:1187-1194 pubmed publisher
  4. Horie K, Kawakami K, Fujita Y, Sugaya M, Kameyama K, Mizutani K, et al. Exosomes expressing carbonic anhydrase 9 promote angiogenesis. Biochem Biophys Res Commun. 2017;492:356-361 pubmed publisher
    ..Taken together, our results suggest the possibility that CA9 exosomes released from hypoxic RCC may enhance angiogenesis in microenvironment, thereby contributing to cancer progression. ..
  5. Zengin Kurt B, Sonmez F, Durdagi S, Aksoydan B, Ekhteiari Salmas R, Angeli A, et al. Synthesis, biological activity and multiscale molecular modeling studies for coumaryl-carboxamide derivatives as selective carbonic anhydrase IX inhibitors. J Enzyme Inhib Med Chem. 2017;32:1042-1052 pubmed publisher
    ..Different molecular docking algorithms were used to investigate binding poses and predicted binding energies of studied compounds at the active sites of the CA I, II, VII and IX isoforms. ..
  6. Abdoli M, Angeli A, Bozdag M, Carta F, Kakanejadifard A, Saeidian H, et al. Synthesis and carbonic anhydrase I, II, VII, and IX inhibition studies with a series of benzo[d]thiazole-5- and 6-sulfonamides. J Enzyme Inhib Med Chem. 2017;32:1071-1078 pubmed publisher
  7. Karali N, Akdemir A, Göktas F, Eraslan Elma P, Angeli A, Kızılırmak M, et al. Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases. Bioorg Med Chem. 2017;25:3714-3718 pubmed publisher
    ..Molecular modelling studies were performed to suggest modes of binding for these compounds. ..
  8. Li F, Fan Z, Qi S, Wang Y, Wang J, Liu Y, et al. Design, Synthesis, Molecular Docking Analysis, and Carbonic Anhydrase IX Inhibitory Evaluations of Novel N-Substituted-β-d-Glucosamine Derivatives that Incorporate Benzenesulfonamides. Molecules. 2017;22: pubmed publisher
    ..In addition, topological polar surface area (TPSA) value-based predictions highlighted the selectivity of these carbohydrate-based inhibitors for membrane-associated CA IX. ..
  9. Bozdag M, Alafeefy A, Altamimi A, Carta F, Supuran C, Vullo D. Synthesis of new 3-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-benzenesulfonamides with strong inhibition properties against the tumor associated carbonic anhydrases IX and XII. Bioorg Med Chem. 2017;25:2782-2788 pubmed publisher
    ..The kinetic data reported here strongly support compounds of this type for their future development as radiotracers in tumor pathologies which are strictly dependent on the enzymatic activity of the hCA IX and XII isoforms. ..

More Information

Publications20

  1. Ivanova J, Carta F, Vullo D, Leitans J, Kazaks A, Tars K, et al. N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII. Bioorg Med Chem. 2017;25:3583-3589 pubmed publisher
  2. Stanica L, Gheorghiu M, Stan M, Polonschii C, David S, Bratu D, et al. Quantitative assessment of specific carbonic anhydrase inhibitors effect on hypoxic cells using electrical impedance assays. J Enzyme Inhib Med Chem. 2017;32:1079-1090 pubmed publisher
    b>Carbonic anhydrase IX (CA IX) is an important orchestrator of hypoxic tumour environment, associated with tumour progression, high incidence of metastasis and poor response to therapy...
  3. Buonanno M, Langella E, Zambrano N, Succoio M, Sasso E, Alterio V, et al. Disclosing the Interaction of Carbonic Anhydrase IX with Cullin-Associated NEDD8-Dissociated Protein 1 by Molecular Modeling and Integrated Binding Measurements. ACS Chem Biol. 2017;12:1460-1465 pubmed publisher
  4. Zhang Z, Lau J, Zhang C, Colpo N, Nocentini A, Supuran C, et al. Design, synthesis and evaluation of 18F-labeled cationic carbonic anhydrase IX inhibitors for PET imaging. J Enzyme Inhib Med Chem. 2017;32:722-730 pubmed publisher
    b>Carbonic anhydrase IX (CA-IX) is a marker for tumor hypoxia, and its expression is negatively correlated with patient survival. CA-IX represents a potential target for eliminating hypoxic cancers...
  5. Angapelly S, Sri Ramya P, Angeli A, Supuran C, Arifuddin M. Sulfocoumarin-, Coumarin-, 4-Sulfamoylphenyl-Bearing Indazole-3-carboxamide Hybrids: Synthesis and Selective Inhibition of Tumor-Associated Carbonic Anhydrase Isozymes IX and XII. ChemMedChem. 2017;12:1578-1584 pubmed publisher
    ..8, 2.3, and 2.0 nm respectively. Further exploration of these compounds could be useful for the development of novel antitumor agents with selective mechanisms of CA inhibitory action. ..
  6. Zhu L, Guo Y, Wang L, Fan X, Xiong X, Fang K, et al. Construction of ultrasonic nanobubbles carrying CAIX polypeptides to target carcinoma cells derived from various organs. J Nanobiotechnology. 2017;15:63 pubmed publisher
    ..b>Carbonic anhydrase IX (CAIX) is highly expressed on cell membranes of various malignant solid tumors, so it's a good target for ..
  7. Nahm J, Kim H, Koo J. Glycolysis-related protein expression in thyroid cancer. Tumour Biol. 2017;39:1010428317695922 pubmed publisher
    ..Immunohistochemical staining for glucose transporter 1, hexokinase II, carbonic anhydrase IX, and monocarbonylate transporter 4 was performed, and the relationship between immunoreactivity and ..
  8. Angeli A, Carta F, Bartolucci G, Supuran C. Synthesis of novel acyl selenoureido benzensulfonamides as carbonic anhydrase I, II, VII and IX inhibitors. Bioorg Med Chem. 2017;25:3567-3573 pubmed publisher
    ..Furthermore, the selenoureido group may provide an antioxidant activity to these enzyme inhibitors. ..
  9. Bozdag M, Bua S, Osman S, Alothman Z, Supuran C. Carbonic anhydrase I, II, IV and IX inhibition with a series of 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives. J Enzyme Inhib Med Chem. 2017;32:885-892 pubmed publisher
  10. Wachters J, Schrijvers M, Slagter Menkema L, Mastik M, de Bock G, Langendijk J, et al. Prognostic significance of HIF-1a, CA-IX, and OPN in T1-T2 laryngeal carcinoma treated with radiotherapy. Laryngoscope. 2013;123:2154-60 pubmed
    ..2008) could not be confirmed. The absence of prognostic significance for HIF-1a and CA-IX toward local control in supraglottic LSCC, unlike glottic LSCC, suggests that supraglottic LSCC might represent another biological entity. ..
  11. Falsini M, Squarcialupi L, Catarzi D, Varano F, Betti M, Di Cesare Mannelli L, et al. 3-Hydroxy-1H-quinazoline-2,4-dione as a New Scaffold To Develop Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrases IX and XII. J Med Chem. 2017;60:6428-6439 pubmed publisher
    ..This finding led us to hypothesize for these compounds more than one mechanism of action involving both CAs IX and XII and other not yet identified target(s). ..