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Items: 1 to 50 of 140

1.

Design, synthesis, in vitro inhibition and toxicological evaluation of human carbonic anhydrases I, II and IX inhibitors in 5-nitroimidazole series.

Aspatwar A, Parvathaneni NK, Barker H, Anduran E, Supuran CT, Dubois L, Lambin P, Parkkila S, Winum JY.

J Enzyme Inhib Med Chem. 2020 Dec;35(1):109-117. doi: 10.1080/14756366.2019.1685510.

PMID:
31687859
2.

Multivalent Carbonic Anhydrases Inhibitors.

Carta F, Dumy P, Supuran CT, Winum JY.

Int J Mol Sci. 2019 Oct 28;20(21). pii: E5352. doi: 10.3390/ijms20215352. Review.

3.

Novel method of treating macular degeneration: a patent evaluation (WO2018/107005).

Capasso C, Winum JY.

Expert Opin Ther Pat. 2019 Oct;29(10):749-752. doi: 10.1080/13543776.2019.1661991. Epub 2019 Sep 1.

PMID:
31456444
4.

Metalloenzymes as Therapeutic Targets.

Richichi B, Spyroulias GA, Winum JY, Žalubovskis R.

Curr Med Chem. 2019;26(15):2556-2557. doi: 10.2174/092986732615190725122012.

PMID:
31453777
5.

Exploring benzoxaborole derivatives as carbonic anhydrase inhibitors: a structural and computational analysis reveals their conformational variability as a tool to increase enzyme selectivity.

Langella E, Alterio V, D'Ambrosio K, Cadoni R, Winum JY, Supuran CT, Monti SM, De Simone G, Di Fiore A.

J Enzyme Inhib Med Chem. 2019 Dec;34(1):1498-1505. doi: 10.1080/14756366.2019.1653291.

6.

Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors.

Larcher A, Nocentini A, Supuran CT, Winum JY, van der Lee A, Vasseur JJ, Laurencin D, Smietana M.

ACS Med Chem Lett. 2019 Jul 11;10(8):1205-1210. doi: 10.1021/acsmedchemlett.9b00252. eCollection 2019 Aug 8.

PMID:
31413806
7.

N-aryl-N'-ureido-O-sulfamates: Potent and selective inhibitors of the human Carbonic Anhydrase VII isoform with neuropathic pain relieving properties.

Bozdag M, Poli G, Angeli A, Lucarini E, Tuccinardi T, Di Cesare Mannelli L, Selleri S, Ghelardini C, Winum JY, Carta F, Supuran CT.

Bioorg Chem. 2019 Aug;89:103033. doi: 10.1016/j.bioorg.2019.103033. Epub 2019 Jun 6.

PMID:
31212085
8.
9.

(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators.

Rami M, Winum JY, Supuran CT, Melnyk P, Yous S.

J Enzyme Inhib Med Chem. 2019 Dec;34(1):224-229. doi: 10.1080/14756366.2018.1543292.

10.

Carbonic Anhydrase Inhibitors as Novel Drugs against Mycobacterial β-Carbonic Anhydrases: An Update on In Vitro and In Vivo Studies.

Aspatwar A, Winum JY, Carta F, Supuran CT, Hammaren M, Parikka M, Parkkila S.

Molecules. 2018 Nov 8;23(11). pii: E2911. doi: 10.3390/molecules23112911. Review.

11.

Inhibition of carbonic anhydrases by a substrate analog: benzyl carbamate directly coordinates the catalytic zinc ion mimicking bicarbonate binding.

De Simone G, Angeli A, Bozdag M, Supuran CT, Winum JY, Monti SM, Alterio V.

Chem Commun (Camb). 2018 Sep 11;54(73):10312-10315. doi: 10.1039/c8cc05755a.

PMID:
30140816
12.

Carbonic anhydrase enzymes for regulating mast cell hematopoiesis and type-2 inflammation: a patent evaluation (WO2017/058370).

Winum JY.

Expert Opin Ther Pat. 2018 Oct;28(10):741-743. doi: 10.1080/13543776.2018.1501472. Epub 2018 Jul 19.

PMID:
30010459
13.

Nitroimidazole-based inhibitors DTP338 and DTP348 are safe for zebrafish embryos and efficiently inhibit the activity of human CA IX in Xenopus oocytes.

Aspatwar A, Becker HM, Parvathaneni NK, Hammaren M, Svorjova A, Barker H, Supuran CT, Dubois L, Lambin P, Parikka M, Parkkila S, Winum JY.

J Enzyme Inhib Med Chem. 2018 Dec;33(1):1064-1073. doi: 10.1080/14756366.2018.1482285.

14.

Benzoxaborole compounds for therapeutic uses: a patent review (2010- 2018).

Nocentini A, Supuran CT, Winum JY.

Expert Opin Ther Pat. 2018 Jun;28(6):493-504. doi: 10.1080/13543776.2018.1473379. Epub 2018 May 11. Review. Erratum in: Expert Opin Ther Pat. 2018 Jun;28(6):vii.

PMID:
29727210
15.

Inhibitors of Selected Bacterial Metalloenzymes.

Žalubovskis R, Winum JY.

Curr Med Chem. 2019;26(15):2690-2714. doi: 10.2174/0929867325666180403154018. Review.

PMID:
29611472
16.

Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles.

Nocentini A, Cadoni R, Dumy P, Supuran CT, Winum JY.

J Enzyme Inhib Med Chem. 2018 Dec;33(1):286-289. doi: 10.1080/14756366.2017.1414808.

17.

Benzoxaboroles as Efficient Inhibitors of the β-Carbonic Anhydrases from Pathogenic Fungi: Activity and Modeling Study.

Nocentini A, Cadoni R, Del Prete S, Capasso C, Dumy P, Gratteri P, Supuran CT, Winum JY.

ACS Med Chem Lett. 2017 Oct 20;8(11):1194-1198. doi: 10.1021/acsmedchemlett.7b00369. eCollection 2017 Nov 9.

18.

Polyhedral Oligomeric Silsesquioxane (POSS) Bearing Glyoxylic Aldehyde as Clickable Platform Towards Multivalent Conjugates.

Kanfar N, Mehdi A, Dumy P, Ulrich S, Winum JY.

Chemistry. 2017 Dec 19;23(71):17867-17869. doi: 10.1002/chem.201703794. Epub 2017 Oct 4.

PMID:
28892198
19.

Anion inhibitors of the β-carbonic anhydrase from the pathogenic bacterium responsible of tularemia, Francisella tularensis.

Del Prete S, Vullo D, Osman SM, AlOthman Z, Donald WA, Winum JY, Supuran CT, Capasso C.

Bioorg Med Chem. 2017 Sep 1;25(17):4800-4804. doi: 10.1016/j.bmc.2017.07.033. Epub 2017 Jul 17.

PMID:
28754318
20.

Insights into the binding mode of sulphamates and sulphamides to hCA II: crystallographic studies and binding free energy calculations.

De Simone G, Langella E, Esposito D, Supuran CT, Monti SM, Winum JY, Alterio V.

J Enzyme Inhib Med Chem. 2017 Dec;32(1):1002-1011. doi: 10.1080/14756366.2017.1349764.

21.

Co-targeting intracellular pH and essential amino acid uptake cooperates to induce cell death of T-ALL/LL cells.

Imbert V, Nebout M, Mary D, Endou H, Wempe MF, Supuran CT, Winum JY, Peyron JF.

Leuk Lymphoma. 2018 Feb;59(2):460-468. doi: 10.1080/10428194.2017.1339875. Epub 2017 Jun 22.

PMID:
28641473
22.

Brucella suis carbonic anhydrases and their inhibitors: Towards alternative antibiotics?

Köhler S, Ouahrani-Bettache S, Winum JY.

J Enzyme Inhib Med Chem. 2017 Dec;32(1):683-687. doi: 10.1080/14756366.2017.1295451. Review.

23.

Effective Access to Multivalent Inhibitors of Carbonic Anhydrases Promoted by Peptide Bioconjugation.

Kanfar N, Tanc M, Dumy P, Supuran CT, Ulrich S, Winum JY.

Chemistry. 2017 May 17;23(28):6788-6794. doi: 10.1002/chem.201700241. Epub 2017 Mar 27.

PMID:
28225196
24.

New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.

van Kuijk SJA, Parvathaneni NK, Niemans R, van Gisbergen MW, Carta F, Vullo D, Pastorekova S, Yaromina A, Supuran CT, Dubois LJ, Winum JY, Lambin P.

Eur J Med Chem. 2017 Feb 15;127:691-702. doi: 10.1016/j.ejmech.2016.10.037. Epub 2016 Oct 19.

25.

Benzoxaborole as a new chemotype for carbonic anhydrase inhibition.

Alterio V, Cadoni R, Esposito D, Vullo D, Fiore AD, Monti SM, Caporale A, Ruvo M, Sechi M, Dumy P, Supuran CT, De Simone G, Winum JY.

Chem Commun (Camb). 2016 Sep 29;52(80):11983-11986.

PMID:
27722534
26.

Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors: a patent evaluation of US20160011199A1.

Winum JY.

Expert Opin Ther Pat. 2016 Nov;26(11):1223-1226. doi: 10.1080/13543776.2016.1241238. Epub 2016 Oct 4.

PMID:
27685539
27.

The anticonvulsant sulfamide JNJ-26990990 and its S,S-dioxide analog strongly inhibit carbonic anhydrases: solution and X-ray crystallographic studies.

Di Fiore A, De Simone G, Alterio V, Riccio V, Winum JY, Carta F, Supuran CT.

Org Biomol Chem. 2016 Jun 7;14(21):4853-8. doi: 10.1039/c6ob00803h. Epub 2016 May 6.

PMID:
27151329
28.

Emerging trends in enzyme inhibition by multivalent nanoconstructs.

Kanfar N, Bartolami E, Zelli R, Marra A, Winum JY, Ulrich S, Dumy P.

Org Biomol Chem. 2015 Oct 21;13(39):9894-906. doi: 10.1039/c5ob01405k. Review.

PMID:
26338715
29.

New ways to image and target tumour hypoxia and its molecular responses.

Dubois LJ, Niemans R, van Kuijk SJ, Panth KM, Parvathaneni NK, Peeters SG, Zegers CM, Rekers NH, van Gisbergen MW, Biemans R, Lieuwes NG, Spiegelberg L, Yaromina A, Winum JY, Vooijs M, Lambin P.

Radiother Oncol. 2015 Sep;116(3):352-7. doi: 10.1016/j.radonc.2015.08.022. Epub 2015 Aug 28. Review.

30.

Evaluation of carbonic anhydrase IX as a therapeutic target for inhibition of breast cancer invasion and metastasis using a series of in vitro breast cancer models.

Ward C, Meehan J, Mullen P, Supuran C, Dixon JM, Thomas JS, Winum JY, Lambin P, Dubois L, Pavathaneni NK, Jarman EJ, Renshaw L, Um IH, Kay C, Harrison DJ, Kunkler IH, Langdon SP.

Oncotarget. 2015 Sep 22;6(28):24856-70. doi: 10.18632/oncotarget.4498.

31.

Carbonic anhydrase IX inhibitors in cancer therapy: an update.

Supuran CT, Winum JY.

Future Med Chem. 2015;7(11):1407-14. doi: 10.4155/fmc.15.71. Review.

PMID:
26230880
32.

Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series.

Ombouma J, Vullo D, Dumy P, Supuran CT, Winum JY.

ACS Med Chem Lett. 2015 Jun 2;6(7):819-21. doi: 10.1021/acsmedchemlett.5b00175. eCollection 2015 Jul 9.

33.

Hydroxylamine-O-sulfonamide is a versatile lead compound for the development of carbonic anhydrase inhibitors.

Di Fiore A, Vergara A, Caterino M, Alterio V, Monti SM, Ombouma J, Dumy P, Vullo D, Supuran CT, Winum JY, De Simone G.

Chem Commun (Camb). 2015 Jul 21;51(57):11519-22. doi: 10.1039/c5cc03711e.

PMID:
26094945
34.

Fluorescent Silica Nanoparticles with Multivalent Inhibitory Effects towards Carbonic Anhydrases.

Touisni N, Kanfar N, Ulrich S, Dumy P, Supuran CT, Mehdi A, Winum JY.

Chemistry. 2015 Jul 13;21(29):10249. doi: 10.1002/chem.201501917. Epub 2015 Jun 8.

PMID:
26061872
35.

Fluorescent Silica Nanoparticles with Multivalent Inhibitory Effects towards Carbonic Anhydrases.

Touisni N, Kanfar N, Ulrich S, Dumy P, Supuran CT, Mehdi A, Winum JY.

Chemistry. 2015 Jul 13;21(29):10306-9. doi: 10.1002/chem.201501037. Epub 2015 May 12.

PMID:
25965260
36.

Designing carbonic anhydrase inhibitors for the treatment of breast cancer.

Supuran CT, Winum JY.

Expert Opin Drug Discov. 2015 Jun;10(6):591-7. doi: 10.1517/17460441.2015.1038235. Epub 2015 Apr 20. Review.

PMID:
25891195
37.

Poly(amidoamine) Dendrimers with Carbonic Anhydrase Inhibitory Activity and Antiglaucoma Action.

Carta F, Osman SM, Vullo D, Gullotto A, Winum JY, AlOthman Z, Masini E, Supuran CT.

J Med Chem. 2015 May 14;58(9):4039-45. doi: 10.1021/acs.jmedchem.5b00383. Epub 2015 Apr 15.

PMID:
25849626
38.

Binding of carbonic anhydrase IX to 45S rDNA genes is prevented by exportin-1 in hypoxic cells.

Sasso E, Vitale M, Monteleone F, Boffo FL, Santoriello M, Sarnataro D, Garbi C, Sabatella M, Crifò B, Paolella LA, Minopoli G, Winum JY, Zambrano N.

Biomed Res Int. 2015;2015:674920. doi: 10.1155/2015/674920. Epub 2015 Feb 22.

39.

N-glycosyl-N-hydroxysulfamides as potent inhibitors of Brucella suis carbonic anhydrases.

Ombouma J, Vullo D, Köhler S, Dumy P, Supuran CT, Winum JY.

J Enzyme Inhib Med Chem. 2015 Dec;30(6):1010-2. doi: 10.3109/14756366.2014.986119. Epub 2015 Mar 20.

PMID:
25792504
40.

Inhibition of β-carbonic anhydrases from Brucella suis with C-cinnamoyl glycosides incorporating the phenol moiety.

Riafrecha LE, Vullo D, Ouahrani-Bettache S, Köhler S, Dumy P, Winum JY, Supuran CT, Colinas PA.

J Enzyme Inhib Med Chem. 2015 Dec;30(6):1017-20. doi: 10.3109/14756366.2014.986120. Epub 2015 Feb 13.

PMID:
25676329
41.

Ferrier sulfamidoglycosylation of glycals catalyzed by nitrosonium tetrafluoroborate: towards new carbonic anhydrase glycoinhibitors.

Ombouma J, Vullo D, Supuran CT, Winum JY.

Bioorg Med Chem. 2014 Nov 15;22(22):6353-9. doi: 10.1016/j.bmc.2014.09.053. Epub 2014 Oct 2.

PMID:
25438758
42.

Oxo- and thiooxo-imidazo[1,5-c]pyrimidine molecule library: beyond their interest in inhibition of Brucella suis histidinol dehydrogenase, a powerful protection tool in the synthesis of histidine analogues.

Turtaut F, Lopez M, Ouahrani-Bettache S, Köhler S, Winum JY.

Bioorg Med Chem Lett. 2014 Nov 1;24(21):5008-10. doi: 10.1016/j.bmcl.2014.09.020. Epub 2014 Sep 16.

PMID:
25278235
43.

Mono- and di-halogenated histamine, histidine and carnosine derivatives are potent carbonic anhydrase I, II, VII, XII and XIV activators.

Saada MC, Vullo D, Montero JL, Scozzafava A, Supuran CT, Winum JY.

Bioorg Med Chem. 2014 Sep 1;22(17):4752-8. doi: 10.1016/j.bmc.2014.07.005. Epub 2014 Jul 10.

PMID:
25082511
44.

Recent advances in the discovery of zinc-binding motifs for the development of carbonic anhydrase inhibitors.

Winum JY, Supuran CT.

J Enzyme Inhib Med Chem. 2015 Apr;30(2):321-4. doi: 10.3109/14756366.2014.913587. Epub 2014 Jun 18. Review.

PMID:
24939097
45.

Dominant behaviours in the expression of human carbonic anhydrase hCA I activity.

Abdelrahim MY, Tanc M, Winum JY, Supuran CT, Barboiu M.

Chem Commun (Camb). 2014 Jul 28;50(59):8043-6. doi: 10.1039/c4cc03289f.

PMID:
24919797
46.

Carbonic anhydrase inhibitors. Inhibition of human cytosolic isoforms I and II with (reduced) Schiff's bases incorporating sulfonamide, carboxylate and carboxymethyl moieties.

Nasr G, Cristian A, Barboiu M, Vullo D, Winum JY, Supuran CT.

Bioorg Med Chem. 2014 May 15;22(10):2867-74. doi: 10.1016/j.bmc.2014.03.041. Epub 2014 Apr 4.

PMID:
24746465
47.

Structural basis for the rational design of new anti-Brucella agents: the crystal structure of the C366S mutant of L-histidinol dehydrogenase from Brucella suis.

D'ambrosio K, Lopez M, Dathan NA, Ouahrani-Bettache S, Köhler S, Ascione G, Monti SM, Winum JY, De Simone G.

Biochimie. 2014 Feb;97:114-20. doi: 10.1016/j.biochi.2013.09.028. Epub 2013 Oct 17.

PMID:
24140957
48.

Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates.

Rami M, Dubois L, Parvathaneni NK, Alterio V, van Kuijk SJ, Monti SM, Lambin P, De Simone G, Supuran CT, Winum JY.

J Med Chem. 2013 Nov 14;56(21):8512-20. doi: 10.1021/jm4009532. Epub 2013 Oct 31.

PMID:
24128000
49.

Metal-based carboxamide-derived compounds endowed with antibacterial and antifungal activity.

Hanif M, Chohan ZH, Winum JY, Akhtar J.

J Enzyme Inhib Med Chem. 2014 Aug;29(4):517-26. doi: 10.3109/14756366.2013.815178. Epub 2013 Aug 5.

PMID:
23914928
50.

Targeting carbonic anhydrase IX by nitroimidazole based sulfamides enhances the therapeutic effect of tumor irradiation: a new concept of dual targeting drugs.

Dubois L, Peeters SG, van Kuijk SJ, Yaromina A, Lieuwes NG, Saraya R, Biemans R, Rami M, Parvathaneni NK, Vullo D, Vooijs M, Supuran CT, Winum JY, Lambin P.

Radiother Oncol. 2013 Sep;108(3):523-8. doi: 10.1016/j.radonc.2013.06.018. Epub 2013 Jul 9.

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