In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas
Cazzamalli S, Figueras Agustí E, Petho L, Borbély AN, Steinkuhler C, Neri D, Sewald N (2018)
ACS Omega 3(11): 14726-14731.
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Autor*in
Cazzamalli, Samuele;
Figueras Agustí, EduardUniBi;
Petho, Lilla;
Borbély, Adina NoémiUniBi;
Steinkuhler, Christian;
Neri, Dario;
Sewald, NorbertUniBi 
Einrichtung
Abstract / Bemerkung
Traditional chemotherapeutics used in cancer therapy do not preferentially accumulate in tumor tissues. The conjugation to delivery vehicles like antibodies or small molecules has been proposed as a strategy to increase the tumor uptake and improve the therapeutic window of these drugs. Here, we report the synthesis and the biological evaluation of a novel small molecule-drug conjugate (SMDC) comprising a high-affinity bidentate acetazolamide derivative, targeting carbonic anhydrase IX (CAIX), and cryptophycin, a potent microtubule destabilizer. The biological activity of the novel SMDC was evaluated in vitro, measuring binding to the CAIX antigen by surface plasmon resonance and cytotoxicity against SKRC-52 cells. In vivo studies showed a delayed growth of tumors in nude mice bearing SKRC-52 renal cell carcinomas.
Erscheinungsjahr
2018
Zeitschriftentitel
ACS Omega
Band
3
Ausgabe
11
Seite(n)
14726-14731
Urheberrecht / Lizenzen
ISSN
2470-1343
Page URI
https://pub.uni-bielefeld.de/record/2932984
Zitieren
Cazzamalli S, Figueras Agustí E, Petho L, et al. In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas. ACS Omega. 2018;3(11):14726-14731.
Cazzamalli, S., Figueras Agustí, E., Petho, L., Borbély, A. N., Steinkuhler, C., Neri, D., & Sewald, N. (2018). In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas. ACS Omega, 3(11), 14726-14731. https://doi.org/10.1021/acsomega.8b02350
Cazzamalli, Samuele, Figueras Agustí, Eduard, Petho, Lilla, Borbély, Adina Noémi, Steinkuhler, Christian, Neri, Dario, and Sewald, Norbert. 2018. “In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas”. ACS Omega 3 (11): 14726-14731.
Cazzamalli, S., Figueras Agustí, E., Petho, L., Borbély, A. N., Steinkuhler, C., Neri, D., and Sewald, N. (2018). In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas. ACS Omega 3, 14726-14731.
Cazzamalli, S., et al., 2018. In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas. ACS Omega, 3(11), p 14726-14731.
S. Cazzamalli, et al., “In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas”, ACS Omega, vol. 3, 2018, pp. 14726-14731.
Cazzamalli, S., Figueras Agustí, E., Petho, L., Borbély, A.N., Steinkuhler, C., Neri, D., Sewald, N.: In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas. ACS Omega. 3, 14726-14731 (2018).
Cazzamalli, Samuele, Figueras Agustí, Eduard, Petho, Lilla, Borbély, Adina Noémi, Steinkuhler, Christian, Neri, Dario, and Sewald, Norbert. “In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas”. ACS Omega 3.11 (2018): 14726-14731.
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Daten bereitgestellt von European Bioinformatics Institute (EBI)
3 Zitationen in Europe PMC
Daten bereitgestellt von Europe PubMed Central.
Synthesis and Biological Evaluation of RGD⁻Cryptophycin Conjugates for Targeted Drug Delivery.
Borbély A, Figueras E, Martins A, Esposito S, Auciello G, Monteagudo E, Di Marco A, Summa V, Cordella P, Perego R, Kemker I, Frese M, Gallinari P, Steinkühler C, Sewald N., Pharmaceutics 11(4), 2019
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Borbély A, Figueras E, Martins A, Esposito S, Auciello G, Monteagudo E, Di Marco A, Summa V, Cordella P, Perego R, Kemker I, Frese M, Gallinari P, Steinkühler C, Sewald N., Pharmaceutics 11(4), 2019
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Octreotide Conjugates for Tumor Targeting and Imaging.
Figueras E, Martins A, Borbély A, Le Joncour V, Cordella P, Perego R, Modena D, Pagani P, Esposito S, Auciello G, Frese M, Gallinari P, Laakkonen P, Steinkühler C, Sewald N., Pharmaceutics 11(5), 2019
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Figueras E, Borbely A, Ismail M, Frese M, Sewald N., Beilstein J Org Chem 14(), 2018
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Krall N, Pretto F, Decurtins W, Bernardes GJ, Supuran CT, Neri D., Angew. Chem. Int. Ed. Engl. 53(16), 2014
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Krall N, Pretto F, Decurtins W, Bernardes GJ, Supuran CT, Neri D., Angew. Chem. Int. Ed. Engl. 53(16), 2014
PMID: 24623670
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Supuran CT, Alterio V, Di Fiore A, D' Ambrosio K, Carta F, Monti SM, De Simone G., Med Res Rev 38(6), 2018
PMID: 29635752
Supuran CT, Alterio V, Di Fiore A, D' Ambrosio K, Carta F, Monti SM, De Simone G., Med Res Rev 38(6), 2018
PMID: 29635752
Protease-Cleavable Linkers Modulate the Anticancer Activity of Noninternalizing Antibody-Drug Conjugates.
Dal Corso A, Cazzamalli S, Gebleux R, Mattarella M, Neri D., Bioconjug. Chem. 28(7), 2017
PMID: 28662334
Dal Corso A, Cazzamalli S, Gebleux R, Mattarella M, Neri D., Bioconjug. Chem. 28(7), 2017
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99mTc-labeled small-molecule inhibitors of prostate-specific membrane antigen for molecular imaging of prostate cancer.
Hillier SM, Maresca KP, Lu G, Merkin RD, Marquis JC, Zimmerman CN, Eckelman WC, Joyal JL, Babich JW., J. Nucl. Med. 54(8), 2013
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A non-internalizing antibody-drug conjugate based on an anthracycline payload displays potent therapeutic activity in vivo.
Dal Corso A, Gebleux R, Murer P, Soltermann A, Neri D., J Control Release 264(), 2017
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Chemically Defined Antibody- and Small Molecule-Drug Conjugates for in Vivo Tumor Targeting Applications: A Comparative Analysis.
Cazzamalli S, Dal Corso A, Widmayer F, Neri D., J. Am. Chem. Soc. 140(5), 2018
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Cazzamalli S, Dal Corso A, Widmayer F, Neri D., J. Am. Chem. Soc. 140(5), 2018
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