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.

Zeitschriftenaufsatz | Veröffentlicht | Englisch
 
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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
ISSN
2470-1343
Page URI
https://pub.uni-bielefeld.de/record/2932984

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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. doi:10.1021/acsomega.8b02350
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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