PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment
Abstract
Elena Iurova, Ivan Beloblov, Evgenii Beloborodov, Eugenia Rastorgueva, Evgenia Pogodina, Elizaveta Tazintseva, Aleksandr Fomin.
Purpose: A comparative study of the efficiency of binding in vitro and in vivo with prostate cancer cells of artificial peptides based on U5-scytotoxin-Sth1a toxin with an inserted peptide tropic to the prostate-specific membrane antigen and the radiopharmaceutical 177Lu-PSMA-617 is carried out.
Objective and Methods: The stability of peptides, toxicity, efficiency of binding to LNCaP, PC3 and CHO-K cells, as well as the biodistribution in a BALB/c mice model with inoculated prostate adenocarcinoma cells are studied using radiometric methods (radio-HPLC, TLC, scintillator radiometer).
Results: Our results show that the synthesized DOTA-Knot/C0-C1, DOTA-Knot/C1-C2 and DOTA-Knot/C2-C3 peptides containing the GTIQPYPFSWGY sequence inserted into U5-Sth1a knottin are more stable in blood plasma and saline and also show a similar degree of binding compared with the 177Lu-PSMA-617 radiopharmaceutical. Biodistribution studies of 177Lu-PSMA-617, 177Lu-DOTA-Knot/C0-C1, 177Lu-DOTA-Knot/C1-C2 and 177Lu-DOTA-Knot/C2-C3 in prostate adenocarcinoma-bearing BALB/c mice demonstrate that, for peptide 177Lu-DOTA-Knot/C1-C2, the tumor binding index is 20.4% ID/g, while for the radiopharmaceutical 177Lu-PSMA-617, it is 11.9% ID/g.
Conclusion: Thus, the modified peptides with a peptide tropic to the PSMA antigen inserted into the structure of U5-Sth1a toxin demonstrate the greatest stability, both in saline and in blood plasma, and good binding both to cell cultures and to tumors in the body.
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| Pubmed Style Iurova E, Beloblov I, Beloborodov E, Rastorgueva E, Pogodina E, Tazintseva E, Fomin A. PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment. SRP. 2020; 11(9): 187-194. doi:10.31838/srp.2020.9.31 Web Style Iurova E, Beloblov I, Beloborodov E, Rastorgueva E, Pogodina E, Tazintseva E, Fomin A. PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment. http://www.sysrevpharm.org/?mno=4119 [Access: March 29, 2021]. doi:10.31838/srp.2020.9.31 AMA (American Medical Association) Style Iurova E, Beloblov I, Beloborodov E, Rastorgueva E, Pogodina E, Tazintseva E, Fomin A. PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment. SRP. 2020; 11(9): 187-194. doi:10.31838/srp.2020.9.31 Vancouver/ICMJE Style Iurova E, Beloblov I, Beloborodov E, Rastorgueva E, Pogodina E, Tazintseva E, Fomin A. PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment. SRP. (2020), [cited March 29, 2021]; 11(9): 187-194. doi:10.31838/srp.2020.9.31 Harvard Style Iurova, E., Beloblov, . I., Beloborodov, . E., Rastorgueva, . E., Pogodina, . E., Tazintseva, . E. & Fomin, . A. (2020) PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment. SRP, 11 (9), 187-194. doi:10.31838/srp.2020.9.31 Turabian Style Iurova, Elena, Ivan Beloblov, Evgenii Beloborodov, Eugenia Rastorgueva, Evgenia Pogodina, Elizaveta Tazintseva, and Aleksandr Fomin. 2020. PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment. Systematic Reviews in Pharmacy, 11 (9), 187-194. doi:10.31838/srp.2020.9.31 Chicago Style Iurova, Elena, Ivan Beloblov, Evgenii Beloborodov, Eugenia Rastorgueva, Evgenia Pogodina, Elizaveta Tazintseva, and Aleksandr Fomin. "PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment." Systematic Reviews in Pharmacy 11 (2020), 187-194. doi:10.31838/srp.2020.9.31 MLA (The Modern Language Association) Style Iurova, Elena, Ivan Beloblov, Evgenii Beloborodov, Eugenia Rastorgueva, Evgenia Pogodina, Elizaveta Tazintseva, and Aleksandr Fomin. "PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment." Systematic Reviews in Pharmacy 11.9 (2020), 187-194. Print. doi:10.31838/srp.2020.9.31 APA (American Psychological Association) Style Iurova, E., Beloblov, . I., Beloborodov, . E., Rastorgueva, . E., Pogodina, . E., Tazintseva, . E. & Fomin, . A. (2020) PSMA-Specific Peptide with Inhibitor Cystine Knot for Prostate Cancer Treatment. Systematic Reviews in Pharmacy, 11 (9), 187-194. doi:10.31838/srp.2020.9.31 |
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