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.
How to Cite this Article |
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 |