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Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition. / Raskolupova, Valeria I; Wang, Meiling; Dymova, Maya A et al.

In: Molecules (Basel, Switzerland), Vol. 28, No. 6, 2672, 15.03.2023.

Research output: Contribution to journal › Article › peer-review

Harvard

Raskolupova, VI, Wang, M, Dymova, MA, Petrov, GO, Shchudlo, IM, Taskaev, SY, Abramova, TV, Godovikova, TS, Silnikov, VN & Popova, TV 2023, 'Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition', Molecules (Basel, Switzerland), vol. 28, no. 6, 2672. https://doi.org/10.3390/molecules28062672

APA

Raskolupova, V. I., Wang, M., Dymova, M. A., Petrov, G. O., Shchudlo, I. M., Taskaev, S. Y., Abramova, T. V., Godovikova, T. S., Silnikov, V. N., & Popova, T. V. (2023). Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition. Molecules (Basel, Switzerland), 28(6), [2672]. https://doi.org/10.3390/molecules28062672

Vancouver

Raskolupova VI, Wang M, Dymova MA, Petrov GO, Shchudlo IM, Taskaev SY et al. Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition. Molecules (Basel, Switzerland). 2023 Mar 15;28(6):2672. doi: 10.3390/molecules28062672

Author

Raskolupova, Valeria I ; Wang, Meiling ; Dymova, Maya A et al. / Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition. In: Molecules (Basel, Switzerland). 2023 ; Vol. 28, No. 6.

BibTeX

@article{06d3182fbba14259bd9947f85a55b247,
title = "Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition",
abstract = "Combination therapy is becoming an increasingly important treatment strategy because multi-drugs can maximize therapeutic effect and overcome potential mechanisms of drug resistance. A new albumin-based theranostic containing gemcitabine closo-dodecaborate analogue has been developed for combining boron neutron capture therapy (BNCT) and chemotheraphy. An exo-heterocyclic amino group of gemcitabine was used to introduce closo-dodecaborate, and a 5'-hydroxy group was used to tether maleimide moiety through an acid-labile phosphamide linker. The N-trifluoroacylated homocysteine thiolactone was used to attach the gemcitabine analogue to human serum albumin (HSA) bearing Cy5 or Cy7 fluorescent dyes. The half-maximal inhibitory concentration (IC50) of the designed theranostic relative to T98G cells was 0.47 mM with the correlation coefficient R = 0.82. BNCT experiments resulted in a decrease in the viability of T98G cells, and the survival fraction was ≈ 0.4.",
keywords = "BORON NEUTRON CAPTURE THERAPY, BORON DELIVERY AGENTS, GEMCITABINE ANALOGUE, BORONATED ALBUMIN THERANOSTIC CONJUGATE, CELL VIABILITY AND PROLIFERATION, CLONOGENIC ASSAY",
author = "Raskolupova, {Valeria I} and Meiling Wang and Dymova, {Maya A} and Petrov, {Gleb O} and Shchudlo, {Ivan M} and Taskaev, {Sergey Yu} and Abramova, {Tatyana V} and Godovikova, {Tatyana S} and Silnikov, {Vladimir N} and Popova, {Tatyana V}",
note = "Funding: This research was funded by the Russian Science Foundation (grant № 19-74-20123).",
year = "2023",
month = mar,
day = "15",
doi = "10.3390/molecules28062672",
language = "English",
volume = "28",
journal = "Molecules",
issn = "1420-3049",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "6",

}

RIS

TY - JOUR

T1 - Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition

AU - Raskolupova, Valeria I

AU - Wang, Meiling

AU - Dymova, Maya A

AU - Petrov, Gleb O

AU - Shchudlo, Ivan M

AU - Taskaev, Sergey Yu

AU - Abramova, Tatyana V

AU - Godovikova, Tatyana S

AU - Silnikov, Vladimir N

AU - Popova, Tatyana V

N1 - Funding: This research was funded by the Russian Science Foundation (grant № 19-74-20123).

PY - 2023/3/15

Y1 - 2023/3/15

N2 - Combination therapy is becoming an increasingly important treatment strategy because multi-drugs can maximize therapeutic effect and overcome potential mechanisms of drug resistance. A new albumin-based theranostic containing gemcitabine closo-dodecaborate analogue has been developed for combining boron neutron capture therapy (BNCT) and chemotheraphy. An exo-heterocyclic amino group of gemcitabine was used to introduce closo-dodecaborate, and a 5'-hydroxy group was used to tether maleimide moiety through an acid-labile phosphamide linker. The N-trifluoroacylated homocysteine thiolactone was used to attach the gemcitabine analogue to human serum albumin (HSA) bearing Cy5 or Cy7 fluorescent dyes. The half-maximal inhibitory concentration (IC50) of the designed theranostic relative to T98G cells was 0.47 mM with the correlation coefficient R = 0.82. BNCT experiments resulted in a decrease in the viability of T98G cells, and the survival fraction was ≈ 0.4.

AB - Combination therapy is becoming an increasingly important treatment strategy because multi-drugs can maximize therapeutic effect and overcome potential mechanisms of drug resistance. A new albumin-based theranostic containing gemcitabine closo-dodecaborate analogue has been developed for combining boron neutron capture therapy (BNCT) and chemotheraphy. An exo-heterocyclic amino group of gemcitabine was used to introduce closo-dodecaborate, and a 5'-hydroxy group was used to tether maleimide moiety through an acid-labile phosphamide linker. The N-trifluoroacylated homocysteine thiolactone was used to attach the gemcitabine analogue to human serum albumin (HSA) bearing Cy5 or Cy7 fluorescent dyes. The half-maximal inhibitory concentration (IC50) of the designed theranostic relative to T98G cells was 0.47 mM with the correlation coefficient R = 0.82. BNCT experiments resulted in a decrease in the viability of T98G cells, and the survival fraction was ≈ 0.4.

KW - BORON NEUTRON CAPTURE THERAPY

KW - BORON DELIVERY AGENTS

KW - GEMCITABINE ANALOGUE

KW - BORONATED ALBUMIN THERANOSTIC CONJUGATE

KW - CELL VIABILITY AND PROLIFERATION

KW - CLONOGENIC ASSAY

UR - https://www.scopus.com/record/display.uri?eid=2-s2.0-85151113824&origin=inward&txGid=45840cc3a87183778a618d3bab16989b

UR - https://elibrary.ru/item.asp?id=50498118

UR - https://www.mendeley.com/catalogue/6d44dd1b-893b-3906-b9cd-bf3bead65374/

U2 - 10.3390/molecules28062672

DO - 10.3390/molecules28062672

M3 - Article

C2 - 36985644

VL - 28

JO - Molecules

JF - Molecules

SN - 1420-3049

IS - 6

M1 - 2672

ER -

ID: 46103373