IN VITRO EFFECT OF THE HOMOCYSTEINE LINKER ON PROPERTIES OF CONJUGATES BETWEEN HUMAN SERUM ALBUMIN AND MONOMETHYL AURISTATIN F. / Wang, M.; Rogaleva, V.i.; Popova, T.v. et al.
In: Chemistry for Sustainable Development, Vol. 32, No. 6, 28.12.2024, p. 750-759.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - IN VITRO EFFECT OF THE HOMOCYSTEINE LINKER ON PROPERTIES OF CONJUGATES BETWEEN HUMAN SERUM ALBUMIN AND MONOMETHYL AURISTATIN F
AU - Wang, M.
AU - Rogaleva, V.i.
AU - Popova, T.v.
AU - Zakharova, O.d.
AU - Godovikova, T.s.
AU - Silnikov, V.n.
N1 - In vitro Effect of the Homocysteine Linker on Properties of Conjugates between Human Serum Albumin and Monomethyl Auristatin F / M. Wang, V. I. Rogaleva, T. V. Popova [et al.] // Chemistry for Sustainable Development. – 2024. – Vol. 32, No. 6. – P. 750-759. – DOI 10.15372/CSD2024610. The study was supported by the State Assignment for ICBFM SB RAS (Project No. 121031300042-1).
PY - 2024/12/28
Y1 - 2024/12/28
N2 - Fluorescent conjugates of human serum albumin and a maleimide derivative of monomethyl auristatin F containing the cleavable peptide linker ValCit were synthesised. Strategies included the direct attachment of the therapeutic peptide to the albumin structure and attachment through the N-trifluoroacetylhomocysteine linker. Confocal microscopy showed that the conjugate with the homocysteine linker effectively accumulated in the cytoplasm of the MCF-7 tumour cells, whereas the conjugate without the linker displayed predominant surface accumulation. In vitro studies demonstrated that the monomethyl auristatin F conjugate exhibited enhanced cytotoxicity against MCF-7 and T98G cancer cells after its attachment to albumin. The homocysteine-containing conjugate showed superior cytotoxicity compared to the conjugate without the linker despite the lower peptide load.
AB - Fluorescent conjugates of human serum albumin and a maleimide derivative of monomethyl auristatin F containing the cleavable peptide linker ValCit were synthesised. Strategies included the direct attachment of the therapeutic peptide to the albumin structure and attachment through the N-trifluoroacetylhomocysteine linker. Confocal microscopy showed that the conjugate with the homocysteine linker effectively accumulated in the cytoplasm of the MCF-7 tumour cells, whereas the conjugate without the linker displayed predominant surface accumulation. In vitro studies demonstrated that the monomethyl auristatin F conjugate exhibited enhanced cytotoxicity against MCF-7 and T98G cancer cells after its attachment to albumin. The homocysteine-containing conjugate showed superior cytotoxicity compared to the conjugate without the linker despite the lower peptide load.
KW - Сывороточный альбумин
KW - Тиолактон гомоцистеина
KW - Тераностика
KW - Противоопухолевая цитотоксичность
KW - Монометилауристатин F
UR - https://www.elibrary.ru/item.asp?id=76074326
UR - https://sibran.ru/en/journals/issue.php?ID=189413&ARTICLE_ID=189418
U2 - 10.15372/CSD2024610
DO - 10.15372/CSD2024610
M3 - Article
VL - 32
SP - 750
EP - 759
JO - Chemistry for Sustainable Development
JF - Chemistry for Sustainable Development
SN - 1817-1818
IS - 6
ER -
ID: 67763007