Research output: Contribution to journal › Article › peer-review
Biotin-decorated anti-cancer nucleotide theranostic conjugate of human serum albumin : Where the seed meets the soil? / Popova, Tatyana V.; Khan, Hamda; Chubarov, Alexey S. et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 28, No. 3, 01.02.2018, p. 260-264.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - Biotin-decorated anti-cancer nucleotide theranostic conjugate of human serum albumin
T2 - Where the seed meets the soil?
AU - Popova, Tatyana V.
AU - Khan, Hamda
AU - Chubarov, Alexey S.
AU - Lisitskiy, Vladimir A.
AU - Antonova, Natalya M.
AU - Akulov, Andrey E.
AU - Shevelev, Oleg B.
AU - Zavjalov, Evgenii L.
AU - Silnikov, Vladimir N.
AU - Ahmad, Saheem
AU - Godovikova, Tatyana S.
N1 - Publisher Copyright: © 2017 Elsevier Ltd
PY - 2018/2/1
Y1 - 2018/2/1
N2 - Human serum albumin is playing an increasing role as a drug carrier in clinical settings. Biotin molecules are often used as suitable tags in targeted anti-tumor drug delivery systems. We report on the synthesis and properties of a new multimodal theranostic conjugate based on an anti-cancer fluorinated nucleotide conjugated with a biotinylated dual-labeled albumin. Interestingly, in vitro and in vivo study revealed stronger anti-tumor activity of the non-tagged theranostic conjugate than that of the biotin-tagged conjugate, which can be explained by decreased binding of the biotin-tagged conjugate to cellular receptors. Our study sheds light on the importance of site-specific albumin modification for the design of albumin-based drugs with desirable pharmaceutical properties.
AB - Human serum albumin is playing an increasing role as a drug carrier in clinical settings. Biotin molecules are often used as suitable tags in targeted anti-tumor drug delivery systems. We report on the synthesis and properties of a new multimodal theranostic conjugate based on an anti-cancer fluorinated nucleotide conjugated with a biotinylated dual-labeled albumin. Interestingly, in vitro and in vivo study revealed stronger anti-tumor activity of the non-tagged theranostic conjugate than that of the biotin-tagged conjugate, which can be explained by decreased binding of the biotin-tagged conjugate to cellular receptors. Our study sheds light on the importance of site-specific albumin modification for the design of albumin-based drugs with desirable pharmaceutical properties.
KW - Anti-tumor activity
KW - Biotinylated albumin conjugate
KW - Dual-labeled human serum albumin
KW - Fluorescence-based molecular imaging
KW - Trifluorothymidine theranostic conjugate
KW - CELLS
KW - PERMEABILITY
KW - DRUG-DELIVERY
KW - VERSATILE PLATFORM
KW - BREAST-CANCER
KW - NANOPARTICLES
KW - FC-RECEPTOR
KW - THERAPY
KW - DEPENDENT MULTIVITAMIN TRANSPORTER
KW - EXPRESSION
KW - Biotin/chemistry
KW - Theranostic Nanomedicine
KW - Humans
KW - Structure-Activity Relationship
KW - Dose-Response Relationship, Drug
KW - Neoplasms, Experimental/drug therapy
KW - Molecular Structure
KW - Cell Proliferation/drug effects
KW - Mice, SCID
KW - Antineoplastic Agents/chemical synthesis
KW - Animals
KW - Cell Line, Tumor
KW - Mice
KW - Serum Albumin, Human/chemistry
KW - Nucleotides/chemical synthesis
KW - Drug Screening Assays, Antitumor
UR - http://www.scopus.com/inward/record.url?scp=85039789362&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2017.12.061
DO - 10.1016/j.bmcl.2017.12.061
M3 - Article
C2 - 29305188
AN - SCOPUS:85039789362
VL - 28
SP - 260
EP - 264
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 3
ER -
ID: 12080297