Biochimie, volume 192, pages 63-71

Biological evaluation and spectral characterization of a novel tetracenomycin X congener

Alferova Vera A 1, 2
Osterman Ilya A 4, 7
Skvortsov Dmitry A.
Vasilyeva Lilia A 3
Sergiev Petr V. 4, 9
Publication typeJournal Article
Publication date2022-01-01
Journal: Biochimie
Quartile SCImago
Q1
Quartile WOS
Q2
Impact factor3.9
ISSN03009084, 61831638
Biochemistry
General Medicine
Abstract
The aromatic polyketide tetracenomycin X (TcmX) was recently found to be a potent inhibitor of protein synthesis; its binding site is located in a unique locus within the tunnel of the large ribosomal subunit. The distinct mode of action makes this relatively narrow class of aromatic polyketides promising for drug development in our quest to prevent the spread of drug-resistant pathogens. Here we report the isolation and structure elucidation of a novel natural tetracenomycin X congener - 6-hydroxytetraceonomycin X (6-OH-TcmX). In contrast to TcmX, 6-OH-TcmX exhibited lower antimicrobial and cytotoxic activity, but comparable in vitro protein synthesis inhibition ability. A survey on spectral properties of tetracenomycins revealed profound differences in both UV-absorption and fluorescence spectra between TcmX and 6-OH-TcmX, suggesting a significant influence of 6-hydroxylation on the tetracenomycin X chromophore. Nonetheless, characteristic spectral properties of tetracenomycins make them suitable candidates for semi-synthetic drug development (e.g., for targeted delivery, chemical biology, or cell imaging).

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Alferova V. A. et al. Biological evaluation and spectral characterization of a novel tetracenomycin X congener // Biochimie. 2022. Vol. 192. pp. 63-71.
GOST all authors (up to 50) Copy
Alferova V. A., Maviza T. P., Biryukov M. V., Zakalyukina Y. V., Lukianov D. A., Tashlitsky V. N., Osterman I. A., Skvortsov D. A., Vasilyeva L. A., Skvortsov D., Polshakov V. I., Sergiev P. V., Korshun V. A. Biological evaluation and spectral characterization of a novel tetracenomycin X congener // Biochimie. 2022. Vol. 192. pp. 63-71.
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TY - JOUR
DO - 10.1016/j.biochi.2021.09.014
UR - https://doi.org/10.1016%2Fj.biochi.2021.09.014
TI - Biological evaluation and spectral characterization of a novel tetracenomycin X congener
T2 - Biochimie
AU - Alferova, Vera A
AU - Maviza, Tinashe P
AU - Biryukov, Mikhail V
AU - Zakalyukina, Yuliya V
AU - Lukianov, Dmitrii A
AU - Tashlitsky, Vadim N.
AU - Osterman, Ilya A
AU - Skvortsov, Dmitry A.
AU - Vasilyeva, Lilia A
AU - Skvortsov, Dmitry
AU - Polshakov, Vladimir I.
AU - Sergiev, Petr V.
AU - Korshun, Vladimir A.
PY - 2022
DA - 2022/01/01 00:00:00
PB - Elsevier
SP - 63-71
VL - 192
SN - 0300-9084
SN - 6183-1638
ER -
BibTex
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BibTex Copy
@article{2022_Alferova,
author = {Vera A Alferova and Tinashe P Maviza and Mikhail V Biryukov and Yuliya V Zakalyukina and Dmitrii A Lukianov and Vadim N. Tashlitsky and Ilya A Osterman and Dmitry A. Skvortsov and Lilia A Vasilyeva and Dmitry Skvortsov and Vladimir I. Polshakov and Petr V. Sergiev and Vladimir A. Korshun},
title = {Biological evaluation and spectral characterization of a novel tetracenomycin X congener},
journal = {Biochimie},
year = {2022},
volume = {192},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016%2Fj.biochi.2021.09.014},
pages = {63--71},
doi = {10.1016/j.biochi.2021.09.014}
}
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