Pharmaceutical Research, volume 35, issue 11, publication number 205

Molecular Targets of the Hydrophobic Block of Pluronics in Cells: a Photo Affinity Labelling Approach

Zhirnov A 1
Nam E 2
Badun G 1
Romanyuk A 3
Ezhov A 4
Melik Nubarov N 1
Publication typeJournal Article
Publication date2018-09-06
Quartile SCImago
Q2
Quartile WOS
Q2
Impact factor3.7
ISSN07248741, 1573904X
Organic Chemistry
Pharmacology
Pharmaceutical Science
Molecular Medicine
Pharmacology (medical)
Biotechnology
Abstract
Pluronics are known as inhibitors of multidrug resistance thus making tumor cells sensitive to therapeutic doses of drugs. The purpose of our study consists in revealing molecular targets of the hydrophobic poly(propylene oxide) block of pluronics in living cells and the dependence of the polymers chemosensitizing efficiency upon targeting. A photo sensitive tracer was attached to the hydrophobic poly(propylene oxide) block of 3H-labeled tert-Bu-EO-PO copolymer. The conjugate was used for treatment cells in culture. We searched for its complexes with cellular lipids or proteins using RP TLC and SDS-electrophoresis, respectively. The chemosensitizing efficiency of pluronics was evaluated by their least concentrations sufficient for MDR reversion (CMDR). The poly(propylene oxide) block inserts in the lipid core of plasma membrane. No preferential binding of the conjugate with any cellular protein, particularly P-gp, has been detected. FITC-labeled pluronic L61 bound to alcohol insoluble cellular targets did not participate in MDR reversion. CMDR values of 13 block copolymers have been determined. These values inversely correlated with the polymers affinity toward lipids and the ability to accelerate flip-flop. Insertion of the hydrophobic poly(propylene oxide) block of amphiphiles in the lipid core of plasma membrane and acceleration of flip-flop of lipids underlie the mechanism of MDR reversion.

Citations by journals

1
Colloids and Surfaces B: Biointerfaces
Colloids and Surfaces B: Biointerfaces, 1, 14.29%
Colloids and Surfaces B: Biointerfaces
1 publication, 14.29%
Polymer Science - Series C
Polymer Science - Series C, 1, 14.29%
Polymer Science - Series C
1 publication, 14.29%
Polymer Science - Series A
Polymer Science - Series A, 1, 14.29%
Polymer Science - Series A
1 publication, 14.29%
ACS Applied Polymer Materials
ACS Applied Polymer Materials, 1, 14.29%
ACS Applied Polymer Materials
1 publication, 14.29%
International Journal of Biological Macromolecules
International Journal of Biological Macromolecules, 1, 14.29%
International Journal of Biological Macromolecules
1 publication, 14.29%
Moscow University Chemistry Bulletin
Moscow University Chemistry Bulletin, 1, 14.29%
Moscow University Chemistry Bulletin
1 publication, 14.29%
1

Citations by publishers

1
2
3
Pleiades Publishing
Pleiades Publishing, 3, 42.86%
Pleiades Publishing
3 publications, 42.86%
Elsevier
Elsevier, 2, 28.57%
Elsevier
2 publications, 28.57%
American Chemical Society (ACS)
American Chemical Society (ACS), 1, 14.29%
American Chemical Society (ACS)
1 publication, 14.29%
1
2
3
  • We do not take into account publications that without a DOI.
  • Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
  • Statistics recalculated weekly.
Metrics
Share
Cite this
GOST |
Cite this
GOST Copy
Zhirnov A. et al. Molecular Targets of the Hydrophobic Block of Pluronics in Cells: a Photo Affinity Labelling Approach // Pharmaceutical Research. 2018. Vol. 35. No. 11. 205
GOST all authors (up to 50) Copy
Zhirnov A., Nam E., Badun G., Romanyuk A., Ezhov A., Melik Nubarov N., Grozdova I. D. Molecular Targets of the Hydrophobic Block of Pluronics in Cells: a Photo Affinity Labelling Approach // Pharmaceutical Research. 2018. Vol. 35. No. 11. 205
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1007/s11095-018-2484-4
UR - https://doi.org/10.1007%2Fs11095-018-2484-4
TI - Molecular Targets of the Hydrophobic Block of Pluronics in Cells: a Photo Affinity Labelling Approach
T2 - Pharmaceutical Research
AU - Zhirnov, A
AU - Nam, E
AU - Badun, G
AU - Romanyuk, A
AU - Ezhov, A
AU - Melik Nubarov, N
AU - Grozdova, Irina D
PY - 2018
DA - 2018/09/06 00:00:00
PB - Springer Nature
IS - 11
VL - 35
SN - 0724-8741
SN - 1573-904X
ER -
BibTex
Cite this
BibTex Copy
@article{2018_Zhirnov
author = {A Zhirnov and E Nam and G Badun and A Romanyuk and A Ezhov and N Melik Nubarov and Irina D Grozdova},
title = {Molecular Targets of the Hydrophobic Block of Pluronics in Cells: a Photo Affinity Labelling Approach},
journal = {Pharmaceutical Research},
year = {2018},
volume = {35},
publisher = {Springer Nature},
month = {sep},
url = {https://doi.org/10.1007%2Fs11095-018-2484-4},
number = {11},
doi = {10.1007/s11095-018-2484-4}
}
Found error?