Protein Information

Name P glycoprotein
Synonyms ABC20; MDR1; ABCB 1; ABCB1; ATP binding cassette sub family B member 1; CD243; CD243 antigen; CLCS…

Compound Information

Name ethylene oxide
CAS oxirane

Reference List

PubMed Abstract RScore(About this table)
18380467 Zastre JA, Jackson JK, Wong W, Burt HM: P-glycoprotein efflux inhibition by amphiphilic diblock copolymers: relationship between copolymer concentration and substrate hydrophobicity. Mol Pharm. 2008 Jul-Aug;5(4):643-53. Epub 2008 Apr 2.

7(0,0,0,7) Details
15751981 Demina T, Grozdova I, Krylova O, Zhirnov A, Istratov V, Frey H, Kautz H, Melik-Nubarov N: Relationship between the structure of amphiphilic copolymers and their ability to disturb lipid bilayers. Biochemistry. 2005 Mar 15;44(10):4042-54.

Nonionic amphiphiles and particularly block copolymers of ethylene oxide and propylene oxide (Pluronics) cause pronounced chemosensitization of tumor cells that exhibit multiple resistance to antineoplastic drugs.
This effect is due to inhibition of P-glycoprotein (P-gp) responsible for drug efflux.
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18838158 Xiong XB, Uludag H, Lavasanifar A: Biodegradable amphiphilic poly (ethylene oxide)-block-polyesters with grafted polyamines as supramolecular nanocarriers for efficient siRNA delivery. Biomaterials. 2009 Jan;30(2):242-53. Epub 2008 Oct 5.

Based on flow cytometry and confocal microscopy, siRNA formulated in PEO-b-P (CL-g-SP) and PEO-b-P (CL-g-TP) micelles showed efficient cellular uptake through endocytosis by MDA435/LCC6 cells transfected with MDR-1, which encodes for the expression of P-glycoprotein (P-gp).
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18588278 Sommer K, Kaiser S, Krylova OO, Kressler J, Pohl P, Busse K: Influence of amphiphilic block copolymer induced changes in membrane ion conductance on the reversal of multidrug resistance. J Med Chem. 2008 Jul 24;51(14):4253-9. Epub 2008 Jun 28.

The drug efflux system's direct and indirect inhibition mediated by polymer P-glycoprotein (Pgp) interactions or adenosine triphosphate (ATP) depletion, respectively, may be involved in MDR reversal as well as damage to the membrane barrier caused by polymer insertion into the membrane.
Therefore, a new triblock copolymer (poly (ethylene oxide)- block-poly (hexafluoropropylene oxide)- block-poly (ethylene oxide)) was designed and synthesized by combined polymerization and polymer analogous reaction.
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19818492 Xiong XB, Ma Z, Lai R, Lavasanifar A: The therapeutic response to multifunctional polymeric nano-conjugates in the targeted cellular and subcellular delivery of doxorubicin. Biomaterials. 2010 Feb;31(4):757-68. Epub 2009 Oct 8.

Towards this goal, two polymeric DOX nano-conjugates were developed, for which the design was based on the use of multi-functionalized poly (ethylene oxide)-block-poly (epsilon-caprolactone) (PEO-b-PCL) micelles decorated with alphavbeta3 integrin-targeting ligand (i.e.
The pH-triggered drug release, cellular uptake, intracellular distribution, and cytotoxicity against MDA-435/LCC6 (WT) (a DOX-sensitive cancer cell line) and MDA-435/LCC6 (MDR) (a DOX-resistant clone expressing a high level of P-glycoprotein) were evaluated.
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18325619 Bromberg L: Polymeric micelles in oral chemotherapy. J Control Release. 2008 Jun 4;128(2):99-112. Epub 2008 Feb 11.

High surface activity of the Pluronic-PAA copolymers in water results in interactions with cell membranes and suppression of the membrane pumps such as P-glycoprotein.
A family of block-graft copolymers of the poly (ethylene oxide) (PEO) and poly (propylene oxide) (PPO) Pluronic (R) polyethers and poly (acrylic acid) (PAA) bound by carbon-carbon bonds emerged, wherein both polymeric components are generally recognized as safe.
1(0,0,0,1) Details
15035640 Krylova OO, Pohl P: Ionophoric activity of pluronic block copolymers. Biochemistry. 2004 Mar 30;43(12):3696-703.

Pluronic block copolymers (triblock copolymers of poly (ethylene oxide) and poly (propylene oxide)) exhibit a chemosensitizing effect on multidrug resistant cell lines.
Changes in membrane permeability are hypothesized to be responsible because inhibition of drug transport mediated by both the multidrug-resistance-associated protein and the P-glycoprotein drug efflux system has been observed.
1(0,0,0,1) Details