Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery.

Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery. Research Abstract Details 

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Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery. Abstract Text:

Olga V Trubetskoy,Moshe Finel,Thomas J Burke,Vladimir S Trubetskoy,

PURPOSE: Polymeric micelles have been used for solubilization of insoluble drugs and as carriers for drug delivery applications. Here we evaluated an application of the synthetic polymeric micelles in experiments designed to improve the handling and stability of membrane proteins targets. METHODS: Particle sizing by dynamic light scattering was performed in a Zeta Plus Photon Correlation Spectrometer at 532 nm. UGT1A1 activity has been measured in fluorescent assay using scopoletin as a substrate. COX-2 activity has been measured in a fluorescent assay using Amplex Red. Fluorescence Resonance Energy Transfer (FRET) was monitored using either 463 nm excitation wavelength (the emission range 500-600 nm) or 395 nm excitation wavelength (the emission range 500-600 nm). RESULTS: Incorporation of membrane proteins into PreserveX-QML polymeric micelles resulted in improved homogeneity and stability of the preparation and in reduced light scattering. Stabilization of the biological activity of micelle-incorporated membrane proteins, such as the human UGT1A1 and COX-2 both during extended incubations at room temperature and during multiple freeze/thaw cycles, has been achieved. CONCLUSION: PreserveX-QML polymeric micelles help to homogenize and disperse membrane proteins preparations and stabilize the biological activity of the proteins making it more suitable for pharmaceutical assays and applications.

Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery. Publishing Authors By Initials

OV Trubetskoy,M Finel,TJ Burke,VS Trubetskoy,

For similar investigative techniques: technology, pharmaceutical research abstracts see: investigative techniques: technology, pharmaceutical research

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Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Journal of pharmacy & pharmaceutical sciences : a

VOLUME: 9

Page Numbers: 271-80

Journal Abbreviation:

ISSN: 1482-1826

DAY: 3

MONTH: 12

YEAR: 2006

Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9807281

Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery. Keywords Mesh Terms:

KEYWORDS: Technology, Pharmaceutical

MESH TERMS: methods

Chemical & Substance for Abstract: Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery. Information

Substance Name: Polymers

Registry Number: 0

Grant and Affiliation Information for Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery.

AFFILIATION: Quintessence Biosciences, Inc., Madison, WI 53719, USA.

Country: Canada

AGENCY: United States NINDS

GRANT: 1R21NS053707-01

ACRONYM: NS

MEDLINETA: J Pharm Pharm Sci

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