Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor.

Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor. Research Abstract Details 

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Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor. Abstract Text:

Atli Thorarensen,Ronald W Sarver,Fang Tian,Andrea Ho,Donna L Romero,Keith R Marotti,

In this paper, we describe a fluorescent antibacterial analog, 6, with utility as a competition probe to determine affinities of other antibacterial analogs for human serum albumin (HSA). Analog 6 bound to HSA with an affinity of 400+/-100 nM and the fluorescence was environmentally sensitive. With 370 nm excitation, environmental sensitivity was indicated by a quenching of the 530 nm emission when the probe bound to HSA. Displacement of dansylsarcosine from HSA by 6 indicated it competed with compounds that bound at site II (ibuprofen binding site) on HSA. Analog 6 also shifted the NMR peaks of an HSA bound oleic acid molecule that itself was affected by compounds that bound at site II. In addition to binding at site II, 6 interacted at site I (warfarin binding site) as indicated by displacement of dansylamide and the shifting of NMR peaks of an HSA bound oleic acid molecule affected by warfarin site binding. Additional evidence for multiple site interaction was discovered when a percentage of 6 could be displaced by either ibuprofen or phenylbutazone. A competition assay was established using 6 to determine relative affinities of other antibacterial inhibitors for HSA.

Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor. Publishing Authors By Initials

A Thorarensen,RW Sarver,F Tian,A Ho,DL Romero,KR Marotti,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: protein binding research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: protein binding research

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Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 4646-9

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 27

MONTH: 05

YEAR: 2007

Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor. Keywords Mesh Terms:

KEYWORDS: Protein Binding

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor. Information

Substance Name: Anti-Bacterial Agents

Registry Number: 0

Grant and Affiliation Information for Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor.

AFFILIATION: Pharmacia Corporation, 301 Henrietta Street, Kalamazoo, MI 49001, USA. atli.thorarensen@pfizer.com

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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