Autoren:	Wenskowsky, Lea Wagner, Michael Reusch, Johannes Schreuder, Herman Matter, Hans Opatz, Till Petry, Stefan Matthias
Titel:	Resolving binding events on the multifunctional human serum albumin
Online-Publikationsdatum:	9-Aug-2021
Erscheinungsdatum:	2020
Sprache des Dokuments:	Englisch
Zusammenfassung/Abstract:	Physiological processes rely on initial recognition events between cellular components and other molecules or modalities. Biomolecules can have multiple sites or mode of interaction with other molecular entities, so that a resolution of the individual binding events in terms of spatial localization as well as association and dissociation kinetics is required for a meaningful description. Here we describe a trichromatic fluorescent binding- and displacement assay for simultaneous monitoring of three individual binding sites in the important transporter and binding protein human serum albumin. Independent investigations of binding events by X-ray crystallography and time-resolved dynamics measurements (switchSENSE technology) confirm the validity of the assay, the localization of binding sites and furthermore reveal conformational changes associated with ligand binding. The described assay system allows for the detailed characterization of albumin-binding drugs and is therefore well-suited for prediction of drug-drug and drug-food interactions. Moreover, conformational changes, usually associated with binding events, can also be analyzed.
DDC-Sachgruppe:	540 Chemie 540 Chemistry and allied sciences
Veröffentlichende Institution:	Johannes Gutenberg-Universität Mainz
Organisationseinheit:	FB 09 Chemie, Pharmazie u. Geowissensch.
Veröffentlichungsort:	Mainz
ROR:	https://ror.org/023b0x485
DOI:	http://doi.org/10.25358/openscience-6256
Version:	Published version
Publikationstyp:	Zeitschriftenaufsatz
Nutzungsrechte:	CC BY-NC-ND
Informationen zu den Nutzungsrechten:	https://creativecommons.org/licenses/by-nc-nd/4.0/
Zeitschrift:	ChemMedChem 15 9
Seitenzahl oder Artikelnummer:	738 743
Verlag:	Wiley-VCH
Verlagsort:	Weinheim u.a.
Erscheinungsdatum:	2020
ISSN:	1860-7187
URL der Originalveröffentlichung:	https://doi.org/10.1002/cmdc.202000069
DOI der Originalveröffentlichung:	10.1002/cmdc.202000069
Enthalten in den Sammlungen:	JGU-Publikationen