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Measurements of plasma protein binding – variety of experimental techniques
dc.creator | Marković, Olivera S. | |
dc.creator | Konstantinović, Jelena M. | |
dc.creator | Cvijetić, Ilija | |
dc.creator | Amézqueta, Susana | |
dc.creator | Valko, Klara | |
dc.creator | Ràfols, Clara | |
dc.creator | Polović, Natalija | |
dc.creator | Šolaja, Bogdan A. | |
dc.creator | Verbić, Tatjana | |
dc.date.accessioned | 2023-08-24T11:36:37Z | |
dc.date.available | 2023-08-24T11:36:37Z | |
dc.date.issued | 2017 | |
dc.identifier.uri | http://cherry.chem.bg.ac.rs/handle/123456789/5959 | |
dc.description.abstract | Drug molecules in vivo may be bound to proteins and lipids in plasma and/or in tissues, or free (unbound) in diffusion among the aqueous environment of the blood and tissues. Data from in vitro plasma protein binding experiments that determine the fraction of protein-bound drug are frequently used in drug discovery [1]. Human plasma proteins contain around 40 % albumin (HSA), 1-acid glycoprotein (AGP) in much lower concentration (1-3 %) and immunoglobulins [2]. Methods used for drug – plasma protein binding (PPB) studies are numerous and can be divided into two main groups: separation methods (enabling the calculation of binding parameters, i.e. the number of binding sites and their respective affinity constants) and non-separation methods (describing predominantly qualitative parameters of the ligand-protein complex) [3]. Sometimes, results of PPB measurements obtained by different techniques are not consistent. High binding affinity to plasma proteins is not necessarily a crucial limiting factor for further delivery of compound to the target organ [1]. As an example, we show the study of the interactions between HSA/AGP and an “in-house” synthesized steroidal derivative that showed remarkable inhibitory potency against BoNT/A holotoxin in mouse embryonic stem cell derived motor neurons [4]. A variety of experimental techniques (ITC, HPLC, spectrofluorimetry, FTIR, and equilibrium dialysis) were used and the results were compared highlighting the advantages and disadvatages of various techniques. | sr |
dc.language.iso | en | sr |
dc.publisher | International Association of Physical Chemists | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS// | sr |
dc.rights | openAccess | sr |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | 6th IAPC Meeting Sixth World Conference on Physico-Chemical Methods in Drug Discovery & Third World Conference on ADMET and DMPK, Zagreb, Croatia, September 4-7, 2017 | sr |
dc.title | Measurements of plasma protein binding – variety of experimental techniques | sr |
dc.type | conferenceObject | sr |
dc.rights.license | BY | sr |
dc.citation.spage | 30 | |
dc.citation.epage | 30 | |
dc.type.version | publishedVersion | sr |
dc.identifier.fulltext | http://cherry.chem.bg.ac.rs/bitstream/id/32750/bitstream_32750.pdf | |
dc.identifier.rcub | https://hdl.handle.net/21.15107/rcub_cherry_5959 |