TY  - CONF
AU  - Marković, Olivera S.
AU  - Konstantinović, Jelena M.
AU  - Cvijetić, Ilija 
AU  - Amézqueta, Susana
AU  - Valko, Klara
AU  - Ràfols, Clara
AU  - Polović, Natalija
AU  - Šolaja, Bogdan A.
AU  - Verbić, Tatjana
PY  - 2017
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/5959
AB  - 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.
PB  - International Association of Physical Chemists
C3  - 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
T1  - Measurements of plasma protein binding – variety of experimental techniques
SP  - 30
EP  - 30
UR  - https://hdl.handle.net/21.15107/rcub_cherry_5959
ER  - 

@conference{
author = "Marković, Olivera S. and Konstantinović, Jelena M. and Cvijetić, Ilija  and Amézqueta, Susana and Valko, Klara and Ràfols, Clara and Polović, Natalija and Šolaja, Bogdan A. and Verbić, Tatjana",
year = "2017",
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.",
publisher = "International Association of Physical Chemists",
journal = "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",
title = "Measurements of plasma protein binding – variety of experimental techniques",
pages = "30-30",
url = "https://hdl.handle.net/21.15107/rcub_cherry_5959"
}

Marković, O. S., Konstantinović, J. M., Cvijetić, I., Amézqueta, S., Valko, K., Ràfols, C., Polović, N., Šolaja, B. A.,& Verbić, T.. (2017). Measurements of plasma protein binding – variety of experimental techniques. in 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
International Association of Physical Chemists., 30-30.
https://hdl.handle.net/21.15107/rcub_cherry_5959

Marković OS, Konstantinović JM, Cvijetić I, Amézqueta S, Valko K, Ràfols C, Polović N, Šolaja BA, Verbić T. Measurements of plasma protein binding – variety of experimental techniques. in 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. 2017;:30-30.
https://hdl.handle.net/21.15107/rcub_cherry_5959 .

Marković, Olivera S., Konstantinović, Jelena M., Cvijetić, Ilija , Amézqueta, Susana, Valko, Klara, Ràfols, Clara, Polović, Natalija, Šolaja, Bogdan A., Verbić, Tatjana, "Measurements of plasma protein binding – variety of experimental techniques" in 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 (2017):30-30,
https://hdl.handle.net/21.15107/rcub_cherry_5959 .