TY - JOUR
T1 - Determine equilibrium dissociation constant of drug-membrane receptor affinity using the cell membrane chromatography relative standard method
AU - Ma, Weina
AU - Yang, Liu
AU - Lv, Yanni
AU - Fu, Jia
AU - Zhang, Yanmin
AU - He, Langchong
N1 - Publisher Copyright:
© 2017 Elsevier B.V.
PY - 2017/6/23
Y1 - 2017/6/23
N2 - The equilibrium dissociation constant (KD) of drug-membrane receptor affinity is the basic parameter that reflects the strength of interaction. The cell membrane chromatography (CMC) method is an effective technique to study the characteristics of drug-membrane receptor affinity. In this study, the KD value of CMC relative standard method for the determination of drug-membrane receptor affinity was established to analyze the relative KD values of drugs binding to the membrane receptors (Epidermal growth factor receptor and angiotensin II receptor). The KD values obtained by the CMC relative standard method had a strong correlation with those obtained by the frontal analysis method. Additionally, the KD values obtained by CMC relative standard method correlated with pharmacological activity of the drug being evaluated. The CMC relative standard method is a convenient and effective method to evaluate drug-membrane receptor affinity.
AB - The equilibrium dissociation constant (KD) of drug-membrane receptor affinity is the basic parameter that reflects the strength of interaction. The cell membrane chromatography (CMC) method is an effective technique to study the characteristics of drug-membrane receptor affinity. In this study, the KD value of CMC relative standard method for the determination of drug-membrane receptor affinity was established to analyze the relative KD values of drugs binding to the membrane receptors (Epidermal growth factor receptor and angiotensin II receptor). The KD values obtained by the CMC relative standard method had a strong correlation with those obtained by the frontal analysis method. Additionally, the KD values obtained by CMC relative standard method correlated with pharmacological activity of the drug being evaluated. The CMC relative standard method is a convenient and effective method to evaluate drug-membrane receptor affinity.
KW - Cell membrane chromatography
KW - Drug-membrane receptor affinity
KW - Equilibrium dissociation constant
KW - Relative standard method
UR - https://www.scopus.com/pages/publications/85019045986
U2 - 10.1016/j.chroma.2017.04.053
DO - 10.1016/j.chroma.2017.04.053
M3 - 文章
C2 - 28495080
AN - SCOPUS:85019045986
SN - 0021-9673
VL - 1503
SP - 12
EP - 20
JO - Journal of Chromatography A
JF - Journal of Chromatography A
ER -