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The importance of plasma protein binding in drug discovery
GL Trainor - Expert opinion on drug discovery, 2007 - Taylor & Francis
Plasma protein binding of drugs is a well-recognised phenomena, but it is only recently that
the implications for drug action in vivo have been fully appreciated. Plasma proteins, by …
the implications for drug action in vivo have been fully appreciated. Plasma proteins, by …
Rational use of plasma protein and tissue binding data in drug design: miniperspective
It is a commonly accepted assumption that only unbound drug molecules are available to
interact with their targets. Therefore, one of the objectives in drug design is to optimize the …
interact with their targets. Therefore, one of the objectives in drug design is to optimize the …
In vitro, in silico and integrated strategies for the estimation of plasma protein binding. A review
G Lambrinidis, T Vallianatou… - Advanced drug delivery …, 2015 - Elsevier
Plasma protein binding (PPB) strongly affects drug distribution and pharmacokinetic
behavior with consequences in overall pharmacological action. Extended plasma protein …
behavior with consequences in overall pharmacological action. Extended plasma protein …
Pharmacokinetic properties and in silico ADME modeling in drug discovery
The discovery and development of a new drug are time-consuming, difficult and expensive.
This complex process has evolved from classical methods into an integration of modern …
This complex process has evolved from classical methods into an integration of modern …
A structure-based model for predicting serum albumin binding
One of the many factors involved in determining the distribution and metabolism of a
compound is the strength of its binding to human serum albumin. While experimental and …
compound is the strength of its binding to human serum albumin. While experimental and …
Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2
A Moriconi, MC Cesta, MN Cervellera… - Journal of medicinal …, 2007 - ACS Publications
Chemokines CXCL8 and CXCL1 play a key role in the recruitment of neutrophils at the site
of inflammation. CXCL8 binds two membrane receptors, CXCR1 and CXCR2, whereas …
of inflammation. CXCL8 binds two membrane receptors, CXCR1 and CXCR2, whereas …
Modeling kinetics of subcellular disposition of chemicals
S Balaz - Chemical reviews, 2009 - ACS Publications
The effects of low-molecular-weight (< 1000 g/mol) chemicals on biosystems ranging from
membranes to organisms are of interest in medicinal chemistry, chemical biology …
membranes to organisms are of interest in medicinal chemistry, chemical biology …
Do we need to optimize plasma protein and tissue binding in drug discovery?
X Liu, C Chen, C ECA Hop - Current Topics in Medicinal …, 2011 - benthamdirect.com
It is a commonly accepted assumption that only unbound drug molecules are available to
interact with their targets. In order to achieve high unbound plasma drug concentration, it …
interact with their targets. In order to achieve high unbound plasma drug concentration, it …
Prediction of blood-βrain partitioning and human serum albumin binding based on COSMO-RS σ-Moments
K Wichmann, M Diedenhofen… - Journal of chemical …, 2007 - ACS Publications
Models for the prediction of blood-brain partitioning (logBB) and human serum albumin
binding (logK (HSA)) of neutral molecules were developed using the set of 5 COSMO-RS σ …
binding (logK (HSA)) of neutral molecules were developed using the set of 5 COSMO-RS σ …
In silico prediction of human serum albumin binding for drug leads
T Vallianatou, G Lambrinidis… - Expert opinion on drug …, 2013 - Taylor & Francis
Introduction: Binding of drugs to human serum albumin (HSA) strongly influences their
pharmacokinetic behavior and is associated with drug safety issues, low clearance, low …
pharmacokinetic behavior and is associated with drug safety issues, low clearance, low …