Membrane transporters in drug development

Nature reviews Drug discovery, 2010 - nature.com
Membrane transporters can be major determinants of the pharmacokinetic, safety and
efficacy profiles of drugs. This presents several key questions for drug development …

In silico repositioning of approved drugs for rare and neglected diseases

S Ekins, AJ Williams, MD Krasowski, JS Freundlich - Drug discovery today, 2011 - Elsevier
One approach to speed up drug discovery is to examine new uses for existing approved
drugs, so-called 'drug repositioning'or 'drug repurposing', which has become increasingly …

Pharmaceutical and pharmacological importance of peptide transporters

M Brandsch, I Knütter… - Journal of Pharmacy …, 2008 - Wiley Online Library
Peptide transport is currently a prominent topic in membrane research. The transport
proteins involved are under intense investigation because of their physiological importance …

Apical sodium dependent bile acid transporter (ASBT, SLC10A2): a potential prodrug target

A Balakrishnan, JE Polli - Molecular pharmaceutics, 2006 - ACS Publications
A major hurdle impeding the successful clinical development of drug candidates can be
poor intestinal permeability. Low intestinal permeability may be enhanced by a prodrug …

Clinical implications of pharmacogenomics of statin treatment

LM Mangravite, CF Thorn, RM Krauss - The pharmacogenomics journal, 2006 - nature.com
The Pharmacogenomics Journal (2006) 6, 360–374. doi: 10.1038/sj. tpj. 6500384;
published online 21 March 2006 β-hydroxy-β-methylglutaryl Coenzyme A (HMG-CoA) …

Structure–activity relationship for FDA approved drugs as inhibitors of the human sodium taurocholate cotransporting polypeptide (NTCP)

Z Dong, S Ekins, JE Polli - Molecular pharmaceutics, 2013 - ACS Publications
The hepatic bile acid uptake transporter sodium taurocholate cotransporting polypeptide
(NTCP) is less well characterized than its ileal paralog, the apical sodium dependent bile …

Transport of drugs by proton-coupled peptide transporters: pearls and pitfalls

M Brandsch - Expert opinion on drug metabolism & toxicology, 2009 - Taylor & Francis
The pharmaceutical relevance of proton-coupled peptide transporters is currently under
intense investigation in many laboratories. Studies have shown that these membrane …

Pharmacophore-based discovery of ligands for drug transporters

C Chang, S Ekins, P Bahadduri, PW Swaan - Advanced drug delivery …, 2006 - Elsevier
The ability to identify ligands for drug transporters is an important step in drug discovery and
development. It can both improve accurate profiling of lead pharmacokinetic properties and …

[图书][B] Drug delivery: fundamentals and applications

A Hillery, K Park - 2016 - taylorfrancis.com
This book provides a comprehensive introduction to advanced drug delivery and targeting,
covering their principles, current applications, and potential future developments. This …

New predictive models for blood–brain barrier permeability of drug-like molecules

S Kortagere, D Chekmarev, WJ Welsh, S Ekins - Pharmaceutical research, 2008 - Springer
Purpose The goals of the present study were to apply a generalized regression model and
support vector machine (SVM) models with Shape Signatures descriptors, to the domain of …