Membrane transporters can be major determinants of the pharmacokinetic, safety and
efficacy profiles of drugs. This presents several key questions for drug development …

Resistance to conventional and target specific antitumor drugs still remains one of the major
cause of treatment failure and patience death. This condition often involves ATP-binding …

With the discovery of P-glycoprotein (P-gp), it became evident that ABC-transporters play a
vital role in bioavailability and toxicity of drugs. They prevent intracellular accumulation of …

Computational (in silico) methods have been developed and widely applied to
pharmacology hypothesis development and testing. These in silico methods include …

The human solute carrier (SLC) transporters are important targets for drug development.
Structure-based drug discovery for SLC transporters requires the description of their …

In the absence of three-dimensional (3D) structures of potential drug targets, ligand-based
drug design is one of the popular approaches for drug discovery and lead optimization. 3D …

Nine proteins of the ABC superfamily (P-glycoprotein, 7 MRPs and BCRP) are involved in
multidrug transport. Being localised at the surface of endothelial or epithelial cells, they …

Develo** a novel drug is a complex, risky, expensive and time-consuming venture. It is
estimated that the conventional drug discovery process ending with a new medicine ready …

Lapatinib [N-{3-chloro-4-[(3-fluorobenzyl) oxy] phenyl}-6-[5-({[2-(methylsulfonyl) ethyl]
amino} methyl)-2-furyl]-4-quinazolinamine, GW572016, Tykerb] is a tyrosine kinase inhibitor …

We have recently identified a new class of compounds that selectively kill cells that express
P-glycoprotein (P-gp, MDR1), the ATPase efflux pump that confers multidrug resistance on …