title: Technologies for transporter drug discovery.
abstract: Transporters represent attractive targets for drug discovery and are implicated in the pathophysiology of disorders across several therapeutic areas including asthma, cardiovascular disease, diabetes and neuroscience. However, the intrinsic mechanistic properties of transporters present significant challenges to the development of high-throughput screening methodologies. This review provides an update on potential transporter targets and evaluates the impact of available technologies to enable transporter screening, lead optimization and assessment of pharmacokinetics.
authors.affiliation: Merck Research Laboratories, Department of Ion Channels, Rahway, New Jersey 07065, USA. adam_weinglass@merck.com
authors.forename: Adam B
authors.initials: AB
authors.lastname: Weinglass
authors.forename: Maria L
authors.initials: ML
authors.lastname: Garcia
authors.forename: Gregory L
authors.initials: GL
authors.lastname: Kaczorowski
mesh_terms: D016503:Drug Delivery Systems / Q000379:methods; D055808:Drug Discovery / Q000379:methods*; D057166:High-Throughput Screening Assays / Q000379:methods; D006801:Humans; D026901:Membrane Transport Proteins / Q000187:drug effects*; D013672:Technology
chemical_list: D026901:Membrane Transport Proteins