Abstract
The Organic Anion Transporters (OATs) are a family of important membrane proteins responsible for the absorption, distribution and excretion of a wide range of substances, including many clinically important drugs.Therefore, the function of OATs is the key determinant of drug response in human. Human genetic polymorphisms often result in the functional alternation of OATs, which in consequence, leads to the interpatient variation of therapies. In this review, we summarize the current findings about OATs, with a focus on the genetic polymorphisms and their influence on transporter function and drug performance, the information of which is critical in elucidating the essential roles of OATs played in body, as well as forming the basis of future therapeutic optimization in individuals.
Highlights
Interpatient variation of drug response becomes a critical issue in rational pharmacotherapy [1,2]
Genetic mutations have been widely recognized in Organic Anion Transporters (OAT), which could result in altering the protein sequence, or regulating the transcription of these genes
Functional analysis of the OAT polymorphisms revealed that the natural mutations may dampen or even eliminate the transporter activity in total
Summary
Interpatient variation of drug response becomes a critical issue in rational pharmacotherapy [1,2]. It is known that drug-metabolizing enzymes and influx/efflux transporters are responsible for the Absorption, Distribution, Metabolism and Elimination (ADME) of drugs in the body, the function of these genes are the key determinants of therapeutic outcomes in individuals [1,2,3,4,5]. The Solute Carrier Transporters (SLCs) are a superfamily of membrane proteins, responsible for the cellular influx of various substances, including many clinically important drugs. Genetic variations often lead to functional alternation of these proteins; naturally occurred polymorphisms of OATs have been widely explored in the last decade, so as to elucidate the variable response of drugs in human
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