The SLC36 family of proton-coupled amino acid transporters and their potential role in drug transport.

摘要: Members of the solute carrier (SLC) 36 family are involved in transmembrane movement amino acids and derivatives. SLC36 consists four members. SLC36A1 SLC36A2 both function as H+-coupled acid symporters. is expressed at luminal surface small intestine but also commonly found lysosomes many cell types (including neurones), suggesting that it a multipurpose with distinct roles different cells including absorption an efflux pathway following intralysosomal protein breakdown. has relatively low affinity (Km 1–10 mM) for its substrates, which include zwitterionic imino acids, heterocyclic acid-based drugs derivatives used experimentally and/or clinically to treat epilepsy, schizophrenia, bacterial infections, hyperglycaemia cancer. apical human renal proximal tubule where functions reabsorption glycine, proline hydroxyproline. transports narrower substrate selectivity higher 0.1–0.7 than SLC36A1. Mutations lead hyperglycinuria iminoglycinuria. SLC36A3 only testes orphan transporter no known function. SLC36A4 widely distributed mRNA level high-affinity 2–3 µM) tryptophan. We have much learn about this transporters, from current knowledge, seems likely their will influence pharmacokinetic profiles by mediating transport kidney. LINKED ARTICLES This article part themed section on Transporters. To view other articles visit http://dx.doi.org/10.1111/bph.2011.164.issue-7