title: Transporter-mediated tissue targeting of therapeutic molecules in drug discovery.
abstract: Tissue concentrations of endogenous chemicals and nutrients are in large part regulated by membrane transporters through their substrate specificity and differential tissue distributions. These transporters also play a key role in the disposition of therapeutic agents thus affecting their efficacy and safety profile. A transporter-mediated tissue targeting strategy, where the structural features recognized by the transporters are incorporated into the therapeutic molecule, is emerging as an effective approach in drug discovery. In this digest, we review this phenomenon and highlight recent cases in the design of liver and kidney targeted drug molecules.
authors: Lilly China Research and Development Center (LCRDC), Eli Lilly and Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
authors: Jingye
authors: J
authors: Zhou
authors: Lilly China Research and Development Center (LCRDC), Eli Lilly and Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
authors: Jianfeng
authors: J
authors: Xu
authors: Lilly China Research and Development Center (LCRDC), Eli Lilly and Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
authors: Zheng
authors: Z
authors: Huang
authors: Lilly China Research and Development Center (LCRDC), Eli Lilly and Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
authors: Minmin
authors: M
authors: Wang
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D007668:Kidney / Q000378:metabolism*; D008099:Liver / Q000378:metabolism*; D026901:Membrane Transport Proteins / Q000378:metabolism*; D027361:Organic Anion Transporters / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D010599:Pharmacokinetics; D051297:Sodium-Glucose Transporter 2 / Q000378:metabolism
chemical_list: D026901:Membrane Transport Proteins; D027361:Organic Anion Transporters; D004364:Pharmaceutical Preparations; D051297:Sodium-Glucose Transporter 2
keywords: Kidney; Liver; OATP; SGLT2; Tissue targeting; Transporter