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How Cryo-EM Has Expanded Our Understanding of Membrane Transporters.

ABSTRACT: Over the past two decades, technological advances in membrane protein structural biology have provided insight into the molecular mechanisms that transporters use to move diverse substrates across the membrane. However, the plasticity of these proteins' ligand binding pockets, which allows them to bind a range of substrates, also poses a challenge for drug development. Here we highlight the structure, function, and transport mechanism of ATP-binding cassette/solute carrier transporters that are related to several diseases and multidrug resistance: ABCB1, ABCC1, ABCG2, SLC19A1, and SLC29A1. SIGNIFICANCE STATEMENT: ATP-binding cassette transporters and solute carriers play vital roles in clinical chemotherapeutic outcomes. This paper describes the current understanding of the structure of five pharmacologically relevant transporters and how they interact with their ligands.

SUBMITTER: Baril SA

PROVIDER: S-EPMC10353158 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature

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How Cryo-EM Has Expanded Our Understanding of Membrane Transporters.

Baril Stefanie A SA Gose Tomoka T Schuetz John D JD

Drug metabolism and disposition: the biological fate of chemicals 20230712 8

Over the past two decades, technological advances in membrane protein structural biology have provided insight into the molecular mechanisms that transporters use to move diverse substrates across the membrane. However, the plasticity of these proteins' ligand binding pockets, which allows them to bind a range of substrates, also poses a challenge for drug development. Here we highlight the structure, function, and transport mechanism of ATP-binding cassette/solute carrier transporters that are ...[more]

PMID: 37438132

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