title: Drugging Membrane Protein Interactions.
abstract: The majority of therapeutics target membrane proteins, accessible on the surface of cells, to alter cellular signaling. Cells use membrane proteins to transduce signals into cells, transport ions and molecules, bind cells to a surface or substrate, and catalyze reactions. Newly devised technologies allow us to drug conventionally "undruggable" regions of membrane proteins, enabling modulation of protein-protein, protein-lipid, and protein-nucleic acid interactions. In this review, we survey the state of the art of high-throughput screening and rational design in drug discovery, and we evaluate the advances in biological understanding and technological capacity that will drive pharmacotherapy forward against unorthodox membrane protein targets.
authors: Department of Chemistry and Biochemistry.|BioFrontiers Institute, and.|Center of Basic Molecular Science, Department of Chemistry, Tsinghua University, Beijing 100082, China.
authors: Hang
authors: H
authors: Yin
authors: BioFrontiers Institute, and.|Department of Molecular, Cellular, and Developmental Biology, University of Colorado, Boulder, Colorado 80309; email: Hubert.Yin@colorado.edu , Aaron.Flynn@colorado.edu.
authors: Aaron D
authors: AD
authors: Flynn
mesh_terms: D000818:Animals; D055808:Drug Discovery / Q000379:methods*; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D008565:Membrane Proteins / Q000187:drug effects* / Q000378:metabolism*; D058990:Molecular Targeted Therapy / Q000379:methods*; D025941:Protein Interaction Mapping / Q000379:methods*
chemical_list: D008565:Membrane Proteins
keywords: curvature sensing; drug discovery; high-throughput screening; rational design; transmembrane domains