Drugging Membrane Protein Interactions

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...

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Bibliographic Details
Published inAnnual review of biomedical engineering Vol. 18; no. 1; pp. 51 - 76
Main Authors Yin, Hang, Flynn, Aaron D
Format Journal Article
LanguageEnglish
Published United States Annual Reviews 11.07.2016
Subjects
Animals
curvature sensing
drug discovery
Drug Discovery - methods
high-throughput screening
High-Throughput Screening Assays - methods
Humans
Membrane Proteins - drug effects
Membrane Proteins - metabolism
Molecular Targeted Therapy - methods
Protein Interaction Mapping - methods
rational design
transmembrane domains
rational design
curvature sensing
drug discovery
transmembrane domains
high-throughput screening
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Summary: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.
ISSN:1523-9829
1545-4274
DOI:10.1146/annurev-bioeng-092115-025322