title: Small Molecule and Peptide Recognition of Protein Transmembrane Domains.
abstract: Membrane proteins play vital roles in cell signaling, molecular transportation, and cell adhesion. The interactions of transmembrane domains are much less well understood than those of their water-soluble counterparts, and they have been deemed "undruggable" despite their important biological functions such as protein anchoring, signal transduction, and ligand recognition. Nevertheless, continual developments in this area have revealed useful probes for investigating and regulating these membrane proteins. This review summarizes and evaluates the strategies available for discovering small molecules and peptides that recognize the protein transmembrane domains of membrane proteins, with a particular focus on rational design and library screening.
authors.affiliation: Center of Basic Molecular Science, Department of Chemistry, Tsinghua University , Beijing 100082, China.
authors.forename: Xianfeng
authors.initials: X
authors.lastname: Zeng
authors.affiliation: Center of Basic Molecular Science, Department of Chemistry, Tsinghua University , Beijing 100082, China.
authors.forename: Peiyao
authors.initials: P
authors.lastname: Wu
authors.affiliation: Center of Basic Molecular Science, Department of Chemistry, Tsinghua University , Beijing 100082, China.
authors.forename: Chengbo
authors.initials: C
authors.lastname: Yao
authors.affiliation: Center of Basic Molecular Science, Department of Chemistry, Tsinghua University , Beijing 100082, China.
authors.forename: Jiaqi
authors.initials: J
authors.lastname: Liang
authors.affiliation: Center of Basic Molecular Science, Department of Chemistry, Tsinghua University , Beijing 100082, China.|School of Chemistry and Chemical Engineering, Henan Normal University , Xinxiang 453007, China.
authors.forename: Shuting
authors.initials: S
authors.lastname: Zhang
authors.affiliation: Center of Basic Molecular Science, Department of Chemistry, Tsinghua University , Beijing 100082, China.
authors.forename: Hang
authors.identifier: 0000-0002-9762-4818
authors.initials: H
authors.lastname: Yin
mesh_terms: D001665:Binding Sites; D045744:Cell Line, Tumor; D006801:Humans; D008297:Male; D008565:Membrane Proteins / Q000378:metabolism*; D010455:Peptides / Q000378:metabolism*; D011485:Protein Binding
chemical_list: D008565:Membrane Proteins; D010455:Peptides