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Module Assembly for Designing Multivalent Mid‐Sized Inhibitors of Protein‐Protein Interactions
Author(s) -
Ohkanda Junko
Publication year - 2013
Publication title -
the chemical record
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.61
H-Index - 78
eISSN - 1528-0691
pISSN - 1527-8999
DOI - 10.1002/tcr.201300026
Subject(s) - combinatorial chemistry , nanotechnology , computational biology , target protein , protein ligand , chemistry , computer science , biochemistry , biology , materials science , gene
Developing clinically relevant synthetic agents that are capable of disrupting protein‐protein interactions ( PPIs ) is now a major goal of scientific research. In an effort to explore new methodologies that are applicable to the design of synthetic PPI inhibitors, we examined a strategy based on the assembly of small module compounds to create multivalent mid‐sized agents. This personal account describes three particular approaches based on module assembly: metal‐chelating‐based ligand assembly, covalent chemical ligation templated by a targeted protein, and bivalent inhibitor design for simultaneous targeting of the active pocket and protein surface. These strategies were shown to be useful for synthesizing minimally sized synthetic agents for targeting PPIs and may enable development of agents that are applicable to inhibition of intracellular PPIs.