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HR22C16: A Potent Small‐Molecule Probe for the Dynamics of Cell Division
Author(s) -
Hotha Srinivas,
Yarrow Justin C.,
Yang Janet G.,
Garrett Sarah,
Renduchintala Kishore V.,
Mayer Thomas U.,
Kapoor Tarun M.
Publication year - 2003
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200351173
Subject(s) - division (mathematics) , small molecule , mitosis , function (biology) , computational biology , cell division , solid phase synthesis , throughput , block (permutation group theory) , computer science , combinatorial chemistry , nanotechnology , chemistry , biology , cell , biological system , information retrieval , microbiology and biotechnology , biochemistry , materials science , peptide , arithmetic , telecommunications , mathematics , geometry , wireless
A high‐throughput, microscopy‐based chemical‐genetic screen identified HR22C16, which causes a monoastral mitotic block, as a small‐molecule probe for cell division (see picture). By using a diastereoselective, traceless solid‐phase synthesis and biological assays, a more potent HR22C16 analogue was then identified. A photocaging strategy for HR22C16 was also developed to allow fast temporal control over the function of the target protein Eg5.