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Cover Picture: Proteasome Inhibitors with Photocontrolled Activity (ChemBioChem 14/2014)
Author(s) -
Hansen Mickel J.,
Velema Willem A.,
de Bruin Gerjan,
Overkleeft Herman S.,
Szymanski Wiktor,
Feringa Ben L.
Publication year - 2014
Publication title -
chembiochem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201490048
Subject(s) - moiety , proteasome , chemistry , azobenzene , hela , stereochemistry , combinatorial chemistry , drug , cover (algebra) , biophysics , biochemistry , pharmacology , biology , in vitro , polymer , organic chemistry , mechanical engineering , engineering
The cover picture shows a schematic representation of the photocontrolled inhibition of the proteasome. The compound (left) with trans ‐azobenzene moiety, a strong inhibitor, can be isomerised by using UV light to the cis isomer (right), which is a weak inhibitor. The process is thermally and photochemically reversible and shown also to be valid in HeLa cells. For more details see the communication by W. Szymanski, B. L. Feringa et al. on p. 2053 ff. This newly developed photoswitchable inhibitor could be used for dynamic cancer phototherapy in which the drug could be selectively “turned on” at the site of the tumour. Selective targeting of a chemotherapeutic drug to the site of action could greatly reduce unwanted side‐effects and improve patient outcomes.