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Structural investigation of protein kinase C inhibitorsThe phospholipid and Ca2+ dependent protein kinase (PKC) plays an essential role in a variety of cellular events. Inhibition of PKC was shown to arrest growth in tumor cell cultures making it a target for possible antitumor therapy. Calphostins are potent inhibitors of PKC with high affinity for the enzyme regulatory site. Structural characteristics of calphostins, which confer the inhibitory activity, are investigated by comparing their optimized structures with the existing models for PKC activation. The resulting model of inhibitory activity assumes interaction with two out of the three electrostatic interaction sites postulated for activators. The model shows two sites of hydrophobic interaction and enables the inhibitory activity of gossypol to be accounted for.
Document ID
20040090161
Acquisition Source
Legacy CDMS
Document Type
Reprint (Version printed in journal)
Authors
Barak, D.
(Roswell Park Memorial Institute Buffalo, NY 14263, United States)
Shibata, M.
Rein, R.
Date Acquired
August 21, 2013
Publication Date
January 1, 1991
Publication Information
Publication: Journal of molecular structure
Volume: 230
ISSN: 0022-2860
Subject Category
Exobiology
Funding Number(s)
CONTRACT_GRANT: NSG-7305
Distribution Limits
Public
Copyright
Other
Keywords
NASA Discipline Exobiology
NASA Discipline Number 52-20
Non-NASA Center
NASA Program Exobiology

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