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Design, synthesis, and biological evaluation of PKD inhibitors

George, KM and Frantz, MC and Bravo-Altamirano, K and la Valle, CR and Tandon, M and Leimgruber, S and Sharlow, ER and Lazo, JS and Jane Wang, Q and Wipf, P (2011) Design, synthesis, and biological evaluation of PKD inhibitors. Pharmaceutics, 3 (2). 186 - 228.

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Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to the lack of a PKD-specific inhibitor. The benzoxoloazepinolone CID755673 was recently reported as the first potent and kinase-selective inhibitor for this enzyme. For structure-activity analysis purposes, a series of analogs was prepared and their in vitro inhibitory potency evaluated. © 2011 by the authors; licensee MDPI, Basel, Switzerland.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
George, KM
Frantz, MC
Bravo-Altamirano, K
la Valle, CR
Tandon, M
Leimgruber, S
Sharlow, ER
Lazo, JS
Jane Wang, Q
Wipf, Ppwipf@pitt.eduPWIPF
Date: 1 June 2011
Date Type: Publication
Journal or Publication Title: Pharmaceutics
Volume: 3
Number: 2
Page Range: 186 - 228
DOI or Unique Handle: 10.3390/pharmaceutics3020186
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
PubMed Central ID: PMC3261798
PubMed ID: 22267986
Date Deposited: 31 Jul 2014 20:47
Last Modified: 04 Feb 2019 15:57


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