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.
Abstract
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
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Status: |
Published |
Creators/Authors: |
Creators | Email | Pitt Username | ORCID  |
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George, KM | | | | Frantz, MC | | | | Bravo-Altamirano, K | | | | la Valle, CR | | | | Tandon, M | | | | Leimgruber, S | | | | Sharlow, ER | | | | Lazo, JS | | | | Jane Wang, Q | | | | Wipf, P | pwipf@pitt.edu | PWIPF | |
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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 |
URI: |
http://d-scholarship.pitt.edu/id/eprint/22337 |
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