Design, Synthesis, and Biological Evaluation of PKD Inhibitors
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-specif...
| Main Authors: | , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2011-04-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1999-4923/3/2/186/ |
| _version_ | 1811184518583812096 |
|---|---|
| author | Marie-Céline Frantz Karla Bravo-Altamirano Courtney R. LaValle Manuj Tandon Stephanie Leimgruber Elizabeth R. Sharlow John S. Lazo Q. Jane Wang Peter Wipf Kara M. George |
| author_facet | Marie-Céline Frantz Karla Bravo-Altamirano Courtney R. LaValle Manuj Tandon Stephanie Leimgruber Elizabeth R. Sharlow John S. Lazo Q. Jane Wang Peter Wipf Kara M. George |
| author_sort | Marie-Céline Frantz |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-11T13:14:33Z |
| format | Article |
| id | doaj.art-3c427ce19ca647e69b452ac7dd756d47 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-11T13:14:33Z |
| publishDate | 2011-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-3c427ce19ca647e69b452ac7dd756d472022-12-22T04:22:27ZengMDPI AGPharmaceutics1999-49232011-04-013218622810.3390/pharmaceutics3020186Design, Synthesis, and Biological Evaluation of PKD InhibitorsMarie-Céline FrantzKarla Bravo-AltamiranoCourtney R. LaValleManuj TandonStephanie LeimgruberElizabeth R. SharlowJohn S. LazoQ. Jane WangPeter WipfKara M. GeorgeProtein 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.http://www.mdpi.com/1999-4923/3/2/186/protein kinase Dsmall molecule inhibitorbenzothienothiazepinonepyrimidinesCID755673thiazepinothiophenopyrimidinone |
| spellingShingle | Marie-Céline Frantz Karla Bravo-Altamirano Courtney R. LaValle Manuj Tandon Stephanie Leimgruber Elizabeth R. Sharlow John S. Lazo Q. Jane Wang Peter Wipf Kara M. George Design, Synthesis, and Biological Evaluation of PKD Inhibitors Pharmaceutics protein kinase D small molecule inhibitor benzothienothiazepinone pyrimidines CID755673 thiazepinothiophenopyrimidinone |
| title | Design, Synthesis, and Biological Evaluation of PKD Inhibitors |
| title_full | Design, Synthesis, and Biological Evaluation of PKD Inhibitors |
| title_fullStr | Design, Synthesis, and Biological Evaluation of PKD Inhibitors |
| title_full_unstemmed | Design, Synthesis, and Biological Evaluation of PKD Inhibitors |
| title_short | Design, Synthesis, and Biological Evaluation of PKD Inhibitors |
| title_sort | design synthesis and biological evaluation of pkd inhibitors |
| topic | protein kinase D small molecule inhibitor benzothienothiazepinone pyrimidines CID755673 thiazepinothiophenopyrimidinone |
| url | http://www.mdpi.com/1999-4923/3/2/186/ |
| work_keys_str_mv | AT mariecelinefrantz designsynthesisandbiologicalevaluationofpkdinhibitors AT karlabravoaltamirano designsynthesisandbiologicalevaluationofpkdinhibitors AT courtneyrlavalle designsynthesisandbiologicalevaluationofpkdinhibitors AT manujtandon designsynthesisandbiologicalevaluationofpkdinhibitors AT stephanieleimgruber designsynthesisandbiologicalevaluationofpkdinhibitors AT elizabethrsharlow designsynthesisandbiologicalevaluationofpkdinhibitors AT johnslazo designsynthesisandbiologicalevaluationofpkdinhibitors AT qjanewang designsynthesisandbiologicalevaluationofpkdinhibitors AT peterwipf designsynthesisandbiologicalevaluationofpkdinhibitors AT karamgeorge designsynthesisandbiologicalevaluationofpkdinhibitors |