Protein kinase D inhibitors uncouple phosphorylation from activity by promoting agonist-dependent activation loop phosphorylation

Chemistry and Biology

Volumn 22, Issue 1, 2015, Pages 98-106

  Kunkel, Maya T ^a   Newton, Alexandra C ^a  

^a San Diego   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DIACYLGLYCEROL; POLYCYSTIN 2; PROTEIN KINASE B; PROTEIN KINASE D; PROTEIN SERINE THREONINE KINASE INHIBITOR; URIDINE TRIPHOSPHATE; PROTEIN BINDING; PROTEIN KINASE C; PROTEIN KINASE INHIBITOR;

ARTICLE; AUTOPHOSPHORYLATION; CARBOXY TERMINAL SEQUENCE; CONFORMATIONAL TRANSITION; COS 7 CELL LINE; DEPHOSPHORYLATION; ENZYME ACTIVITY; ENZYME PHOSPHORYLATION; FLUORESCENCE RESONANCE ENERGY TRANSFER; GOLGI MEMBRANE; IMMUNOPRECIPITATION; MEMBRANE BINDING; PRIORITY JOURNAL; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; CHLOROCEBUS AETHIOPS; COS 1 CELL LINE; DRUG EFFECTS; ENZYME ACTIVATION; ENZYME ACTIVE SITE; GENETICS; GOLGI COMPLEX; METABOLISM; PHOSPHORYLATION; TEMPERATURE;

ANIMALS; CATALYTIC DOMAIN; CERCOPITHECUS AETHIOPS; COS CELLS; DIGLYCERIDES; ENZYME ACTIVATION; GOLGI APPARATUS; PHOSPHORYLATION; PROTEIN BINDING; PROTEIN KINASE C; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-AKT; TEMPERATURE;

EID: 84921491493     PISSN: 10745521     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.chembiol.2014.11.014     Document Type: Article

References (26)

1. C.E. Antal, J.D. Violin, M.T. Kunkel, S. Skovsø, and A.C. Newton Intramolecular conformational changes optimize protein kinase C signaling Chem. Biol. 21 2014 459 469
2. C.L. Baron, and V. Malhotra Role of diacylglycerol in PKD recruitment to the TGN and protein transport to the plasma membrane Science 295 2002 325 328
3. D.C. Braun, S.H. Garfield, and P.M. Blumberg Analysis by fluorescence resonance energy transfer of the interaction between ligands and protein kinase Cdelta in the intact cell J. Biol. Chem. 280 2005 8164 8171
4. V. Calleja, S.M. Ameer-Beg, B. Vojnovic, R. Woscholski, J. Downward, and B. Larijani Monitoring conformational changes of proteins in cells by fluorescence lifetime imaging microscopy Biochem. J. 372 2003 33 40
5. A.J. Cameron, C. Escribano, A.T. Saurin, B. Kostelecky, and P.J. Parker PKC maturation is promoted by nucleotide pocket occupation independently of intrinsic kinase activity Nat. Struct. Mol. Biol. 16 2009 624 630
6. T.O. Chan, J. Zhang, U. Rodeck, J.M. Pascal, R.S. Armen, M. Spring, C.D. Dumitru, V. Myers, X. Li, J.Y. Cheung, and A.M. Feldman Resistance of Akt kinases to dephosphorylation through ATP-dependent conformational plasticity Proc. Natl. Acad. Sci. USA 108 2011 E1120 E1127
7. E.M. Dutil, and A.C. Newton Dual role of pseudosubstrate in the coordinated regulation of protein kinase C by phosphorylation and diacylglycerol J. Biol. Chem. 275 2000 10697 10701
8. L.L. Gallegos, M.T. Kunkel, and A.C. Newton Targeting protein kinase C activity reporter to discrete intracellular regions reveals spatiotemporal differences in agonist-dependent signaling J. Biol. Chem. 281 2006 30947 30956
9. T. Gao, A. Toker, and A.C. Newton The carboxyl terminus of protein kinase c provides a switch to regulate its interaction with the phosphoinositide-dependent kinase, PDK-1 J. Biol. Chem. 276 2001 19588 19596
10. C.M. Gould, C.E. Antal, G. Reyes, M.T. Kunkel, R.A. Adams, A. Ziyar, T. Riveros, and A.C. Newton Active site inhibitors protect protein kinase C from dephosphorylation and stabilize its mature form J. Biol. Chem. 286 2011 28922 28930
11. K.B. Harikumar, A.B. Kunnumakkara, N. Ochi, Z. Tong, A. Deorukhkar, B. Sung, L. Kelland, S. Jamieson, R. Sutherland, and T. Raynham A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo Mol. Cancer Ther. 9 2010 1136 1146
12. N. Hoshi, L.K. Langeberg, C.M. Gould, A.C. Newton, and J.D. Scott Interaction with AKAP79 modifies the cellular pharmacology of PKC Mol. Cell 37 2010 541 550
13. T. Iglesias, and E. Rozengurt Protein kinase D activation by mutations within its pleckstrin homology domain J. Biol. Chem. 273 1998 410 416
14. T. Iglesias, and E. Rozengurt Protein kinase D activation by deletion of its cysteine-rich motifs FEBS Lett. 454 1999 53 56
15. M.T. Kunkel, and A.C. Newton Calcium transduces plasma membrane receptor signals to produce diacylglycerol at Golgi membranes J. Biol. Chem. 285 2010 22748 22752
16. M.T. Kunkel, Q. Ni, R.Y. Tsien, J. Zhang, and A.C. Newton Spatio-temporal dynamics of protein kinase B/Akt signaling revealed by a genetically encoded fluorescent reporter J. Biol. Chem. 280 2005 5581 5587
17. M.T. Kunkel, A. Toker, R.Y. Tsien, and A.C. Newton Calcium-dependent regulation of protein kinase D revealed by a genetically encoded kinase activity reporter J. Biol. Chem. 282 2007 6733 6742
18. M.T. Kunkel, E.L. Garcia, T. Kajimoto, R.A. Hall, and A.C. Newton The protein scaffold NHERF-1 controls the amplitude and duration of localized protein kinase D activity J. Biol. Chem. 284 2009 24653 24661
19. K. Lin, J. Lin, W.I. Wu, J. Ballard, B.B. Lee, S.L. Gloor, G.P. Vigers, T.H. Morales, L.S. Friedman, N. Skelton, and B.J. Brandhuber An ATP-site on-off switch that restricts phosphatase accessibility of Akt Sci. Signal. 5 2012 ra37
20. A.C. Newton, and D.E. Koshland Jr. Protein kinase C autophosphorylates by an intrapeptide reaction J. Biol. Chem. 262 1987 10185 10188
21. T. Okuzumi, D. Fiedler, C. Zhang, D.C. Gray, B. Aizenstein, R. Hoffman, and K.M. Shokat Inhibitor hijacking of Akt activation Nat. Chem. Biol. 5 2009 484 493
22. E. Rozengurt Protein kinase D signaling: multiple biological functions in health and disease Physiology (Bethesda) 26 2011 23 33
23. E. Rozengurt, O. Rey, and R.T. Waldron Protein kinase D signaling J. Biol. Chem. 280 2005 13205 13208
24. E.R. Sharlow, K.V. Giridhar, C.R. LaValle, J. Chen, S. Leimgruber, R. Barrett, K. Bravo-Altamirano, P. Wipf, J.S. Lazo, and Q.J. Wang Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone J. Biol. Chem. 283 2008 33516 33526
25. J. Srivastava, J. Goris, S.M. Dilworth, and P.J. Parker Dephosphorylation of PKCdelta by protein phosphatase 2Ac and its inhibition by nucleotides FEBS Lett. 516 2002 265 269
26. A. Toker The biology and biochemistry of diacylglycerol signalling. Meeting on molecular advances in diacylglycerol signalling EMBO Rep. 6 2005 310 314