Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic

Cancer Research

Volumn 68, Issue 18, 2008, Pages 7475-7483

  Sherk, Andrea B ^a   Frigo, Daniel E ^a   Schnackenberg, Christine G ^b   Bray, Jeffrey D ^b   Laping, Nicholas J ^b   Trizna, Walter ^b   Hammond, Marlys ^b   Patterson, Jaclyn R ^b   Thompson, Scott K ^b   Kazmin, Dmitri ^a   Norris, John D ^a   McDonnell, Donald P ^a,c  

^a DUKE UNIVERSITY MEDICAL CENTER   (United States)

^b GLAXOSMITHKLINE   (United States)

^c DUKE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANDROGEN; CASPASE 2; ENZYME INHIBITOR; GSK 650394; SERUM AND GLUCOCORTICOID REGULATED KINASE 1; SMALL INTERFERING RNA; UBIQUITIN PROTEIN LIGASE NEDD4; UNCLASSIFIED DRUG;

ARTICLE; CANCER GROWTH; CELL STRAIN LNCAP; CONTROLLED STUDY; DRUG STRUCTURE; ENZYME ACTIVITY; FLUORESCENCE POLARIZATION; GENE; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; IMMUNOBLOTTING; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN PHOSPHORYLATION; PROTEIN TARGETING; RNA INTERFERENCE; SGK1 GENE;

BENZOIC ACIDS; BICYCLO COMPOUNDS, HETEROCYCLIC; CELL GROWTH PROCESSES; CELL LINE, TUMOR; HELA CELLS; HUMANS; IMMEDIATE-EARLY PROTEINS; MALE; METRIBOLONE; PROSTATIC NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; RECEPTORS, ANDROGEN; RNA, MESSENGER; RNA, SMALL INTERFERING; UP-REGULATION;

EID: 54749127362     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: 10.1158/0008-5472.CAN-08-1047     Document Type: Article

References (40)

1. Cancer facts and figures. American Cancer Society; 2007.
2. Bolla M, Collette L, Blank L, et al. Long-term results with immediate androgen suppression and external irradiation in patients with locally advanced prostate cancer (an EORTC study): a phase III randomised trial. Lancet 2002;360:103-6.
3. Lawton CA, Winter K, Murray K, et al. Updated results of the phase III Radiation Therapy Oncology Group (RTOG) trial 85-31 evaluating the potential benefit of androgen suppression following standard radiation therapy for unfavorable prognosis carcinoma of the prostate. Int J Radiat Oncol Biol Phys 2001;49:937-46.
4. Holzbeierlein J, Lal P, LaTulippe E, et al. Gene expression analysis of human prostate carcinoma during hormonal therapy identifies androgen-responsive genes and mechanisms of therapy resistance. Am J Pathol 2004;164:217-27.
5. Kazmin D, Prytkova T, Cook CE, et al. Linking ligand-induced alterations in androgen receptor structure to differential gene expression: a first step in the rational design of selective androgen receptor modulators. Mol Endocrinol 2006;20:1201-17.
6. Shanmugam I, Cheng G, Terranova PF, Thrasher JB, Thomas CP, Li B. Serum/glucocorticoid-induced protein kinase-1 facilitates androgen receptor-dependent cell survival. Cell Death Differ 2007;14:2085-94.
7. Xu Y, Chen SY, Ross KN, Balk SP. Androgens induce prostate cancer cell proliferation through mammalian target of rapamycin activation and post-transcriptional increases in cyclin D proteins. Cancer Res 2006;66:7783-92.
8. Alliston TN, Maiyar AC, Buse P, Firestone GL, Richards JS. Follicle stimulating hormone-regulated expression of serum/glucocorticoid-inducible kinase in rat ovarian granulosa cells: a functional role for the Sp1 family in promoter activity. Mol Endocrinol 1997;11:1934-49.
9. Bell LM, Leong ML, Kim B, et al. Hyperosmotic stress stimulates promoter activity and regulates cellular utilization of the serum- and glucocorticoid-inducible protein kinase (Sgk) by a p38 MAPK-dependent pathway. J Biol Chem 2000;275:25262-72.
10. Hollister RD, Page KJ, Hyman BT. Distribution of the messenger RNA for the extracellularly regulated kinases 1, 2 and 3 in rat brain: effects of excitotoxic hippocampal lesions. Neuroscience 1997;79:1111-9.
11. Imaizumi K, Tsuda M, Wanaka A, Tohyama M, Takagi T. Differential expression of sgk mRNA, a member of the Ser/Thr protein kinase gene family, in rat brain after CNS injury. Brain Res Mol Brain Res 1994;26:189-96.
12. Leong ML, Maiyar AC, Kim B, O'Keeffe BA, Firestone GL. Expression of the serum- and glucocorticoid-inducible protein kinase, Sgk, is a cell survival response to multiple types of environmental stress stimuli in mammary epithelial cells. J Biol Chem 2003;278:5871-82.
13. Maiyar AC, Phu PT, Huang AJ, Firestone GL. Repression of glucocorticoid receptor transactivation and DNA binding of a glucocorticoid response element within the serum/glucocorticoid-inducible protein kinase (sgk) gene promoter by the p53 tumor suppressor protein. Mol Endocrinol 1997;11:312-29.
14. Waldegger S, Barth P, Raber G, Lang F. Cloning and characterization of a putative human serine/threonine protein kinase transcriptionally modified during anisotonic and isotonic alterations of cell volume. Proc Natl Acad Sci U S A 1997;94:4440-5.
15. Webster MK, Goya L, Ge Y, Maiyar AC, Firestone GL. Characterization of sgk, a novel member of the serine/threonine protein kinase gene family which is transcriptionally induced by glucocorticoids and serum. Mol Cell Biol 1993;13:2031-40.
16. Biondi RM, Kieloch A, Currie RA, Deak M, Alessi DR. The PIF-binding pocket in PDK1 is essential for activation of S6K and SGK, but not PKB. EMBO J 2001;20:4380-90.
17. Collins BJ, Deak M, Arthur JS, Armit LJ, Alessi DR. In vivo role of the PIF-binding docking site of PDK1 defined by knock-in mutation. EMBO J 2003;22:4202-11.
18. Frodin M, Antal TL, Dummler BA, et al. A phosphoserine/threonine-binding pocket in AGC kinases and PDK1 mediates activation by hydrophobic motif phosphorylation. EMBO J 2002;21:5396-407.
19. Kobayashi T, Cohen P. Activation of serum- and glucocorticoid-regulated protein kinase by agonists that activate phosphatidylinositide 3-kinase is mediated by 3-phosphoinositide-dependent protein kinase-1 (PDK1) and PDK2. Biochem J 1999;339:319-28.
20. Park J, Leong ML, Buse P, Maiyar AC, Firestone GL, Hemmings BA. Serum and glucocorticoid-inducible kinase (SGK) is a target of the PI 3-kinase-stimulated signaling pathway. EMBO J 1999;18:3024-33.
21. Majumder PK, Sellers WR. Akt-regulated pathways in prostate cancer. Oncogene 2005;24:7465-74.
22. Sulis ML, Parsons R. PTEN: from pathology to biology. Trends Cell Biol 2003;13:478-83.
23. Ma X, Ziel-van der Made AC, Autar B, et al. Targeted biallelic inactivation of Pten in the mouse prostate leads to prostate cancer accompanied by increased epithelial cell proliferation but not by reduced apoptosis. Cancer Res 2005;65:5730-9.
24. Aoyama T, Matsui T, Novikov M, Park J, Hemmings B, Rosenzweig A. Serum and glucocorticoid-responsive kinase-1 regulates cardiomyocyte survival and hypertrophic response. Circulation 2005;111:1652-9.
25. Schoenebeck B, Bader V, Zhu XR, Schmitz B, Lubbert H, Stichel CC. Sgk1, a cell survival response in neurodegenerative diseases. Mol Cell Neurosci 2005;30:249-64.
26. Wu W, Chaudhuri S, Brickley DR, Pang D, Karrison T, Conzen SD. Microarray analysis reveals glucocorticoid-regulated survival genes that are associated with inhibition of apoptosis in breast epithelial cells. Cancer Res 2004;64:1757-64.
27. Zhang L, Cui R, Cheng X, Du J. Antiapoptotic effect of serum and glucocorticoid-inducible protein kinase is mediated by novel mechanism activating IκB kinase. Cancer Res 2005;65:457-64.
28. Frigo DE, McDonnell DP. Differential effects of prostate cancer therapeutics on neuroendocrine transdifferentiation. Mol Cancer Ther 2008;7:659-69.
29. Wolf DA, Schulz P, Fittler F. Transcriptional regulation of prostate kallikrein-like genes by androgen. Mol Endocrinol 1992;6:753-62.
30. Nakhoul NL, Hering-Smith KS, Gambala CT, Hamm LL. Regulation of sodium transport in M-1 cells. Am J Physiol 1998;275:F998-1007.
31. Li J, Yen C, Liaw D, et al. PTEN, a putative protein tyrosine phosphatase gene mutated in human brain, breast, and prostate cancer. Science 1997;275:1943-7.
32. + transport in cortical collecting duct cells. J Am Soc Nephrol 2005;16:2279-87.
33. Busjahn A, Aydin A, Uhlmann R, et al. Serum- and glucocorticoid-regulated kinase (SGK1) gene and blood pressure. Hypertension 2002;40:256-60.
34. Lifton RP, Gharavi AG, Geller DS. Molecular mechanisms of human hypertension. Cell 2001;104:545-56.
35. Avruch J, Hara K, Lin Y, et al. Insulin and amino-acid regulation of mTOR signaling and kinase activity through the Rheb GTPase. Oncogene 2006;25:6361-72.
36. Kobayashi T, Deak M, Morrice N, Cohen P. Characterization of the structure and regulation of two novel isoforms of serum- and glucocorticoid-induced protein kinase. Biochem J 1999;344 Pt 1:189-97.
37. Xu J, Liu D, Gill G, Songyang Z. Regulation of cytokine-independent survival kinase (CISK) by the Phoxhomolog y domain and phosphoinositides. J Cell Biol 2001;154:699-705.
38. Majumder PK, Yeh JJ, George DJ, et al. Prostate intraepithelial neoplasia induced by prostate restricted Akt activation: the MPAKT model. Proc Natl Acad Sci U S A 2003;100:7841-6.
39. Baron S, Manin M, Beaudoin C, et al. Androgen receptor mediates non-genomic activation of phosphatidylinositol 3-OH kinase in androgen-sensitive epithelial cells. J Biol Chem 2004;279:14579-86.
40. Sun M, Yang L, Feldman RI, et al. Activation of phosphatidylinositol 3-kinase/Akt pathway by androgen through interaction of p85α, androgen receptor, and Src. J Biol Chem 2003;278:42992-3000.