Peptidomimetic targeting of critical androgen receptor-coregulator interactions in prostate cancer

Nature Communications

Volumn 4, Issue , 2013, Pages

  Ravindranathan, Preethi ^a   Lee, Tae Kyung ^b   Yang, Lin ^a,c   Centenera, Margaret M ^d   Butler, Lisa ^d   Tilley, Wayne D ^d   Hsieh, Jer Tsong ^a   Ahn, Jung Mo ^b   Raj, Ganesh V ^a  

^a UNIVERSITY OF TEXAS SOUTHWESTERN MEDICAL CENTER   (United States)

^b UNIVERSITY OF TEXAS AT DALLAS   (United States)

^c THE FIRST AFFILIATED HOSPITAL OF XI AN JIAOTONG UNIVERSITY   (China)

^d UNIVERSITY OF ADELAIDE   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

ANDROGEN RECEPTOR; ANTINEOPLASTIC AGENT; D 2; PELP1 PROTEIN; PEPTIDOMIMETIC AGENT; REGULATOR PROTEIN; UNCLASSIFIED DRUG;

ANDROGEN; CANCER; GROWTH; INHIBITION; NUMERICAL MODEL; PROTEIN; SIGNALING; TOXICITY;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CANCER CELL; CANCER INHIBITION; CELL PROLIFERATION; CONTROLLED STUDY; GENE OVEREXPRESSION; HUMAN; HUMAN CELL; IC 50; MALE; MOLECULAR INTERACTION; MOUSE; NONHUMAN; PROSTATE CANCER; PROTEIN PROTEIN INTERACTION; SIGNAL TRANSDUCTION; TUMOR XENOGRAFT;

EID: 84878645503     PISSN: None     EISSN: 20411723     Source Type: Journal    
DOI: 10.1038/ncomms2912     Document Type: Article

References (43)

1. Attard, G., Cooper, C. S. & de Bono, J. S Steroid hormone receptors in prostate cancer: a hard habit to break? Cancer Cell 16, 458-462 (2009).
2. Scher, H. I., Buchanan, G., Gerald, W., Butler, L. M. & Tilley, W. D. Targeting the androgen receptor: improving outcomes for castration-resistant prostate cancer. Endocr. Relat. Cancer 11, 459-476 (2004). (Pubitemid 39331277)
3. Chen, C. D. et al. Molecular determinants of resistance to antiandrogen therapy. Nat. Med. 10, 33-39 (2004). (Pubitemid 38524696)
4. Harris, W. P., Mostaghel, E. A., Nelson, P. S. & Montgomery, B. Androgen deprivation therapy: progress in understanding mechanisms of resistance and optimizing androgen depletion. Nat. Clin. Pract. Urol. 6, 76-85 (2009).
5. Knudsen, K. E. & Scher, H. I. Starving the addiction: new opportunities for durable suppression of AR signaling in prostate cancer. Clin. Cancer Res. 15, 4792-4798 (2009).
6. Hsieh, A. C., Small, E. J. & Ryan, C. J. Androgen-response elements in hormone-refractory prostate cancer: implications for treatment development. Lancet Oncol. 8, 933-939 (2007). (Pubitemid 47488068)
7. Mostaghel, E. A. et al. Intraprostatic androgens and androgen-regulated gene expression persist after testosterone suppression: therapeutic implications for castration-resistant prostate cancer. Cancer Res. 67, 5033-5041 (2007). (Pubitemid 46910214)
8. Sharifi, N. Hormonal therapy for prostate cancer: toward further unraveling of androgen receptor function. Anticancer Agents Med. Chem. 9, 1046-1051 (2009).
9. Wang, Q. et al. Androgen receptor regulates a distinct transcription program in androgen-independent prostate cancer. Cell 138, 245-256 (2009).
10. Yuan, X. & Balk, S. P. Mechanisms mediating androgen receptor reactivation after castration. Urol. Oncol. 27, 36-41 (2009).
11. Agoulnik, I. U. & Weigel, N. L. Androgen receptor coactivators and prostate cancer. Adv. Exp. Med. Biol. 617, 245-255 (2008).
12. Agoulnik, I. U. & Weigel, N. L. Coactivator selective regulation of androgen receptor activity. Steroids 74, 669-674 (2009).
13. Nair, S. & Vadlamudi, R. K. Emerging significance of ER-coregulator PELP1/ MNAR in cancer. Histol. Histopathol. 22, 91-96 (2007). (Pubitemid 46117094)
14. Vadlamudi, R. K. & Kumar, R. Functional and biological properties of the nuclear receptor coregulator PELP1/MNAR. Nucl. Recept. Signal. 5, e004 (2007).
15. Vadlamudi, R. K., Balasenthil, S., Broaddus, R. R., Gustafsson, J. A. & Kumar, R. Deregulation of estrogen receptor coactivator proline-, glutamic acid-, and leucine-rich protein-1/modulator of nongenomic activity of estrogen receptor in human endometrial tumors. J. Clin. Endocrinol. Metab. 89, 6130-6138 (2004). (Pubitemid 39628425)
16. Chakravarty, D., Tekmal, R. R. & Vadlamudi, R. K. PELP1: A novel therapeutic target for hormonal cancers. IUBMB Life 62, 162-169 (2010).
17. Nair, S. S. et al. Proline-, glutamic acid-, and leucine-rich protein-1/modulator of nongenomic activity of estrogen receptor enhances androgen receptor functions through LIM-only coactivator, four-and-a-half LIM-only protein 2. Mol. Endocrinol. 21, 613-624 (2007).
18. Chakravarty, D. et al. Therapeutic targeting of PELP1 prevents ovarian cancer growth and metastasis. Clin. Cancer Res. 17, 2250-2259 (2011).
19. Roy, S. et al. Significance of PELP1 in ER-negative breast cancer metastasis. Mol. Cancer Res. 10, 25-33 (2012).
20. Yang, L. et al. Central role for PELP1 in nonandrogenic activation of the androgen receptor in prostate cancer. Mol. Endocrinol. 26, 550-561 (2012).
21. Estebanez-Perpina, E. et al. The molecular mechanisms of coactivator utilization in ligand-dependent transactivation by the androgen receptor. J. Biol. Chem. 280, 8060-8068 (2005). (Pubitemid 40349704)
22. Cheng, W. & Lim, L. Peroral delivery of peptide drugs. Am. Pharm. Rev. 11, 33-41 (2008).
23. Ahn, J. M., Boyle, N. A., MacDonald, M. T. & Janda, K. D. Peptidomimetics and peptide backbone modifications. Mini Rev. Med. Chem. 2, 463-473 (2002).
24. He, B. et al. Structural basis for androgen receptor interdomain and coactivator interactions suggests a transition in nuclear receptor activation function dominance. Mol. Cell 16, 425-438 (2004). (Pubitemid 39504796)
25. Hur, E. et al. Recognition and accommodation at the androgen receptor coactivator binding interface. PLoS Biol. 2, E274 (2004).
26. Ahn, J. -M. H. & Han, S. -Y. Facile synthesis of benzamides to mimic an ahelix. Tetrahedron Lett. 48, 3543-3547 (2007). (Pubitemid 46590196)
27. Mohamadi, F. et al. MacroModel- An integrated software system for modeling organic and bioorganic molecules using molecular mechanics. J. Comput. Chem. 11, 440-467 (1990).
28. Allinger, N. I., Yuh, Y. H. & Lii, J.-H Molecular mechanics. The MM3 force field for hydrocarbons 1. J. Am. Chem. Soc. 111, 8551-8565 (1989).
29. Morris, G. M. et al. Automated docking using a lamarckian genetic algorithm and an empirical binding free energy function. J. Comput. Chem. 19, 1639-1662 (1998). (Pubitemid 128590223)
30. Lee, T. K. & Ahn, J. M. Solid-phase synthesis of tris-benzamides as alpha-helix mimetics. ACS Comb. Sci. 13, 107-111 (2011).
31. Heemers, H. V. & Tindall, D. J. Androgen receptor (AR) coregulators: a diversity of functions converging on and regulating the AR transcriptional complex. Endocr. Rev. 28, 778-808 (2007). (Pubitemid 350294296)
32. Heemers, H. V. & Tindall, D. J. Unraveling the complexities of androgen receptor signaling in prostate cancer cells. Cancer Cell 15, 245-247 (2009).
33. Marimganti, S., Cheemala, M. N. & Ahn, J. M. Novel amphiphilic alpha-helix mimetics based on a bis-benzamide scaffold. Org. Lett. 11, 4418-4421 (2009).
34. Plante, J. P. et al. Oligobenzamide proteomimetic inhibitors of the p53-hDM2 protein-protein interaction. Chem. Commun. 34, 5091-5093 (2009).
35. Saraogi, I., Incarvito, C. D. & Hamilton, A. D. Controlling curvature in a family of oligoamide alpha-helix mimetics. Angew. Chem. Int. Ed. 47, 9691-9694 (2008).
36. Shaginia, A. et al. Design, synthesis, and evaluation of an alpha-helix mimetic library targeting protein-protein interactions. J. Am. Chem. Soc. 131, 5564-5572 (2009).
37. Tran, C. et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science 324, 787-790 (2009).
38. Ryan, C. J. & Tindall, D. J. Androgen receptor rediscovered: the new biology and targeting the androgen receptor therapeutically. J. Clin. Oncol. 29, 3651-3658 (2011).
39. Scher, H. I. et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet 375, 1437-1446 (2010).
40. Mukherji, D., Eichholz, A. & De Bono, J. S. Management of metastatic castration-resistant prostate cancer: recent advances. Drugs 72, 1011-1028 (2012).
41. Motzer, R. J. et al. Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N. Engl. J. Med. 356, 115-124 (2007). (Pubitemid 46089672)
42. Motzer, R. J. et al. Activity of SU11248, a multitargeted inhibitor of vascular endothelial growth factor receptor and platelet-derived growth factor receptor, in patients with metastatic renal cell carcinoma. J. Clin. Oncol. 24, 16-24 (2006). (Pubitemid 46630489)
43. Centenera, M. M. et al. Evidence for efficacy of new Hsp90 inhibitors revealed by ex vivo culture of human prostate tumors. Clin. Cancer Res. 18, 3562-3570 (2012).