Targeting the Protein-Protein Interaction between IRS1 and Mutant p110α for Cancer Therapy

Toxicologic Pathology

Volumn 42, Issue 1, 2014, Pages 140-147

  Hao, Yujun ^a   Zhao, Shuliang ^a,b,c   Wang, Zhenghe ^a  

^a CASE WESTERN RESERVE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b SHANGHAI JIAO TONG UNIVERSITY SCHOOL OF MEDICINE   (China)

^c BEIJING HOSPITAL   (China)

Author keywords

cancer; genomics.; molecular biology

Indexed keywords

INSULIN RECEPTOR SUBSTRATE 1; MUTANT PROTEIN; P110ALPHA PROTEIN; PHOSPHATIDYLINOSITOL 3 KINASE; UNCLASSIFIED DRUG;

ARTICLE; BRAIN CANCER; BREAST CANCER; CANCER INHIBITION; CARCINOGENESIS; COLORECTAL CANCER; ENDOMETRIUM CANCER; ESOPHAGUS CANCER; GENE; GENE MUTATION; HUMAN; INTRACELLULAR SIGNALING; LIVER CANCER; LUNG CANCER; MOLECULAR MECHANICS; MOLECULARLY TARGETED THERAPY; MUTATION RATE; OVARY CANCER; PANCREAS CANCER; PI3K GENE; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN PROTEIN INTERACTION; PROTEIN TARGETING; SOMATIC MUTATION; STOMACH CANCER; THYROID CANCER; UTERINE CERVIX CANCER;

CANCER; GENOMICS.; MOLECULAR BIOLOGY;

CATALYTIC DOMAIN; HUMANS; INSULIN RECEPTOR SUBSTRATE PROTEINS; MOLECULAR TARGETED THERAPY; MUTANT PROTEINS; MUTATION; NEOPLASMS; ONCOGENES; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN INTERACTION DOMAINS AND MOTIFS; SIGNAL TRANSDUCTION;

EID: 84892725821     PISSN: 01926233     EISSN: 15331601     Source Type: Journal    
DOI: 10.1177/0192623313506794     Document Type: Article

References (42)

1. Bachman K. E., Argani P., Samuels Y., Silliman N., Ptak J., Szabo S., Konishi H., Karakas B., Blair B. G., Lin C., Peters B. A., Velculescu V. E., Park B. H.. The PIK3CA gene is mutated with high frequency in human breast cancers. Cancer Biol Ther. 2004 ; 3: 772-5
2. Broderick D. K., Di C., Parrett T. J., Samuels Y. R., Cummins J. M., McLendon R. E., Fults D. W., Velculescu V. E., Bigner D. D., Yan H.. Mutations of PIK3CA in anaplastic oligodendrogliomas, high-grade astrocytomas, and medulloblastomas. Cancer Res. 2004 ; 64: 5048-50
3. Burke J. E., Perisic O., Masson G. R., Vadas O., Williams R. L.. Oncogenic mutations mimic and enhance dynamic events in the natural activation of phosphoinositide 3-kinase p110alpha (PIK3CA). Proc Natl Acad Sci U S A. 2012 ; 109: 15259-64
4. Campbell I. G., Russell S. E., Choong D. Y., Montgomery K. G., Ciavarella M. L., Hooi C. S., Cristiano B. E., Pearson R. B., Phillips W. A.. Mutation of the PIK3CA gene in ovarian and breast cancer. Cancer Res. 2004 ; 64: 7678-81
5. Cantley L. C.. The phosphoinositide 3-kinase pathway. Science. 2002 ; 296: 1655-57
6. Chakrabarty A., Rexer B. N., Wang S. E., Cook R. S., Engelman J. A., Arteaga C. L.. H1047R phosphatidylinositol 3-kinase mutant enhances HER2-mediated transformation by heregulin production and activation of HER3. Oncogene. 2010 ; 29: 5193-203
7. Colombino M., Sperlongano P., Izzo F., Tatangelo F., Botti G., Lombardi A., Accardo M., Tarantino L., Sordelli I., Agresti M., Abbruzzese A., Caraglia M., Palmieri G.. BRAF and PIK3CA genes are somatically mutated in hepatocellular carcinoma among patients from South Italy. Cell Death Dis. 2012 ; 3: e259
8. Druker B. J., Talpaz M., Resta D. J., Peng B., Buchdunger E., Ford J. M., Lydon N. B., Kantarjian H., Capdeville R., Ohno-Jones S., Sawyers C. L.. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med. 2001 ; 344: 1031-37
9. Dulak A. M., Stojanov P., Peng S., Lawrence M. S., Fox C., Stewart C., Bandla S., Imamura Y., Schumacher S. E., Shefler E., McKenna A., Carter S. L., Cibulskis K., Sivachenko A., Saksena G., Voet D., Ramos A. H., Auclair D., Thompson K., Sougnez C., Onofrio R. C., Guiducci C., Beroukhim R., Zhou Z., Lin L., Lin J., Reddy R., Chang A., Landrenau R., Pennathur A., Ogino S., Luketich J. D., Golub T. R., Gabriel S. B., Lander E. S., Beer D. G., Godfrey T. E., Getz G., Bass A. J.. Exome and whole-genome sequencing of esophageal adenocarcinoma identifies recurrent driver events and mutational complexity. Nat Genet. 2013 ; 45: 478-86
10. Essmann F., Schulze-Osthoff K. Translational approaches targeting the p53 pathway for anticancer therapy. Br J Pharmacol. 2011 ; 165: 328-44
11. Garcia-Dios D. A., Lambrechts D., Coenegrachts L., Vandenput I., Capoen A., Webb P. M., Ferguson K., Anecs Akslen L. A., Claes B., Vergote I., Moerman P., Van Robays J., Marcickiewicz J., Salvesen H. B., Spurdle A. B., Amant F.. High-throughput interrogation of PIK3CA, PTEN, KRAS, FBXW7 and TP53 mutations in primary endometrial carcinoma. Gynecol Oncol. 2013 ; 128: 327-34
12. Garcia-Rostan G., Costa A. M., Pereira-Castro I., Salvatore G., Hernandez R., Hermsem M. J., Herrero A., Fusco A., Cameselle-Teijeiro J., Santoro M. Mutation of the PIK3CA gene in anaplastic thyroid cancer. Cancer Res. 2005 ; 65: 10199-207
13. Garraway L. A., Lander E. S. Lessons from the cancer genome. Cell. 2013 ; 153: 17-37
14. Gschwind A., Fischer O. M., Ullrich A. The discovery of receptor tyrosine kinases: Targets for cancer therapy. Nat Rev Cancer. 2004 ; 4: 361-70
15. Hao Y., Wang C., Cao B., Hirsch B. M., Song J., Markowitz S. D., Ewing R. M., Sedwick D., Liu L., Zheng W., Wang Z. Gain of interaction with IRS1 by p110alpha-helical domain mutants is crucial for their oncogenic functions. Cancer Cell. 2013 ; 23: 583-93
16. Hartmann C., Bartels G., Gehlhaar C., Holtkamp N., von Deimling A. PIK3CA mutations in glioblastoma multiforme. Acta Neuropathol. 2005 ; 109: 639-42
17. Huang C. H., Mandelker D., Schmidt-Kittler O., Samuels Y., Velculescu V. E., Kinzler K. W., Vogelstein B., Gabelli S. B., Amzel L. M.. The structure of a human p110alpha/p85alpha complex elucidates the effects of oncogenic PI3Kalpha mutations. Science. 2007 ; 318: 1744-48
18. Janku F., Lee J. J., Tsimberidou A. M., Hong D. S., Naing A., Falchook G. S., Fu S., Luthra R., Garrido-Laguna I., Kurzrock R.. PIK3CA mutations frequently coexist with RAS and BRAF mutations in patients with advanced cancers. PLoS One. 2011 ; 6: e22769
19. Khaw S. L., Huang D. C., Roberts A. W.. Overcoming blocks in apoptosis with BH3-mimetic therapy in haematological malignancies. Pathology. 2011 ; 43: 525-35
20. Lee J. H., Huynh M., Silhavy J. L., Kim S., Dixon-Salazar T., Heiberg A., Scott E., Bafna V., Hill K. J., Collazo A., Funari V., Russ C., Gabriel S. B., Mathern G. W., Gleeson J. G.. De novo somatic mutations in components of the PI3K-AKT3-mTOR pathway cause hemimegalencephaly. Nat Genet. 2012 ; 44: 941-45
21. Lee J. W., Soung Y. H., Kim S. Y., Lee H. W., Park W. S., Nam S. W., Kim S. H., Lee J. Y., Yoo N. J., Lee S. H.. PIK3CA gene is frequently mutated in breast carcinomas and hepatocellular carcinomas. Oncogene. 2005 ; 24: 1477-80
22. Levine D. A., Bogomolniy F., Yee C. J., Lash A., Barakat R. R., Borgen P. I., Boyd J.. Frequent mutation of the PIK3CA gene in ovarian and breast cancers. Clin Cancer Res. 2005 ; 11: 2875-78
23. Li J., Yen C., Liaw D., Podsypanina K., Bose S., Wang S. I., Puc J., Miliaresis C., Rodgers L., McCombie R., Bigner S. H., Giovanella B. C., Ittmann M., Tycko B., Hibshoosh H., Wigler M. H., Parsons R.. PTEN, a putative protein tyrosine phosphatase gene mutated in human brain, breast, and prostate cancer. Science. 1997 ; 275: 1943-47
24. Li V. S., Wong C. W., Chan T. L., Chan A. S., Zhao W., Chu K. M., So S., Chen X., Yuen S. T., Leung S. Y.. Mutations of PIK3CA in gastric adenocarcinoma. BMC Cancer. 2005 ; 5: 29
25. Liu P., Cheng H., Roberts T. M., Zhao J. J.. Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 ; 8: 627-44
26. Mandelker D., Gabelli S. B., Schmidt-Kittler O., Zhu J., Cheong I., Huang C. H., Kinzler K. W., Vogelstein B., Amzel L. M.. A frequent kinase domain mutation that changes the interaction between PI3Kalpha and the membrane. Proc Natl Acad Sci U S A. 2009 ; 106: 16996-7001
27. Miled N., Yan Y., Hon W. C., Perisic O., Zvelebil M., Inbar Y., Schneidman-Duhovny D., Wolfson H. J., Backer J. M., Williams R. L.. Mechanism of two classes of cancer mutations in the phosphoinositide 3-kinase catalytic subunit. Science. 2007 ; 317: 239-42
28. Oda K., Stokoe D., Taketani Y., McCormick F.. High frequency of coexistent mutations of PIK3CA and PTEN genes in endometrial carcinoma. Cancer Res. 2005 ; 65: 10669-73
29. Pang H., Flinn R., Patsialou A., Wyckoff J., Roussos E. T., Wu H., Pozzuto M., Goswami S., Condeelis J. S., Bresnick A. R., Segall J. E., Backer J. M.. Differential enhancement of breast cancer cell motility and metastasis by helical and kinase domain mutations of class IA phosphoinositide 3-kinase. Cancer Res. 2009 ; 69: 8868-76
30. Phillips W. A., Russell S. E., Ciavarella M. L., Choong D. Y., Montgomery K. G., Smith K., Pearson R. B., Thomas R. J., Campbell I. G.. Mutation analysis of PIK3CA and PIK3CB in esophageal cancer and Barrett's esophagus. Int J Cancer. 2006 ; 118: 2644-46
31. Rodon J., Dienstmann R., Serra V., Tabernero J.. Development of PI3K inhibitors: Lessons learned from early clinical trials. Nat Rev Clin Oncol. 2013 ; 10: 143-53
32. Saal L. H., Holm K., Maurer M., Memeo L., Su T., Wang X., Yu J. S., Malmstrom P. O., Mansukhani M., Enoksson J., Hibshoosh H., Borg A., Parsons R.. PIK3CA mutations correlate with hormone receptors, node metastasis, and ERBB2, and are mutually exclusive with PTEN loss in human breast carcinoma. Cancer Res. 2005 ; 65: 2554-59
33. Samuels Y., Diaz L. A., Schmidt-Kittler O., Cummins J. M., Delong L., Cheong I., Rago C., Huso D. L., Lengauer C., Kinzler K. W., Vogelstein B., Velculescu V. E.. Mutant PIK3CA promotes cell growth and invasion of human cancer cells. Cancer Cell. 2005 ; 7: 561-73
34. Samuels Y., Wang Z., Bardelli A., Silliman N., Ptak J., Szabo S., Yan H., Gazdar A., Powell S. M., Riggins G. J., Willson J. K., Markowitz S., Kinzler K. W., Vogelstein B., Velculescu V. E.. High frequency of mutations of the PIK3CA gene in human cancers. Science. 2004 ; 304: 554
35. Schonleben F., Qiu W., Ciau N. T., Ho D. J., Li X., Allendorf J. D., Remotti H. E., Su G. H.. PIK3CA mutations in intraductal papillary mucinous neoplasm/carcinoma of the pancreas. Clin Cancer Res. 2006 ; 12: 3851-55
36. Sosman J. A., Kim K. B., Schuchter L., Gonzalez R., Pavlick A. C., Weber J. S., McArthur G. A., Hutson T. E., Moschos S. J., Flaherty K. T., Hersey P., Kefford R., Lawrence D., Puzanov I., Lewis K. D., Amaravadi R. K., Chmielowski B., Lawrence H. J., Shyr Y., Ye F., Li J., Nolop K. B., Lee R. J., Joe A. K., Ribas A.. Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med. 2012 ; 366: 707-14
37. Vadas O., Burke J. E., Zhang X., Berndt A., Williams R. L. Structural basis for activation and inhibition of class I phosphoinositide 3-kinases. Sci Signal. 2011 ; 4 :
38. Vasudevan K. M., Barbie D. A., Davies M. A., Rabinovsky R., McNear C. J., Kim J. J., Hennessy B. T., Tseng H., Pochanard P., Kim S. Y., Dunn I. F., Schinzel A. C., Sandy P., Hoersch S., Sheng Q., Gupta P. B., Boehm J. S., Reiling J. H., Silver S., Lu Y., Stemke-Hale K., Dutta B., Joy C., Sahin A. A., Gonzalez-Angulo A. M., Lluch A., Rameh L. E., Jacks T., Root D. E., Lander E. S., Mills G. B., Hahn W. C., Sellers W. R., Garraway L. A. AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer. Cancer Cell. 2009 ; 16: 21-32
39. White A. W., Westwell A. D., Brahemi G. Protein-protein interactions as targets for small-molecule therapeutics in cancer. Expert Rev Mol Med. 2008 ; 10: e8
40. Yamamoto H., Shigematsu H., Nomura M., Lockwood W. W., Sato M., Okumura N., Soh J., Suzuki M., Wistuba II, Fong K. M., Lee H., Toyooka S., Date H., Lam W. L., Minna J. D., Gazdar A. F. PIK3CA mutations and copy number gains in human lung cancers. Cancer Res. 2008 ; 68: 6913-21
41. Zhao L., Vogt P. K. Class I PI3K in oncogenic cellular transformation. Oncogene. 2008a ; 27: 5486-96
42. Zhao L., Vogt P. K. Helical domain and kinase domain mutations in p110alpha of phosphatidylinositol 3-kinase induce gain of function by different mechanisms. Proc Natl Acad Sci U S A. 2008b ; 105: 2652-57