REFERENCES

1. Feig LA, Buchsbaum RJ. Cell signaling: life or death decisions of Ras proteins. Curr Biol 2002;12:259-61.

2. Shields JM, Pruitt K, Shaub A, Der CJ. Understanding Ras : ‘it ain’t over ‘til it’s over’. Trends Cell Biol 2000;10:147-54.

3. Bos JL. ras oncogenes in human cancer : a review. Cancer Res 1989;49:4682-9.

4. Vetter IR, Wittinghofer A. The guanine nucleotide - binding switch in three dimensions. Science 2001;294:1299-304.

5. Lenzen C, Cool RH, Prinz H, Wittinghofer A. Kinetic analysis by fluorescence of the interaction between Ras and the catalytic domain of the guanine nucleotide exchange factor Cdc25Mm. Biochemistry 1998;37:7420-30.

6. Karnoub AE, Weinberg RA. Ras oncogenes: split personalities. Nat Rev Mol Cell Biol 2008;9:517-31.

7. Vetter IR. The structure of the G domain of the Ras superfamily. Ras Superfamily Small G Proteins: Biology and Mechanisms 1. Wien: Springer Verlag; 2014. pp. 25-51.

8. Wittinghofer A, Vetter IR. Structure-function relationships of the G domain, a canonical switch motif. Ann Rev Biochem 2011;80:943-71.

9. Spoerner M, Nuehs A, Herrmann C, Steiner G, Kalbitzer HR. Slow conformational dynamics of the guanine nucleotide-binding protein Ras complexed with the GTP analogue GTPγS. FEBS J 2007;274:1419-33.

10. Spoerner M, Hozsa C, Poetzl JA, Reiss K, Ganser P, et al. Conformational states of human rat sarcoma (Ras) protein complexed with its natural ligand GTP and their role for effector interaction and GTP hydrolysis. J Biol Chem 2010;285:39768-78.

11. Ito Y, Yamasaki K, Iwahara J, Terada T, Kamiya A, et al. Regional polysterism in the GTP-bound form of the human c-Ha-Ras protein. Biochemistry 1997;36:9109-19.

12. Barbacid M. ras genes. Annu Rev Biochem 1987;56:779-827.

13. Malumbres M, Barbacid M. RAS oncogenes: the first 30 years. Nat Rev Cancer 2003;3:459-65.

14. Vetter IR, Wittinghofer A. The guanine nucleotide-binding switch in three dimensions. Science 2001;294:1299-304.

15. Hancock JF. Ras proteins: different signals from different locations. Nat Rev Mol Cell Biol 2003;4:373-84.

16. Lemmon MA, Schlessinger J. Cell signaling by receptor tyrosine kinases. Cell 2010;141:1117-34.

17. Cox AD, Der CJ. Ras history: the saga continues. Small GTPases 2010;1:2-27.

18. Gibbs JB, Sigal IS, Poe M, Scolnick EM. Intrinsic GTPase activity distinguishes normal and oncogenic ras p21 molecules. Proc Natl Acad Sci U S A 1984;81:5704-8.

19. McGrath JP, Capon DJ, Goeddel DV, Levinson AD. Comparative biochemical properties of normal and activated human ras p21 protein. Nature 1984;310:644-9.

20. Sweet RW, Yokoyama S, Kamata T, Feramisco JR, Rosenberg M, et al. The product of ras is a GTPase and the T24 oncogenic mutant is deficient in this activity. Nature 1984;311:273-5.

21. Scheffzek K, Lautwein A, Kabsch W, Ahmadian MR, Wittinghofer A. Crystal structure of the GTPase-activating domain of human p120GAP and implications for the interaction with Ras. Nature 1996;384:591-6.

22. Schubbert S, Shannon K, Bollag G. Hyperactive Ras in developmental disorders and cancer. Nat Rev Cancer 2007;7:295-308.

23. Jemal A, Siegel R, Xu J, Ward E. Cancer statistics, 2010. CA Cancer J Clin 2010;60:277-300.

24. Dhillon AS, Hagan S, Rath O, Kolch W. MAP kinase signalling pathways in cancer. Oncogene 2007;26:3279-90.

25. De Luca A, Maiello MR, D'Alessio A, Pergameno M, Normanno N. The RAS/RAF/MEK/ERK and the PI3K/AKT signalling pathways: role in cancer pathogenesis and implications for therapeutic approaches. Expert Opin Ther Targets 2012;16 Suppl 2:S17-27.

26. Pullikuth AK, Catling AD. Scaffold mediated regulation of MAPK signaling and cytoskeletal dynamics: a perspective. Cell Signal 2007;19:1621-32.

27. Ma L, Chen Z, Erdjument-Bromage H, Tempst P, Pandolfi PP. Phosphorylation and functional inactivation of TSC2 by Erk implications for tuberous sclerosis and cancer pathogenesis. Cell 2005;121:179-93.

28. Choi M, Bien H, Mofunanya A, Powers S. Challenges in Ras therapeutics in pancreatic cancer. Semin Cancer Biol 2019;54:101-8.

29. Yang SH, Sharrocks AD, Whitmarsh AJ. MAP kinase signalling cascades and transcriptional regulation. Gene 2013;513:1-13.

30. Andjelkovic M, Alessi DR, Meier R, Fernandez A, Lamb NJ, et al. Role of translocation in the activation and function of protein kinase B. J Biol Chem 1997;272:31515-24.

31. Cai SL, Tee AR, Short JD, Bergeron JM, Kim J, et al. Activity of TSC2 is inhibited by AKT-mediated phosphorylation and membrane partitioning. J Cell Biol 2006;173:279-89.

32. Long GV, Hauschild A, Santinami M, Atkinson V, Mandala M, et al. Adjuvant Dabrafenib plus Trametinib in stage III BRAF-mutated melanoma. N Engl J Med 2017;377:1813-23.

33. Janne PA, van den Heuvel MM, Barlesi F, Cobo M, Mazieres J, et al. Selumetinib plus docetaxel compared with docetaxel alone and progression-free survival in patients with KRAS-mutant advanced non-small cell lung cancer: the SELECT-1 randomized clinical trial. JAMA 2017;317:1844-53.

34. Pulido JS, Heier JS, Marmorstein AD. Selumetinib in plexiform neurofibromas. N Engl J Med 2017;376:1195.

35. Signorelli J, Shah Gandhi A. Cobimetinib. Ann Pharmacother 2017;51:146-53.

36. Dummer R, Schadendorf D, Ascierto PA, Arance A, Dutriaux C, et al. Binimetinib versus dacarbazine in patients with advanced NRAS-mutant melanoma (NEMO): a multicentre, open-label, randomised, phase 3 trial. Lancet Oncol 2017;18:435-45.

37. Nijenhuis CM, Huitema AD, Blank C, Haanen JB, van Thienen JV, et al. Clinical Pharmacokinetics of Vemurafenib in BRAF-mutated melanoma patients. J Clin Pharmacol 2017;57:125-8.

38. Zhang W, Heinzmann D, Grippo JF. Clinical pharmacokinetics of vemurafenib. Clin Pharmacokinet 2017;56:1033-43.

39. Delord JP, Robert C, Nyakas M, McArthur GA, Kudchakar R, et al. Phase I dose-escalation and -expansion study of the BRAF inhibitor encorafenib (LGX818) in metastatic BRAF-mutant melanoma. Clin Cancer Res 2017;23:5339-48.

40. Gounder MM, Mahoney MR, Van Tine BA, Ravi V, Attia S, et al. Sorafenib for advanced and refractory desmoid tumors. N Engl J Med 2018;379:2417-28.

41. Di Leo A, Johnston S, Lee KS, Ciruelos E, Lonning PE, et al. Buparlisib plus fulvestrant in postmenopausal women with hormone-receptor-positive, HER2-negative, advanced breast cancer progressing on or after mTOR inhibition (BELLE-3): a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet Oncol 2018;19:87-100.

42. Furman RR, Sharman JP, Coutre SE, Cheson BD, Pagel JM, et al. Idelalisib and rituximab in relapsed chronic lymphocytic leukemia. N Engl J Med 2014;370:997-1007.

43. Gopal AK, Kahl BS, de Vos S, Wagner-Johnston ND, Schuster SJ, et al. PI3Kdelta inhibition by idelalisib in patients with relapsed indolent lymphoma. N Engl J Med 2014;370:1008-18.

44. Younes A, Salles G, Martinelli G, Bociek RG, Barrigon DC, et al. Pan-phosphatidylinositol 3-kinase inhibition with buparlisib in patients with relapsed or refractory non-Hodgkin lymphoma. Haematologica 2017;102:2104-12.

45. Wang C, Liu B, Xu X, Zhuang B, Li H, et al. Toward targeted therapy in chemotherapy-resistant pancreatic cancer with a smart triptolide nanomedicine. Oncotarget 2016;7:8360-72.

46. Takai E, Yachida S. Genomic alterations in pancreatic cancer and their relevance to therapy. World J Gastrointest Oncol 2015;7:250-8.

47. Grasso C, Jansen G, Giovannetti E. Drug resistance in pancreatic cancer: Impact of altered energy metabolism. Crit Rev Oncol Hematol 2017;114:139-52.

48. Hezel AF, Kimmelman AC, Stanger BZ, Bardeesy N, Depinho RA. Genetics and biology of pancreatic ductal adenocarcinoma. Genes Dev 2006;20:1218-49.

49. Cetinbas NM, Sudderth J, Harris RC, Cebeci A, Negri GL, et al. Glucose-dependent anaplerosis in cancer cells is required for cellular redox balance in the absence of glutamine. Sci Rep 2016;6:32606.

50. Soleimani A, Amirinejad M, Rahsepar S, Vazirian F, Bahrami A, et al. Therapeutic potential of RAS prenylation pharmacological inhibitors in the treatment of breast cancer, recent progress, and prospective. J Cell Biochem 2019;120:6860-7.

51. Whyte DB, Kirschmeier P, Hockenberry TN, Nunez-Oliva I, James L, et al. K- and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors. J Biol Chem 1997;272:14459-64.

52. Feuerstein J, Kalbitzer HR, John J, Goody RS, Wittinghofer A. Characterisation of the metal-ion-GDP complex at the active sites of transforming and nontransforming p21 proteins by observation of the 17O-Mn superhyperfine coupling and by kinetic methods. Eur J Biochem 1987;162:49-55.

53. Traut TW. Physiological concentrations of purines and pyrimidines. Mol Cell Biochem 1994;140:1-22.

54. Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl 2014;53:199-204.

55. Patricelli MP, Janes MR, Li LS, Hansen R, Peters U, et al. Selective inhibition of oncogenic KRAS output with small molecules targeting the inactive state. Cancer Discov 2016;6:316.

56. Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature 2013;503:548-51.

57. Patgiri A, Yadav KK, Arora PS, Bar-sagi D. An orthosteric inhibitor of Ras-Sos interaction. Nat Chem Biol 2011;7:585-7.

58. Cochet O, Kenigsberg M, Delumeau I, Virone-Oddos A, Multon MC, et al. Intracellular Expression of an Antibody Fragment-neutralizing p21 Ras Promotes Tumor Regression. Cancer Research 1998;58:1170.

59. Maurer T, Garrenton LS, Oh A, Pitts K, Anderson DJ, et al. Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity. Proc Natl Acad Sci U S A 2012;109:5299-304.

60. Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, et al. Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation. Angew Chem Int Ed Engl 2012;51:6140-3.

61. Schöpel M, Shkura O, Seidel J, Kock K, Zhong X, et al. Allosteric activation of GDP-bound ras isoforms by bisphenol derivative plasticisers. Int J Mol Sci 2018;19:1133.

62. Xie C, Li Y, Li LL, Fan XX, Wang YW, et al. Identification of a new potent inhibitor targeting KRAS in non-small cell lung cancer cells. Front Pharmacol 2017;8:823.

63. Welsch ME, Kaplan A, Chambers JM, Stokes ME, Bos PH, et al. Multivalent small-molecule Pan-RAS inhibitors. Cell 2017;168:878-89.e29.

64. Quevedo CE, Cruz-Migoni A, Bery N, Miller A, Tanaka T, et al. Small molecule inhibitors of RAS-effector protein interactions derived using an intracellular antibody fragment. Nature communications 2018;9:3169.

65. McCarthy MJ, Pagba CV, Prakash P, Naji AK, van der Hoeven D, et al. Discovery of high-affinity noncovalent allosteric KRAS inhibitors that disrupt effector binding. ACS Omega 2019;4:2921-30.

66. Schöpel M, Jockers KFG, Düppe PM, Autzen J, Potheraveedu VN, et al. Bisphenol a binds to Ras proteins and competes with guanine nucleotide exchange: implications for GTPase-selective antagonists. J Med Chem 2013;56:9664-72.

67. Rogers JA, Metz L, Yong VW. Review: endocrine disrupting chemicals and immune responses: a focus on bisphenol-A and its potential mechanisms. Mol Immunol 2013;53:421-30.

68. Herr HW, Morales A. History of bacillus calmette-guerin and bladder cancer: an immunotherapy success story. J Urol 2008;179:53-6.

69. Balakrishnan AS, Washington SL 3rd, Meng MV, Porten SP. Determinants of guideline-based treatment in patients With cT1 bladder cancer. Clin Genitourin Cancer 2019;17:e461-71.

70. Ishida Y, Agata Y, Shibahara K, Honjo T. Induced expression of PD-1, a novel member of the immunoglobulin gene superfamily, upon programmed cell death. EMBO J 1992;11:3887-95.

71. Xia Y, Jeffrey Medeiros L, Young KH. Signaling pathway and dysregulation of PD1 and its ligands in lymphoid malignancies. Biochim Biophys Acta 2016;1865:58-71.

72. Iwai Y, Terawaki S, Honjo T. PD-1 blockade inhibits hematogenous spread of poorly immunogenic tumor cells by enhanced recruitment of effector T cells. Int Immunol 2005;17:133-44.

73. Gong J, Chehrazi-Raffle A, Reddi S, Salgia R. Development of PD-1 and PD-L1 inhibitors as a form of cancer immunotherapy: a comprehensive review of registration trials and future considerations. J Immunother Cancer 2018;6:8.

74. Hanahan D, Weinberg RA. Hallmarks of cancer: the next generation. Cell 2011;144:646-74.

75. McKinney EF, Smith KG. T cell exhaustion and immune-mediated disease-the potential for therapeutic exhaustion. Curr Opin Immunol 2016;43:74-80.

76. Garon EB, Rizvi NA, Hui R, Leighl N, Balmanoukian AS, et al. Pembrolizumab for the treatment of non-small-cell lung cancer. N Engl J Med 2015;372:2018-28.

77. Borghaei H, Paz-Ares L, Horn L, Spigel DR, Steins M, et al. Nivolumab versus docetaxel in advanced nonsquamous non-small-cell lung cancer. N Engl J Med 2015;373:1627-39.

78. Song TL, Nairismagi ML, Laurensia Y, Lim JQ, Tan J, et al. Oncogenic activation of the STAT3 pathway drives PD-L1 expression in natural killer/T-cell lymphoma. Blood 2018;132:1146-58.

79. Marzec M, Zhang Q, Goradia A, Raghunath PN, Liu X, et al. Oncogenic kinase NPM/ALK induces through STAT3 expression of immunosuppressive protein CD274 (PD-L1, B7-H1). Proc Natl Acad Sci U S A 2008;105:20852-7.

80. Atsaves V, Tsesmetzis N, Chioureas D, Kis L, Leventaki V, et al. PD-L1 is commonly expressed and transcriptionally regulated by STAT3 and MYC in ALK-negative anaplastic large-cell lymphoma. Leukemia 2017;31:1633-7.

81. Sumimoto H, Takano A, Teramoto K, Daigo Y. RAS-mitogen-activated protein kinase signal is required for enhanced PD-L1 expression in human lung cancers. PLoS One 2016;11:e0166626.

82. Coelho MA, de Carne Trecesson S, Rana S, Zecchin D, Moore C, et al. Oncogenic RAS signaling promotes tumor immunoresistance by stabilizing PD-L1 mRNA. Immunity 2017;47:1083-99.e6.

83. Jiang X, Zhou J, Giobbie-Hurder A, Wargo J, Hodi FS. The activation of MAPK in melanoma cells resistant to BRAF inhibition promotes PD-L1 expression that is reversible by MEK and PI3K inhibition. Clin Cancer Res 2013;19:598-609.

84. Sanlorenzo M, Vujic I, Floris A, Novelli M, Gammaitoni L, et al. BRAF and MEK inhibitors increase PD-1-positive melanoma cells leading to a potential lymphocyte-independent synergism with anti-PD-1 antibody. Clin Cancer Res 2018;24:3377-85.

85. Mittendorf EA, Philips AV, Meric-Bernstam F, Qiao N, Wu Y, et al. PD-L1 expression in triple-negative breast cancer. Cancer Immunol Res 2014;2:361-70.

86. Xu C, Fillmore CM, Koyama S, Wu H, Zhao Y, et al. Loss of Lkb1 and Pten leads to lung squamous cell carcinoma with elevated PD-L1 expression. Cancer Cell 2014;25:590-604.

87. Lastwika KJ, Wilson W 3rd, Li QK, Norris J, Xu H, et al. Control of PD-L1 Expression by oncogenic activation of the AKT-mTOR pathway in non-small cell lung cancer. Cancer Res 2016;76:227-38.

88. Balan M, Miery Teran E, Waaga-Gasser AM, Gasser M, Choueiri TK, et al. Novel roles of c-Met in the survival of renal cancer cells through the regulation of HO-1 and PD-L1 expression. J Biol Chem 2015;290:8110-20.

89. Wang Q, Ning H, Peng H, Wei L, Hou R, et al. Tristetraprolin inhibits macrophage IL-27-induced activation of antitumour cytotoxic T cell responses. Nat Commun 2017;8:867.

90. Kataoka K, Shiraishi Y, Takeda Y, Sakata S, Matsumoto M, et al. Aberrant PD-L1 expression through 3'-UTR disruption in multiple cancers. Nature 2016;534:402-6.

91. Falk AT, Yazbeck N, Guibert N, Chamorey E, Paquet A, et al. Effect of mutant variants of the KRAS gene on PD-L1 expression and on the immune microenvironment and association with clinical outcome in lung adenocarcinoma patients. Lung Cancer 2018;121:70-5.

92. Pallis M, Abdul-Aziz A, Burrows F, Seedhouse C, Grundy M, et al. The multi-kinase inhibitor TG02 overcomes signalling activation by survival factors to deplete MCL1 and XIAP and induce cell death in primary acute myeloid leukaemia cells. Br J Haematol 2012;159:191-203.

93. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, et al. TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Leukemia 2012;26:236-43.

94. Su YT, Chen R, Wang H, Song H, Zhang Q, et al. Novel targeting of transcription and metabolism in glioblastoma. Clin Cancer Res 2018;24:1124-37.

Cancer Drug Resistance
ISSN 2578-532X (Online)

Portico

All published articles will preserved here permanently:

https://www.portico.org/publishers/oae/

Portico

All published articles will preserved here permanently:

https://www.portico.org/publishers/oae/