Page 72 - Read Online

Page 364 Raczka et al. Cancer Drug Resist 2019;2:356-64 I http://dx.doi.org/10.20517/cdr.2018.004

deregulated glutamine metabolism pathway and its suppression synergizes with mTOR inhibition. PLoS One 2017;12:e0185092.
44. Parlati F. CB-839, a selective glutaminase inhibitor, synergizes with signaling pathway inhibitors to produce an anti-tumor effect in
cell lines and tumor xenografts. Available from: https://www.calithera.com/wp-content/uploads/2017/12/AACR-2015-final.pdf. [Last
accessed on 24 Apr 2019]
45. Gameiro PA, Yang J, Metelo AM, Perez-Carro R, Baker R, et al. In virto HIF-mediated reductive carboxylation is regulated by citrate
levels and sensitizes VHL-deficient cells to glutamine deprivation. Cell Metabolism 17;372-85.
46. Study of the Glutaminase Inhibitor CB-839 in Solid Tumors. Available from: https://clinicaltrials.gov/ct2/show/NCT02071862. [Last
accessed on 24 Apr 2019]
47. Harding J, Telli M, Munster P, Le M, Molineaux C, et al. Safety and tolerability of increasing doses of CB-839, a first-in-class, orally
administered small molecule inhibitor of glutaminase, in solid tumors. J Clin Oncol 2015;33:2512.
48. Meric-Bernstam F, Tannir N, Mier J, DeMichele A, Telli M, et al. Phase 1 study of CB-839, a small molecule inhibitor of glutaminase
(GLS), alone and in combination with everolimus (E) in patients (pts) with renal cell cancer (RCC). J Clin Oncol 2016;34:4568.
49. Guo H, German P, Bai S, Barnes S, Guo W, Qi X, et al. The PI3K/AKT pathway and renal cell carcinoma. J Genet Genomics
2015;42:343-53.
50. Bernardi R, Guernah I, Jin D, Grisendi S, Alimonti A, et al. PML inhibits HIF-1α translation and neoangiogenesis through repression of
mTOR. Nature 2006;442:779.
51. Brodaczewska K, Szczylik C, Fiedorowicz M, Porta C, Czarnecka A. Choosing the right cell line for renal cell cancer research. Mol
Cancer 2016;15:83.
52. Tannir N, Fan A, Lee R, Carthon B, Iliopoulos O, et al. Phase 1 study of glutaminase (GLS) inhibitor CB-839 combined with either
everolimus (E) or cabozantinib (Cabo) in patients (pts) with clear cell (cc) and papillary (pap) metastatic renal cell cancer (mRCC). J
Clin Oncol 2018;36:603.
53. Meric-Bernstam F, Tannir N, Harding J, Voss M, Mier J, DeMichele A, et al. Phase 1 study of CB-839, a small molecule inhibitor
of glutaminase, in combination with everolimus in patients (pts) with clear cell and papillary renal cell cancer (RCC). Eur J Cancer
2016;69:S12-S3.
54. Guo L, Zhang H, Chen B. Nivolumab as programmed death-1 (PD-1) inhibitor for targeted immunotherapy in tumor. J Cancer
2017;8:410-6.
55. Gross M, Chen J, Englert J, Janes J, Leone R, et al. Abstract 2329: glutaminase inhibition with CB-839 enhances anti-tumor activity of
PD-1 and PD-L1 antibodies by overcoming a metabolic checkpoint blocking T cell activation. Cancer Research 2016;76:2329.
56. Study CB-839 in combination with nivolumab in patients with melanoma, ccRCC and NSCLC. Available from: https://clinicaltrials.
gov/ct2/show/NCT02771626. [Last accessed on 24 Apr 2019]
57. Emberley E, Bennett M, Chen J, Gross M, Huang T, et al. CB-839, a selective glutaminase inhibitor, has anti-tumor activity in
renal cell carcinoma and synergizes with cabozantinib and everolimus. Available from: https://www.calithera.com/wp-content/
uploads/2017/12/03.2017-Keystone-poster-Emberley-2017.pdf. [Last accessed on 24 Apr 2019]
58. Tannir N, Motzer R, Agarwal N, Liu P-Y, Whiting S, et al. CANTATA: a randomized phase 2 study of CB-839 in combination with
cabozantinib vs. placebo with cabozantinib in patients with advanced/metastatic renal cell carcinoma. J Clin Oncol 2018;36:TPS4601.
59. Halama A, Kulinski M, Dib SS, Zaghlool SB, Siveen KS, et al. Accelerated lipid catabolism and autophagy are cancer survival
mechanisms under inhibited glutaminolysis. Cancer Lett 2018;430:133-47.