Page 38 - Read Online
P. 38
Conroy et al. Cancer Drug Resist 2021;4:543-58 https://dx.doi.org/10.20517/cdr.2021.07 Page 15
(ARRY-142886) versus pemetrexed in patients with non-small cell lung cancer who have failed one or two prior chemotherapeutic
regimens. J Thorac Oncol 2010;5:1630-6. DOI PubMed
52. Kinsey CG, Camolotto SA, Boespflug AM, et al. Protective autophagy elicited by RAF→MEK→ERK inhibition suggests a treatment
strategy for RAS-driven cancers. Nat Med 2019;25:620-7. DOI PubMed
53. Yang S, Wang X, Contino G, et al. Pancreatic cancers require autophagy for tumor growth. Genes Dev 2011;25:717-29. DOI PubMed
PMC
54. Rahib L, Chen K, Ocean AJ, et al. Use of a real-world data approach to rapidly generate outcomes data following a case study of a
novel treatment combination in pancreatic adenocarcinoma. J Clin Oncol 2020;38:e16735. DOI
55. Moschos SJ, Sullivan RJ, Hwu WJ, et al. Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with
advanced solid tumors. JCI Insight 2018;3:92352. DOI PubMed PMC
56. Merchant M, Moffat J, Schaefer G, et al. Combined MEK and ERK inhibition overcomes therapy-mediated pathway reactivation in
RAS mutant tumors. PLoS ONE 2017;12:e0185862. DOI PubMed PMC
57. Weekes C, Lockhart A, LoRusso P, et al. A Phase Ib Study to Evaluate the MEK Inhibitor Cobimetinib in Combination with the
ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors. Oncologist 2020;25:833-e1438. DOI PubMed PMC
58. Varga A, Soria JC, Hollebecque A, et al. A First-in-Human Phase I Study to Evaluate the ERK1/2 Inhibitor GDC-0994 in Patients with
Advanced Solid Tumors. Clin Cancer Res 2020;26:1229-36. DOI PubMed
59. Sullivan RJ, Infante JR, Janku F, et al. First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant
Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study. Cancer Discov 2018;8:184-95. DOI PubMed
60. Bhagwat SV, McMillen WT, Cai S, et al. ERK Inhibitor LY3214996 Targets ERK Pathway-Driven Cancers: A Therapeutic Approach
Toward Precision Medicine. Mol Cancer Ther 2020;19:325-36. DOI PubMed
61. Burrows F, Kessler L, Chen J, et al. Abstract 5168: KO-947, a potent ERK inhibitor with robust preclinical single agent activity in
MAPK pathway dysregulated tumors. Cancer Research 2017;77 (13 Supplement):5168. DOI
62. Britten CD. PI3K and MEK inhibitor combinations: examining the evidence in selected tumor types. Cancer Chemother Pharmacol
2013;71:1395-409. DOI PubMed
63. Belmont PJ, Jiang P, McKee TD, et al. Resistance to dual blockade of the kinases PI3K and mTOR in KRAS-mutant colorectal cancer
models results in combined sensitivity to inhibition of the receptor tyrosine kinase EGFR. Sci Signal 2014;7:ra107. DOI PubMed
64. Mohan S, Vander Broek R, Shah S, et al. MEK Inhibitor PD-0325901 Overcomes Resistance to PI3K/mTOR Inhibitor PF-5212384
and Potentiates Antitumor Effects in Human Head and Neck Squamous Cell Carcinoma. Clin Cancer Res 2015;21:3946-56. DOI
PubMed PMC
65. Shapiro GI, LoRusso P, Kwak E, et al. Phase Ib study of the MEK inhibitor cobimetinib (GDC-0973) in combination with the PI3K
inhibitor pictilisib (GDC-0941) in patients with advanced solid tumors. Invest New Drugs 2020;38:419-32. DOI PubMed
66. Aoki M, Batista O, Bellacosa A, Tsichlis P, Vogt PK. The akt kinase: molecular determinants of oncogenicity. Proc Natl Acad Sci U S
A 1998;95:14950-5. DOI PubMed PMC
67. Tolcher AW, Kurzrock R, Valero V, et al. Phase I dose-escalation trial of the oral AKT inhibitor uprosertib in combination with the
oral MEK1/MEK2 inhibitor trametinib in patients with solid tumors. Cancer Chemother Pharmacol 2020;85:673-83. DOI PubMed
68. Kessler D, Bergner A, Böttcher J, et al. Drugging all RAS isoforms with one pocket. Future Med Chem 2020;12:1911-23. DOI
PubMed
69. Kessler D, Gmachl M, Mantoulidis A, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A 2019;116:15823-9.
DOI PubMed PMC
70. Taveras A, Remiszewski S, Doll R, et al. Ras oncoprotein inhibitors: The discovery of potent, ras nucleotide exchange inhibitors and
the structural determination of a drug-protein complex. Bioorganic & Medicinal Chemistry 1997;5:125-33. DOI PubMed
71. Karaguni IM, Herter P, Debruyne P, et al. The new sulindac derivative IND 12 reverses Ras-induced cell transformation. Cancer Res
2002;62:1718-23. PubMed
72. Lim SM, Westover KD, Ficarro SB, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem
Int Ed Engl 2014;53:199-204. DOI PubMed PMC
73. 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. DOI PubMed PMC
74. Gehringer M, Laufer SA. Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal
Chemistry and Chemical Biology. J Med Chem 2019;62:5673-724. DOI PubMed
75. Janes MR, Zhang J, Li LS, et al. Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor. Cell 2018;172:578-
589.e17. DOI PubMed
76. Patricelli MP, Janes MR, Li LS, et al. Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive
State. Cancer Discov 2016;6:316-29. DOI PubMed
77. Canon J, Rex K, Saiki AY, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature 2019;575:217-
23. DOI PubMed
78. Hong DS, Fakih MG, Strickler JH, et al. KRAS G12C Inhibition with Sotorasib in Advanced Solid Tumors. N Engl J Med
2020;383:1207-17. DOI PubMed PMC
79. Saiki A. Y GK, Rex K, Achanta P, San Miguel T, Koppada N et al. Discovery and in vitro characterization of AMG 510-a potent and
selective covalent small-molecule inhibitor of KRASG12C [abstract]. Proceedings of AACR Annual Meeting; 2019 Mar 29-Apr 3;
Atlanta, GA; 2019.
80. Hallin J, Engstrom LD, Hargis L, et al. The KRAS G12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of