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Global Translational Medicine Role of HTS in cancer therapeutics

91. Lin X, Huang XP, Chen G, et al. Life beyond kinases: Structure‑ 102. Van’t Veer LJ, Bernards R. Enabling personalized cancer
based discovery of sorafenib as nanomolar antagonist of medicine through analysis of gene-expression patterns.
5-HT receptors. J Med Chem. 2012;55(12):5749‑5759. Nature. 2008;452(7187):564‑570.
doi: 10.1021/jm300338m doi: 10.1038/nature06915
92. Schneidewind T, Brause A, Pahl A, et al. Morphological 103. Bertos NR, Park M. Breast cancer‑one term, many entities?
profiling identifies a common mode of action for J Clin Invest. 2011;121(10):3789‑3796.
small molecules with different targets. Chembiochem.
2020;21(22):3197‑3207. doi: 10.1172/JCI57100
104. Huang E, Ishida S, Pittman J, et al. Gene expression
doi: 10.1002/cbic.202000381
phenotypic models that predict the activity of oncogenic
93. Han X, Zhou C, Jiang M, et al. Discovery of RG7834: The pathways. Nat Genet. 2003;34(2):226‑230.
first-in-class selective and orally available small molecule
hepatitis B virus expression inhibitor with novel mechanism doi: 10.1038/ng1167
of action. J Med Chem. 2018;61(23):10619‑10634. 105. Loboda A, Nebozhyn M, Klinghoffer R, et al. A gene
doi: 10.1021/acs.jmedchem.8b01245 expression signature of RAS pathway dependence predicts
response to PI3K and RAS pathway inhibitors and expands
94. Moffat JG, Vincent F, Lee JA, Eder J, Prunotto M. the population of RAS pathway activated tumors. BMC
Opportunities and challenges in phenotypic drug Med Genomics. 2010;3(1):26.
discovery: An industry perspective. Nat Rev Drug Discov.
2017;16(8):531‑543. doi: 10.1186/1755‑8794‑3‑26
doi: 10.1038/nrd.2017.111 106. Loboda A, Nebozhyn MV, Watters JW, et al. EMT is the
dominant program in human colon cancer. BMC Med
95. Vincent F, Loria PM, Weston AD, et al. Hit triage and Genomics. 2011;4(1):9.
validation in phenotypic screening: Considerations and
strategies. Cell Chem Biol. 2020;27(11):1332‑1346. doi: 10.1186/1755‑8794‑4‑9
doi: 10.1016/j.chembiol.2020.08.009 107. Méndez‑Lucio O, Naveja JJ, Vite‑Caritino H, Prieto‑
Martínez FD, Medina‑Franco JL. One drug for multiple
96. Warchal SJ, Unciti‑Broceta A, Carragher NO. Next‑ targets: A computational perspective. J Mex Chem Soc.
generation phenotypic screening. Future Med Chem. 2016;60(3):168‑181.
2016;8(11):1331‑1347.
doi: 10.29356/jmcs.v60i3.100
doi: 10.4155/fmc‑2016‑0025
108. Hsieh JH, Smith‑Roe SL, Huang R, et al. Identifying
97. Comess KM, McLoughlin SM, Oyer JA, et al. Emerging compounds with genotoxicity potential using Tox21
approaches for the identification of protein targets of high‑throughput screening assays. Chem Res Toxicol.
small molecules-a practitioners’ perspective. J Med Chem. 2019;32(7):1384‑1401.
2018;61(19):8504‑8535.
doi: 10.1021/acs.chemrestox.9b00053
doi: 10.1021/acs.jmedchem.7b01921
109. Michod D, Widmann C. DNA‑damage sensitizers: Potential
98. Lee J, Bogyo M. Target deconvolution techniques in modern new therapeutical tools to improve chemotherapy. Crit
phenotypic profiling. Curr Opin Chem Biol. 2013;17(1):118‑126. Rev Oncol Hematol. 2007;63(2):160‑171.
doi: 10.1016/j.cbpa.2012.12.022 doi: 10.1016/j.critrevonc.2007.04.003
99. Lu JJ, Pan W, Hu YJ, Wang YT. Multi‑target drugs: the 110. Evans TJ, Yamamoto KN, Hirota K, Takeda S. Mutant cells
trend of drug research and development. PLoS One. defective in DNA repair pathways provide a sensitive high-
2012;7(6):e40262. throughput assay for genotoxicity. DNA Repair (Amst).
doi: 10.1371/journal.pone.0040262 2010;9(12):1292‑1298.
100. Rena G, Hardie DG, Pearson ER. The mechanisms of doi: 10.1016/j.dnarep.2010.09.017
action of metformin. Diabetologia. 2017;60(9):1577‑1585.
111. Ji K, Kogame T, Choi K, et al. A novel approach using DNA‑
doi: 10.1007/s00125‑017‑4342‑z repair-deficient chicken DT40 cell lines for screening and
characterizing the genotoxicity of environmental contaminants.
101. Keller MP, Attie AD. Physiological insights gained from
gene expression analysis in obesity and diabetes. Annu Rev Environ Health Perspect. 2009;117(11):1737‑1744.
Nutr. 2010;30:341‑364. doi: 10.1289/ehp.0900842
doi: 10.1146/annurev.nutr.012809.104747 112. Buerstedde JM, Takeda S. Increased ratio of targeted to

Volume 3 Issue 1 (2024) 18 https://doi.org/10.36922/gtm.2448