Page 23 - GTM-3-1

Global Translational Medicine Role of HTS in cancer therapeutics

22. Koeberle A, Werz O. Multi-target approach for Vicente F. Current screening methodologies in drug
natural products in inflammation. Drug Discov Today. discovery for selected human diseases. Mar Drugs.
2014;19(12):1871‑1882. 2018;16(8):279.
doi: 10.1016/j.drudis.2014.08.006 doi: 10.3390/md16080279
23. Konecny GE, Pegram MD, Venkatesan N, et al. Activity 34. Sriram K, Insel PA. G Protein-coupled receptors as targets
of the dual kinase inhibitor lapatinib (GW572016) against for approved drugs: How many targets and how many
HER-2-overexpressing and trastuzumab-treated breast drugs? Mol Pharmacol. 2018;93(4):251‑258.
cancer cells. Cancer Res. 2006;66(3):1630‑1639. doi: 10.1124/mol.117.111062
doi: 10.1158/0008‑5472.Can‑05‑1182 35. Kenny CH, Ding W, Kelleher K, et al. Development of a
24. Flinn IW, O’Brien S, Kahl B, et al. Duvelisib, a novel oral fluorescence polarization assay to screen for inhibitors of the
dual inhibitor of PI3K-δ,γ, is clinically active in advanced FtsZ/ZipA interaction. Anal Biochem. 2003;323(2):224‑233.
hematologic malignancies. Blood. 2018;131(8):877‑887. doi: 10.1016/j.ab.2003.08.033
doi: 10.1182/blood‑2017‑05‑786566 36. Burns S, Travers J, Collins I, et al. Identification of small-
25. Murai R, Yoshida Y, Muraguchi T, et al. A novel screen using molecule inhibitors of protein kinase B (PKB/AKT) in
the Reck tumor suppressor gene promoter detects both an AlphaScreen™ high‑throughput screen. SLAS Discov.
conventional and metastasis-suppressing anticancer drugs. 2006;11(7):822‑827.
Oncotarget. 2010;1(4):252‑264. doi: 10.1177/1087057106290992
26. Herrmann IK, Wood MJA, Fuhrmann G. Extracellular 37. Sudo K, Yamaji K, Kawamura K, et al. High-throughput
vesicles as a next-generation drug delivery platform. Nat screening of low molecular weight NS3-NS4A protease
Nanotechnol. 2021;16(7):748‑759. inhibitors using a fluorescence resonance energy transfer
doi: 10.1038/s41565‑021‑00931‑2 substrate. Antivir Chem Chemother. 2005;16(6):385‑392.
27. Ohtaka H, Velázquez‑Campoy A, Xie D, Freire E. doi: 10.1177/095632020501600605
Overcoming drug resistance in HIV‑1 chemotherapy: The 38. Swaney S, McCroskey M, Shinabarger D, Wang Z,
binding thermodynamics of Amprenavir and TMC‑126 to Turner BA, Parker CN. Characterization of a high‑
wild-type and drug-resistant mutants of the HIV-1 protease. throughput screening assay for inhibitors of elongation
Protein Sci. 2002;11(8):1908‑1916. factor P and ribosomal peptidyl transferase activity. J Biomol
doi: 10.1110/ps.0206402 Screen. 2006;11(7):736‑742.
28. Wei F, Wang S, Gou X. A review for cell‑based screening doi: 10.1177/1087057106291634
methods in drug discovery. Biophys Rep. 2021;7(6):504‑516. 39. Allen M, Reeves J, Mellor G. High throughput fluorescence
doi: 10.52601/bpr.2021.210042 polarization: A homogeneous alternative to radioligand
binding for cell surface receptors. J Biomol Screen.
29. Pathe-Neuschäfer-Rube A, Neuschäfer-Rube F, Püschel GP. 2000;5(2):63‑69.
Cell‑based reporter release assay to determine the activity
of calcium-dependent neurotoxins and neuroactive doi: 10.1177/108705710000500202
pharmaceuticals. Toxins (Basel). 2021;13(4):247. 40. Xu J, Wang X, Ensign B, et al. Ion‑channel assay technologies:
doi: 10.3390/toxins13040247 Quo vadis? Drug Discov Today. 2001;6(24):1278‑1287.
30. Sanookpan K, Nonpanya N, Sritularak B, Chanvorachote P. doi: 10.1016/s1359‑6446(01)02095‑5
Ovalitenone inhibits the migration of lung cancer cells 41. Parker GJ, Law TL, Lenoch FJ, Bolger RE. Development
via the suppression of AKT/mTOR and epithelial-to- of high throughput screening assays using fluorescence
mesenchymal transition. Molecules. 2021;26(3):638. polarization: Nuclear receptor‑ligand‑binding and kinase/
phosphatase assays. J Biomol Screen. 2000;5(2):77‑88.
doi: 10.3390/molecules26030638
doi: 10.1177/108705710000500204
31. An WF, Tolliday N. Cell‑based assays for high‑throughput
screening. Mol Biotechnol. 2010;45(2):180‑186. 42. Bagal SK, Brown AD, Cox PJ, et al. Ion channels as
therapeutic targets: A drug discovery perspective. J Med
doi: 10.1007/s12033‑010‑9251‑z
Chem. 2013;56(3):593‑624.
32. Takenaka T. Classical vs reverse pharmacology in drug doi: 10.1021/jm3011433
discovery. BJU Int. 2001;88 Suppl 2:7‑10; discussion 49‑50.
43. Morachis JM, Huang R, Emerson BM. Identification of
doi: 10.1111/j.1464‑410x.2001.00112.x
kinase inhibitors that target transcription initiation by RNA
33. Lage OM, Ramos MC, Calisto R, Almeida E, Vasconcelos V, polymerase II. Oncotarget. 2011;2(1‑2):18‑28.

Volume 3 Issue 1 (2024) 15 https://doi.org/10.36922/gtm.2448