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MeSH Review

Drug Evaluation, Preclinical

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Disease relevance of Drug Evaluation, Preclinical


High impact information on Drug Evaluation, Preclinical

  • The finding that presenilin itself may be the long-sought gamma-secretase, coupled with the recent identification of beta-secretase, has provided discrete biochemical targets for drug screening and development [6].
  • The efficacy of preemployment drug screening for marijuana and cocaine in predicting employment outcome [7].
  • Drug screenings performed on all patients showed the presence of a cocaine metabolite and the absence of acetaminophen, alcohol, and other potential toxins [8].
  • By testing 58 tumor cell lines of the National Cancer Institute's anticancer drug-screening panel for apoptosis sensitivity to S2 and performing death-inducing signaling complex analyses, we determined that half of the CD95-sensitive cells are type I and half are type II [9].
  • A native or engineered cysteine in a protein is allowed to react reversibly with a small library of disulfide-containing molecules ( approximately 1,200 compounds) at concentrations typically used in drug screening (10 to 200 microM) [10].

Chemical compound and disease context of Drug Evaluation, Preclinical


Biological context of Drug Evaluation, Preclinical


Anatomical context of Drug Evaluation, Preclinical

  • Identification of MDR cell lines used for large-scale in vitro anticancer drug screening will facilitate interpretation of data in a way which may allow identification of new drug leads of potential value in treatment of MDR tumor cell populations [17].
  • Electrical kindling via unilateral implanted depth electrodes in rats is currently the most commonly used model for temporal lobe epilepsy, but the use of this model in drug screening for the identification of novel anticonvulsants is markedly hampered by the laborious and time-consuming preparation and the size of the animals [18].
  • To develop a drug screening system, we introduced expression vectors carrying the mouse N-methyl-D-aspartate (NMDA) receptor channel epsilon1 and zeta1 subunit cDNAs under the promoter of the Drosophila heat shock protein hsp70 into Chinese hamster ovary (CHO) cells [19].
  • Targeted drug screening revealed a compound, Ruthenium Red, which potently blocked proliferation of human T-cells [20].
  • The possible bifunctional activity of the Neutral Red assay as a test for cellular viability and estimating the DNA content of hybridoma cells is discussed along with its application in a drug screening programme [21].

Associations of Drug Evaluation, Preclinical with chemical compounds

  • Some of the subjects with postdexamethasone cortisol increases reported drug discontinuation in the drug histories they gave at admission, but in three, drug screening provided the only evidence of prior drug use [22].
  • Glutathione-associated enzymes in the human cell lines of the National Cancer Institute Drug Screening Program [23].
  • This technique has potential applications in drug screening, such as measuring the dose-response curve of isoproterenol, a beta-adrenergic agonist with a positive chronotropic effect [24].
  • Univariate analyses of aggregates of urine drug screening showed generally favorable outcomes for baclofen, but not at statistically significant levels [25].
  • In response to the need for rapid, inexpensive, high-throughput assays for antimycobacterial drug screening, a microplate-based assay which uses Alamar blue reagent for determination of growth was evaluated [26].

Gene context of Drug Evaluation, Preclinical

  • Here, we described a novel drug screening system designated to detect compounds that inhibit the function of Pdr5 [27].
  • Repression of Nrf2-mediated transcription by E(2)-bound ERalpha expands our knowledge of E(2)-regulated genes and provides a potential drug-screening target for the development of selective estrogen receptor modulators with a lower risk of causing cancer [28].
  • These results strongly support the conclusion that recombinant human DBH from Drosophila S2 cells can be used in place of human neuroblastoma-derived DBH for drug screening, characterization of the enzyme's physicochemical properties, and determination of structure-function relationships [29].
  • An amperometric biosensor with human CYP3A4 as a novel drug screening tool [30].
  • Interlocking MELK with the drug screening machinery provides new clues related to the selection of target proteins, and functionally relevant hits and drug leads [31].

Analytical, diagnostic and therapeutic context of Drug Evaluation, Preclinical


  1. Development of a panel of 15 human ovarian cancer xenografts for drug screening and determination of the role of the glutathione detoxification system. Kolfschoten, G.M., Pinedo, H.M., Scheffer, P.G., Schlüper, H.M., Erkelens, C.A., Boven, E. Gynecol. Oncol. (2000) [Pubmed]
  2. A clinical screening program for topical chemotherapeutic drugs in psoriasis. Weinstein, G.D., McCullough, J.L., Eaglstein, W.H., Golub, A., Cornell, R.C., Stoughton, R.B., Clendenning, W., Zackheim, H., Maibach, H., Kulp, K.R., King, L., Baden, H.P., Taylor, J.S., Deneau, D.D. Archives of dermatology. (1981) [Pubmed]
  3. Generation of the replication-competent human immunodeficiency virus type 1 which expresses a jellyfish green fluorescent protein. Lee, A.H., Han, J.M., Sung, Y.C. Biochem. Biophys. Res. Commun. (1997) [Pubmed]
  4. Carbon monoxide (CO)-induced hypoxia in mice: evaluation as an experimental model of cerebral ischemia for drug screening. Koida, M., Nakamuta, H., Yasuda, K., Muguruma, K., Hiramatsu, Y., Ogawa, Y., Kato, Y. Jpn. J. Pharmacol. (1989) [Pubmed]
  5. Pharmacologic treatment of autonomic dysreflexia in the rat. Chiou-Tan, F.Y., Lenz, M.L., Robertson, C.S., Grabois, M. American journal of physical medicine & rehabilitation / Association of Academic Physiatrists. (1994) [Pubmed]
  6. Alzheimer's disease: genes, proteins, and therapy. Selkoe, D.J. Physiol. Rev. (2001) [Pubmed]
  7. The efficacy of preemployment drug screening for marijuana and cocaine in predicting employment outcome. Zwerling, C., Ryan, J., Orav, E.J. JAMA (1990) [Pubmed]
  8. Histopathology of cocaine hepatotoxicity. Report of four patients. Wanless, I.R., Dore, S., Gopinath, N., Tan, J., Cameron, R., Heathcote, E.J., Blendis, L.M., Levy, G. Gastroenterology (1990) [Pubmed]
  9. Two CD95 tumor classes with different sensitivities to antitumor drugs. Algeciras-Schimnich, A., Pietras, E.M., Barnhart, B.C., Legembre, P., Vijayan, S., Holbeck, S.L., Peter, M.E. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  10. Site-directed ligand discovery. Erlanson, D.A., Braisted, A.C., Raphael, D.R., Randal, M., Stroud, R.M., Gordon, E.M., Wells, J.A. Proc. Natl. Acad. Sci. U.S.A. (2000) [Pubmed]
  11. Antitumor activity of a new platinum compound (glycolate-o,o') diammineplatinum (II) (254-S), against non-small cell lung carcinoma grown in a human tumor clonogenic assay system. Kanzawa, F., Matsushima, Y., Nakano, H., Nakagawa, K., Takahashi, H., Sasaki, Y., Saijo, N. Anticancer Res. (1988) [Pubmed]
  12. Studies on human colon cancer gene APC by targeted expression in Drosophila. Bhandari, P., Shashidhara, L.S. Oncogene (2001) [Pubmed]
  13. Impact of lowering the screening and confirmation cutoff values for urine drug testing based on dilution indicators. Fraser, A.D., Zamecnik, J. Therapeutic drug monitoring. (2003) [Pubmed]
  14. Atherosclerotic plaque rupture: emerging insights and opportunities. Plutzky, J. Am. J. Cardiol. (1999) [Pubmed]
  15. Predictive relationships for the effects of triglyceride ester concentration and water uptake on solubility and partitioning of small molecules into lipid vehicles. Cao, Y., Marra, M., Anderson, B.D. Journal of pharmaceutical sciences. (2004) [Pubmed]
  16. Detection of a decrease in green fluorescent protein fluorescence for the monitoring of cell death: an assay amenable to high-throughput screening technologies. Steff, A.M., Fortin, M., Arguin, C., Hugo, P. Cytometry. (2001) [Pubmed]
  17. Multidrug-resistant phenotype of disease-oriented panels of human tumor cell lines used for anticancer drug screening. Wu, L., Smythe, A.M., Stinson, S.F., Mullendore, L.A., Monks, A., Scudiero, D.A., Paull, K.D., Koutsoukos, A.D., Rubinstein, L.V., Boyd, M.R. Cancer Res. (1992) [Pubmed]
  18. Corneal kindling in mice: behavioral and pharmacological differences to conventional kindling. Potschka, H., Löscher, W. Epilepsy Res. (1999) [Pubmed]
  19. Inducible expression of N-methyl-D-aspartate (NMDA) receptor channels from cloned cDNAs in CHO cells. Uchino, S., Kudo, Y., Watanabe, W., Nakajima-Iijima, S., Mishina, M. Brain Res. Mol. Brain Res. (1997) [Pubmed]
  20. Ruthenium Red potently inhibits immune responses both in vitro and in vivo. Dwyer, D.S., Gordon, K., Jones, B. Int. J. Immunopharmacol. (1995) [Pubmed]
  21. The determination of cellular viability of hybridoma cells in microtitre plates: a colorimetric assay based on neutral red. Modha, K., Whiteside, J.P., Spier, R.E. Cytotechnology. (1993) [Pubmed]
  22. Psychotropic drug withdrawal and the dexamethasone suppression test. Kraus, R.P., Hux, M., Grof, P. The American journal of psychiatry. (1987) [Pubmed]
  23. Glutathione-associated enzymes in the human cell lines of the National Cancer Institute Drug Screening Program. Tew, K.D., Monks, A., Barone, L., Rosser, D., Akerman, G., Montali, J.A., Wheatley, J.B., Schmidt, D.E. Mol. Pharmacol. (1996) [Pubmed]
  24. Cell-transistor hybrid systems and their potential applications. Offenhäusser, A., Knoll, W. Trends Biotechnol. (2001) [Pubmed]
  25. Randomized placebo-controlled trial of baclofen for cocaine dependence: preliminary effects for individuals with chronic patterns of cocaine use. Shoptaw, S., Yang, X., Rotheram-Fuller, E.J., Hsieh, Y.C., Kintaudi, P.C., Charuvastra, V.C., Ling, W. The Journal of clinical psychiatry. (2003) [Pubmed]
  26. Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium. Collins, L., Franzblau, S.G. Antimicrob. Agents Chemother. (1997) [Pubmed]
  27. A novel screening for inhibitors of a pleiotropic drug resistant pump, Pdr5, in Saccharomyces cerevisiae. Hiraga, K., Wanigasekera, A., Sugi, H., Hamanaka, N., Oda, K. Biosci. Biotechnol. Biochem. (2001) [Pubmed]
  28. Repression of cancer protective genes by 17beta-estradiol: ligand-dependent interaction between human Nrf2 and estrogen receptor alpha. Ansell, P.J., Lo, S.C., Newton, L.G., Espinosa-Nicholas, C., Zhang, D.D., Liu, J.H., Hannink, M., Lubahn, D.B. Mol. Cell. Endocrinol. (2005) [Pubmed]
  29. Expression of human dopamine beta-hydroxylase in Drosophila Schneider 2 cells. Li, B., Tsing, S., Kosaka, A.H., Nguyen, B., Osen, E.G., Bach, C., Chan, H., Barnett, J. Biochem. J. (1996) [Pubmed]
  30. An amperometric biosensor with human CYP3A4 as a novel drug screening tool. Joseph, S., Rusling, J.F., Lvov, Y.M., Friedberg, T., Fuhr, U. Biochem. Pharmacol. (2003) [Pubmed]
  31. Topological proteomics, toponomics, MELK-technology. Schubert, W. Adv. Biochem. Eng. Biotechnol. (2003) [Pubmed]
  32. Carisoprodol: an unrecognized drug of abuse. Bailey, D.N., Briggs, J.R. Am. J. Clin. Pathol. (2002) [Pubmed]
  33. HMG-CoA reductase inhibitors and P-glycoprotein modulation. Bogman, K., Peyer, A.K., Török, M., Küsters, E., Drewe, J. Br. J. Pharmacol. (2001) [Pubmed]
  34. Phase I trial of combination therapy of cancer with N-phosphonacetyl-L-aspartic acid and dipyridamole. Markman, M., Chan, T.C., Cleary, S., Howell, S.B. Cancer Chemother. Pharmacol. (1987) [Pubmed]
  35. Urine drug screening for cocaine after lacrimal surgery. Cruz, O.A., Patrinely, J.R., Reyna, G.S., King, J.W. Am. J. Ophthalmol. (1991) [Pubmed]
  36. MDA-MDMA concentrations in urine specimens. Kunsman, G.W., Levine, B., Kuhlman, J.J., Jones, R.L., Hughes, R.O., Fujiyama, C.I., Smith, M.L. Journal of analytical toxicology. (1996) [Pubmed]
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