Molecule Inhibitors of the Mitotic Kinase Haspin By High-Throughput Screening Using a Homogeneous Time-Resolved Fluorescence Resonance Energy Transfer Assay

Journal of biomolecular screening

Patnaik D, Xian J
Journal of biomolecular screening - vol. 13 1025-1034 (2008)

A high-throughput screening strategy identifies cardiotonic steroids as alternative splicing modulators

Proceedings of the National Academy of Sciences

Stoilov P, Lin C, Damoiseaux R, Nikolic J, Black DL
Proceedings of the National Academy of Sciences - vol. 105 11218-11223 (2008)

10.1073/pnas.0801661105 Alternative splicing has emerged as a promising therapeutic target in a number of human disorders. However, the discovery of compounds that target the splicing reaction has been hindered by the lack of suitable high-throughput screening assays. Conversely, the effects of known drugs on the splicing reaction are mostly unclear and not routinely assessed. We […]

A High-Throughput Screening Assay for Small Molecules

Krysan DJ, Didone L

Homogeneous time-resolved fluorescence resonance energy transfer assay for measurement of Phox/Bem1p (PB1) domain heterodimerization.

Journal of biomolecular screening

Nakamura K, Zawistowski JS, Hughes MA, Sexton JZ, Yeh L, Johnson GL, Scott JE
Journal of biomolecular screening - vol. 13 396-405 (2008)

Twenty human proteins encode Phox/Bem1p (PB1) domains, which are involved in forming protein heterodimers. MEKK2, MEKK3, and MEK5 are 3 serine-threonine protein kinases that have PB1 domains. MEKK2, MEKK3, and MEK5 are the MAP3Ks and the MAP2K in the ERK5 mitogen-activated protein kinase (MAPK) signaling module. ERK5 is a critical MAPK for both development of […]

Protein Folding Activity of Ribosomal RNA Is a Selective Target of Two Unrelated Antiprion Drugs


D T, Reis SD, Gug F, Huang C, Sabate R, Kikovska E, Talarek N, Vilette D
PLoS ONE - vol. 3 (2008)

Assay for therapies that inhibit expression of the cytosolic CU/ZN superoxide dismutase (SOD1) gene

Brown RH, Broom W
- vol. 1 (2008)

Identification of Chemical Inhibitors to Human Tissue Transglutaminase by Screening Existing Drug Libraries

Chemistry and Biology

Lai TS, Liu Y, Tucker T, Daniel KR, Sane DC, Toone E, Burke JR, Strittmatter WJ, Greenberg CS
Chemistry and Biology - vol. 15 969-978 (2008)

Human tissue transglutaminase (TGM2) is a calcium-dependent crosslinking enzyme involved in the posttranslational modification of intra- and extracellular proteins and implicated in several neurodegenerative diseases. To find specific inhibitors to TGM2, two structurally diverse chemical libraries (LOPAC and Prestwick) were screened. We found that ZM39923, a Janus kinase inhibitor, and its metabolite ZM449829 were the […]

High-throughput flow cytometry to detect selective inhibitors of ABCB1, ABCC1, and ABCG2 transporters.

Assay and drug development technologies

Ivnitski-Steele I, Larson RS, Lovato DM, Khawaja HM, Winter SS, Oprea TI, Sklar LA, Edwards BS
Assay and drug development technologies - vol. 6 263-276 (2008)

Up-regulation of pump (transporter) expression and selection of resistant cancer cells result in cancer multidrug resistance to diverse substrates of these transporters. While more than 48 members of the ATP binding cassette (ABC) transporter superfamily have been identified, up to now only three human ABC transporters-ABCB1, ABCC1, and ABCG2-have unambiguously been shown to contribute to […]

A high-content chemical screen identifies ellipticine as a modulator of p53 nuclear localization


Xu GW, Mawji IA, Macrae CJ, Koch CA, Datti A, Wrana JL, Dennis JW, Schimmer AD
Apoptosis - vol. 13 413-422 (2008)

p53 regulates apoptosis and the cell cycle through actions in the nucleus and cytoplasm. Altering the subcellular localization of p53 can alter its biological function. Therefore, small molecules that change the localization of p53 would be useful chemical probes to understand the influence of subcellular localization on the function of p53. To identify such molecules, […]

Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade

PLoS Neglected Tropical Diseases

Simeonov A, Jadhav A, Sayed AA, Wang Y, Nelson ME, Thomas CJ, Inglese J, Williams DL, Austin CP
PLoS Neglected Tropical Diseases - vol. 2 (2008)

Schistosomiasis is a tropical disease associated with high morbidity and mortality, currently affecting over 200 million people worldwide. Praziquantel is the only drug used to treat the disease, and with its increased use the probability of developing drug resistance has grown significantly. The Schistosoma parasites can survive for up to decades in the human host […]