J Biomol Screen
Ewald JA, Peters N, Desotelle JA, Hoffmann FM, Jarrard DF
J Biomol Screen - vol. 14 853-858 (2009)
Ewald JA, Peters N, Desotelle JA, Hoffmann FM, Jarrard DF
J Biomol Screen - vol. 14 853-858 (2009)
Manuscript A, Formation HTF
- vol. 358 1-6 (2009)
Hutchinson D, Ho V, Dodd M, Dawson HN, Zumwalt AC, Colton CA
- vol. 148 825-832 (2008)
Winter SS, Lovato DM, Khawaja HM, Edwards BS, Steele ID, Young SM, Oprea TI, Sklar LA, Larson RS
Journal of biomolecular screening - vol. 13 185-93 (2008)
The overexpression of P-glycoprotein, encoded by the ATP Binding Cassette B1 (ABCB1) gene, contributes to multidrug resistance (MDR) and is considered one of the major obstacles to successful cancer chemotherapy. The authors previously developed a T-lineage acute lymphoblastic leukemia (T-ALL) cell line that overexpresses ABCB1 and exhibits MDR to daunorubicin (DNR), prednisolone, and vincristine. Using […]
Tribouillard-Tanvier D, Béringue V, Desban N, Gug F, Bach S, Voisset C, Galons H, Laude H, Vilette D, Blondel M
PLoS ONE - vol. 3 (2008)
BACKGROUND: Prion-based diseases are incurable transmissible neurodegenerative disorders affecting animals and humans.nnMETHODOLOGY/PRINCIPAL FINDINGS: Here we report the discovery of the in vivo antiprion activity of Guanabenz (GA), an agonist of alpha2-adrenergic receptors routinely used in human medicine as an antihypertensive drug. We isolated GA in a screen for drugs active in vivo against two different […]
Wu Z, Liu D, Sui Y
Journal of biomolecular screening - vol. 13 159-67 (2008)
The process of identifying active targets (hits) in high-throughput screening (HTS) usually involves 2 steps: first, removing or adjusting for systematic variation in the measurement process so that extreme values represent strong biological activity instead of systematic biases such as plate effect or edge effect and, second, choosing a meaningful cutoff on the calculated statistic […]
Senisterra GA, Soo Hong B, Park H, Vedadi M
Journal of biomolecular screening - vol. 13 337-42 (2008)
Many diseases in humans are caused by mutations that decrease the stability of specific proteins or increase their susceptibility to aggregation. Consequently, the availability of high-throughput methods for assessing protein stability and aggregation properties under physiological conditions (e.g., 37 degrees C) is necessary to analyze physicochemical properties under conditions that are closer to in vivo […]
Simeonov A, Jadhav A, Thomas CJ, Wang Y, Huang R, Southall NT, Shinn P, Smith J, Austin CP, Auld DS, Inglese J
Journal of Medicinal Chemistry - vol. 51 2363-2371 (2008)
Chromo/fluorophoric properties often accompany the heterocyclic scaffolds and impurities that comprise libraries used for high-throughput screening (HTS). These properties affect assay outputs obtained with optical detection, thus complicating analysis and leading to false positives and negatives. Here, we report the fluorescence profile of more than 70,000 samples across spectral regions commonly utilized in HTS. The […]
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 […]
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 […]
