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| | SAR Compounds tested by Dose Response Screen via Multiplex HTS Assay for Inhibitors of MEK Kinase PB1 Domains, specifically MEK5 binding to MEK Kinase 3 Wildtype. |
| Description: | University of New Mexico Assay Overview: Assay Support: 1R03MH084830-01 Project Title: TR-FRET HTS Assay for Inhibitors of MEKK2-MEK5 PB1 Domain Interaction PI: Kazuhiro Nakamura, Ph.D Center PI: Larry Sklar, Ph.D Assay Implementatiion: Zurab Surviladze Ph.D, Mark Haynes Ph.D, Anna Waller Ph.D, Mark Carter MS Assay Background and Significance: PB1 (Phox/Bem1p) domains function as protein-protein interaction sites by forming PB1-PB1 domain heterodimers (Moscat, et al. 2006). There are at least 20 human PB1 domain-containing proteins. Different PB1 domains contribute to the formation of specific protein complexes critical for biological responses including proliferation, apoptosis, cell polarity, and angiogenesis. These proteins include the mitogen/extracellular signal regulated kinase kinases MEKK2 and MEKK3 (MAP3Ks), as well as the downstream regulated kinase MEK5 (a MAP2K), which solely govern the ERK5 MAPK pathway involved in angiogenesis, cell growth and inhibition of apo |
| Affinity data for this assay | |
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