Abstract

ASSAY DEVELOPMENT/ADAPTATION CORE In La Jolla, 600 square ft of laboratory space is dedicated to the MLPCN effort. The lab is configured for maximal use of space with the tissue culture room adjacent to the automation bench. The tissue culture room has two 6-foot biosafety cabinets. In addition, the PI has 2500 sq. ft lab space immediately below the assay development facility. The lab is fully equipped for cell and molecular biology and is used in assay development efforts requiring these capabilities. The tissue culture lab has a Zeiss Axiovert fluorescent microscope equipped with filters for visual detection of green fluorescence (FITC, GFP) and CCF2/4 (b-lactamase substrate) loaded cells. The ICND building has a core microscopy facility available for secondary assays (e.g. GPCR internalization) with the following equipment. ? Brightfield and fluorescence microscopes ? Dissecting stereoscope with color camera ? Calcium imaging automated system with micromanipulator for cell picking Olympus confocal laser-scanning microscope with 4 laser lines ? DeltaVision deconvolution acquisition system ? Spinning-disk confocal microscope (2 laser lines) with incubator chamber for live-cell fluorescence microscopy ? Live-cell brightfield microscope with incubator ? Eppendorf microinjection system on inverted fluorescence microscope ? MetaMorph 6.5 acquisition and image analysis software

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute of Mental Health (NIMH)
Type
Specialized Center--Cooperative Agreements (U54)
Project #
5U54MH084512-06
Application #
8525451
Study Section
Special Emphasis Panel (ZRG1-BCMB-D)
Project Start
Project End
Budget Start
2013-06-01
Budget End
2014-05-31
Support Year
6
Fiscal Year
2013
Total Cost
$1,795,929
Indirect Cost
$1,016,697

  Institution

Name
Scripps Research Institute
Department
Type
DUNS #
781613492
City
La Jolla
State
CA
Country
United States
Zip Code
92037

  Publications

Swingle, Mark; Volmar, Claude-Henry; Saldanha, S Adrian et al. (2017) An Ultra-High-Throughput Screen for Catalytic Inhibitors of Serine/Threonine Protein Phosphatases Types 1 and 5 (PP1C and PP5C). SLAS Discov 22:21-31
Dusaban, Stephanie S; Chun, Jerold; Rosen, Hugh et al. (2017) Sphingosine 1-phosphate receptor 3 and RhoA signaling mediate inflammatory gene expression in astrocytes. J Neuroinflammation 14:111
Darrah, Erika; Kim, AeRyon; Zhang, Xi et al. (2017) Proteolysis by Granzyme B Enhances Presentation of Autoantigenic Peptidylarginine Deiminase 4 Epitopes in Rheumatoid Arthritis. J Proteome Res 16:355-365
Fanning, Sean W; Mayne, Christopher G; Dharmarajan, Venkatasubramanian et al. (2016) Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation. Elife 5:
Sanna, M Germana; Vincent, Kevin P; Repetto, Emanuela et al. (2016) Bitopic Sphingosine 1-Phosphate Receptor 3 (S1P3) Antagonist Rescue from Complete Heart Block: Pharmacological and Genetic Evidence for Direct S1P3 Regulation of Mouse Cardiac Conduction. Mol Pharmacol 89:176-86
Wood, Michael R; Noetzel, Meredith J; Tarr, James C et al. (2016) Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition. Bioorg Med Chem Lett 26:4282-6
Teijaro, John R; Studer, Sean; Leaf, Nora et al. (2016) S1PR1-mediated IFNAR1 degradation modulates plasmacytoid dendritic cell interferon-? autoamplification. Proc Natl Acad Sci U S A 113:1351-6
Madoux, Franck; Dreymuller, Daniela; Pettiloud, Jean-Phillipe et al. (2016) Discovery of an enzyme and substrate selective inhibitor of ADAM10 using an exosite-binding glycosylated substrate. Sci Rep 6:11
Pan, Xiaohong; Yang, Chunying; Cleveland, John L et al. (2016) Synthesis and Cytoxicity of Sempervirine and Analogues. J Org Chem 81:2194-200
Wood, Michael R; Noetzel, Meredith J; Engers, Julie L et al. (2016) Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. Bioorg Med Chem Lett 26:3029-3033

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