Abstract

DMPK COREThe DMPK core provides enabling technologies and capabilities to support the discovery of new chemicalentities, ranging from in vitro ADMET assays to in vivo pharmacokinetics in rats and mice. In vitro assaysinclude measures for cell permeability, protein binding, metabolic stability, and drug-drug interaction liabilities.The DMPK group at Scripps Florida currently occupies approximately 1000 sq/ft of laboratory and the officespace housed in a 41,000 sq/ft research facility in Jupiter, Florida. Animal services are provided in a new stateof-the-art facility of approximately 5,000 square feet with the capacity to house approximately 1500 mouse and240 rat cages. The Vivarium includes animal quarantine and holding rooms for rodents, dedicated procedurespace, and a biosafety level 3 (BSL3) containment suite with shower-in requirement, biosafety cabinets,ventilated racks, and pass-through autoclave. Animal services are provided by a fully trained staff with acontract veterinarian.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute of Mental Health (NIMH)
Type
Specialized Center--Cooperative Agreements (U54)
Project #
1U54MH084512-01
Application #
7650953
Study Section
Special Emphasis Panel (ZRG1-BCMB-D (50))
Project Start
2008-09-01
Project End
2014-05-31
Budget Start
2008-09-01
Budget End
2009-05-31
Support Year
1
Fiscal Year
2008
Total Cost
$315,468
Indirect Cost

  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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