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Mice overexpressing human uncoupling protein-3 in skeletal muscle are hyperphagic and lean
Uncoupling protein-3 (UCP-3) is a recently identified member of the mitochondrial transporter superfamily that is expressed predominantly in skeletal muscle. However, its close relative UCP-1 isExpand
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Company Takeovers and Equity Returns: The Target Size Effect
This paper examines the relationship between the size of a target and the market's reaction to the announcement of a takeover offer. Using the constrained (0,1) market model to estimate abnormalExpand
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Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
2-Amino-2-(4-octylphenethyl)propane-1,3-diol 1 (fingolimod, FTY720) has been recently marketed in the United States for the treatment of patients with remitting relapsing multiple sclerosis (RRMS).Expand
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Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
The efficacy of the recently approved drug fingolimod (FTY720) in multiple sclerosis patients results from the action of its phosphate metabolite on sphingosine-1-phosphate S1P1 receptors, while aExpand
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The utility of pharmacokinetic–pharmacodynamic modeling in the discovery and optimization of selective S1P1 agonists
Sphingosine-1-phosphate (S1P1) receptor agonists such as Fingolimod (FTY-720) are a novel class of immunomodulators that have clinical utility in the treatment of remitting relapsing multiplesExpand
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Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.
A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands.Expand
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Technical Advance: Function and efficacy of an α4‐integrin antagonist using bioluminescence imaging to detect leukocyte trafficking in murine experimental colitis
Leukocyte trafficking is a therapeutic target in IBD. The integrins α4β7 and α4β1 regulate leukocyte migration into tissues and lymphoid organs. Current strategies rely on biologics, such as mAb, toExpand
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Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
FTY720 is the first oral small molecule approved for the treatment of people suffering from relapsing-remitting multiple sclerosis. It is a potent agonist of the S1P1 receptor, but its lack ofExpand
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Spherical geometry and the least symmetric triangle
We study the problem of determining the least symmetric triangle, which arises both from pure geometry and from the study of molecular chirality in chemistry. Using the correspondence between planarExpand