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Full Pharmacological Efficacy of a Novel S1P1 Agonist That Does Not Require S1P-Like Headgroup Interactions
TLDR
Data show that CYM-5442 activates S1P1-dependent pathways in vitro and to levels of full efficacy in vivo through a hydrophobic pocket separate from the orthosteric site of S 1P binding that is headgroup-dependent. Expand
Evidence that vasopressin V1b receptors mediate the transition to excessive drinking in ethanol‐dependent rats
TLDR
The present study determined state‐dependent alterations in vasopressin/V1bR signaling in an animal model of ethanol dependence and suggests a key role for vasoppressin/ V1b R signaling in the transition to ethanol dependence. Expand
Local Not Systemic Modulation of Dendritic Cell S1P Receptors in Lung Blunts Virus-Specific Immune Responses to Influenza
TLDR
The results suggest that locally delivered sphingosine analogs induce immunosuppression by modulating S 1P receptors other than S1P1 or S1p2 on dendritic cells in the lungs after influenza virus infection. Expand
Novel selective allosteric and bitopic ligands for the S1P(3) receptor.
TLDR
The coordinated approach with biochemical data and molecular modeling, based on the recently published S1P(1) crystal structure data in a highly conserved set of related receptors with a shared ligand, provides a strong basis for the successful optimization of orthosteric, allosterics, and bitopic modulators of S1p(3). Expand
A sphingosine 1-phosphate receptor 2 selective allosteric agonist.
TLDR
High throughput screening to identify two compounds which activate the S1PR2 receptor led to compounds with high nanomolar potency, XAX-162 and CYM-5520, which are highly selective and do not activate other S1P receptors. Expand
Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.
TLDR
Rational chemical modifications of the hit allowed the disclosure of the first reported highly selective S1P(4) antagonists with low nanomolar activity and adequate physicochemical properties suitable for further lead-optimization studies. Expand
Sphingosine 1-Phosphate Receptor 1 (S1P1) Upregulation and Amelioration of Experimental Autoimmune Encephalomyelitis by an S1P1 Antagonist
TLDR
It is shown that lymphocyte sequestration via S1P1 antagonism is sufficient to alleviate autoimmune pathology and reverses experimental autoimmune encephalomyelitis in mice without acting on S1p1 expressed within the central nervous system. Expand
Modulators of the Sphingosine 1-phosphate receptor 1.
TLDR
This review provides the latest advances on next-generation S1P1-R modulators from 2012 up to date, with an overview of the chemical structures, structure-activity relationships, and relevant biological and clinical properties. Expand
Sphingosine 1-phosphate enhances the excitability of rat sensory neurons through activation of sphingosine 1-phosphate receptors 1 and/or 3
TLDR
These results demonstrate that the enhanced excitability produced by S1P is mediated by activation of S1 PR1 and/or S1PR3. Expand
Sphingosine 1-phosphate receptor 1 agonists: a patent review (2013-2015)
TLDR
Clinical and preclinical studies of second generation S1P1-R agonists have been generating interesting results and may finally provide pharmacological agents with improved therapeutic profile than FTY720, particularly in terms of cardiovascular and pulmonary liabilities. Expand
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