• Publications
  • Influence
Endothelial Cells Are Central Orchestrators of Cytokine Amplification during Influenza Virus Infection
TLDR
It is demonstrated that suppression of early innate immune responses through S1P1 signaling results in reduced mortality during infection with a human pathogenic strain of influenza virus, suggesting that diseases in which amplification of cytokine storm is a significant pathological component could be chemically tractable. Expand
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
Ozanimod (RPC1063) is a potent sphingosine‐1‐phosphate receptor‐1 (S1P1) and receptor‐5 (S1P5) agonist with autoimmune disease‐modifying activity
TLDR
This study assessed RPC1063 for its therapeutic utility in autoimmune diseases and targeting S1P receptors for treating autoimmune disease has been established in clinical studies with the non‐selective S 1P modulator, FTY720. Expand
Sphingosine-1-phosphate and its receptors: structure, signaling, and influence.
TLDR
The sphingosine-1-phosphate receptor signaling system has biological and medical importance and is the first lipid G protein-coupled receptor structure to be solved to 2.8-Å resolution, and can now directly understand causal relationships among protein expression, signal, and control points in physiology and pathology. 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
Essential Requirement for Sphingosine Kinase 2 in a Sphingolipid Apoptosis Pathway Activated by FTY720 Analogues*
TLDR
An apoptotic pathway triggered by intracellular accumulation of sphingolipid base phosphates is described and it is suggested that sphingoid base substrates for Sphk2 acting intrACEllularly could be useful in the treatment of lymphoproliferative diseases. 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
Identification of a μ-δ opioid receptor heteromer-biased agonist with antinociceptive activity
TLDR
CYM51010, a μOR-δOR–biased ligand, could serve as a scaffold for the development of a unique type (heteromer-biased) of drug that is more potent and without the severe side effects associated with conventional clinical opioids. Expand
...
1
2
3
4
5
...