Article

Pseudoirreversible inhibition elicits persistent efficacy of a sphigosine-1-phosphate receptor-1 antagonist

2023-05-09

Abstract excerpt

<h4>ABSTRACT</h4> Sphingosine 1-phosphate receptor 1 (S1PR1), a G protein-coupled receptor, is required for lymphocyte trafficking, and is a promising therapeutic target in inflammatory diseases. We synthesized a competitive antagonist, KSI-6666, that persistently inhibits S1PR1 activity and effectively suppresses pathogenic inflammation. Metadynamics simulation proposed that the interaction of KSI-6666 with a me...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: e0080d30-1e7b-5199-9866-3c89d0843bd4
DOI: 10.1101/2023.05.08.539826

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Pseudoirreversible inhibition elicits persistent efficacy of a sphigosine-1-phosphate receptor-1 antagonistDOI 10.1101/2023.05.08.539826Read

S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate.Semantic proximity Read

In-silico characterization of deleterious non-synonymous SNPs in the human S1PR1 gene reveals structural instability and altered ligand affinity.Semantic proximity Read

A sphingosine 1-phosphate receptor 2 selective allosteric agonist.Semantic proximity Read

Agonist-dependent effects of mutations in the sphingosine-1-phosphate type 1 receptor.Semantic proximity Read

Amelioration of Collagen-Induced Arthritis by a Novel S1P1 Antagonist with Immunomodulatory ActivitiesSemantic proximity Read

Structural dynamics of sphingosine kinase 1 regulation and inhibitionSemantic proximity Read

Structural dynamics of sphingosine kinase 1 regulation and inhibitionSemantic proximity Read

A G(q/11)-coupled mutant histamine H(1) receptor F435A activated solely by synthetic ligands (RASSL).Semantic proximity Read

Sphingosine 1-phosphate analogue recognition and selectivity at S1P4 within the endothelial differentiation gene family of receptors.Semantic proximity Read

Transmembrane protein CD69 acts as an S1PR1 agonistSemantic proximity Read

Activation by statins unveils two putative agonist binding sites in the pore domain of TRPA1Semantic proximity Read

Identification of Edg1 receptor residues that recognize sphingosine 1-phosphate.Semantic proximity Read