syk-in-ii

SYK-IN-II is an inhibitor of the spleen tyrosine kinase (STK).

Naldemedine tosylate (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) with high binding affinities (K_i = 0.34, 0.43, 0.94 nM) and potent antagonist activities (IC_50 = 25.57, 7.09, 16.1 nM) towards human recombinant μ-, δ-, and κ-opioid receptors, respectively. It is utilized in research on opioid-induced constipation (OIC) and is anticipated to interact with the 3CL proenzyme encoded by the SARS-CoV-2 genome.

The impact of spleen tyrosine kinase (Syk) signaling might be prominent in lupus because (i) Syk is a shared downstream signaling molecule among circulating immune complex, LPS, and (1→3)-β-D-glucan (BG), and (ii) all of these factors are detectable in the serum of Fc gamma receptor IIb-deficient (FcgRIIb- -) mice with sepsis. Syk inhibition downregulated several inflammatory pathways in FcgRIIb- - macrophages activated with BG + LPS suggesting the potential anti-inflammatory impact of Syk inhibitors in lupus. Indeed, administration of a Syk inhibitor prior to cecal ligation and puncture (CLP) sepsis in FcgRIIb- - mice reduced baseline lupus-induced proinflammatory cytokines and attenuated sepsis severity as evaluated by mortality, organ injury, serum LPS, and post-sepsis serum cytokines.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit