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MRS-1706 is a Selective A(2B) Adenosine Receptor Inverse Agonist
The human adenosine A2B receptor belongs to class A G proteincoupled receptors (GPCRs). And previous studies have verified that constitutively active mutant (CAM) human adenosine A2B receptors were identified from…
AMG 487 is a Selective CXCR3 Antagonist
Chemokine receptor CXCR3 is a chemokine receptor primarily expresses on activated CD4+ and CD8+ T cells with a Th1 phenotype. CXCR3 also expresses on B cells, natural killer (NK) cells,…
DB550, Targeting PLCγ1, Prevents Th17-driven Inflammation via Disrupting the CD95-PLCγ1 Interaction
CD95L is a transmembrane ligand (m-CD95L) releases a soluble ligand (s-CD95L) that is cleaved by metalloproteases. Unlike m-CD95L, the interaction between s-CD95L and CD95 fails to recruit caspase-8 and FADD…
NG25, a Dual Inhibitor of TAK1 and MAP4K2, Suppresses Production of IFNα
TAK1 is also called Mitogen-activated protein kinase kinase kinase 7 (MAP3K7). It belongs to the serine/threonine protein kinase family. The kinase regulates cell death, and its activation is through a…
Ly93, an Oral Active SMS2 Inhibitor, Has Anti-Atherosclerotic Activity
The sphingomyelin synthase 2 (SMS2) is a potential target for pharmacological intervention in atherosclerosis. However, as far as now, reports about selective SMS2 inhibitors and their pharmacological activities were lacked.…
S18-000003 is an Orally Acitive RORγt Inhibitor
RORγ (RAR-related orphan receptor gamma) is a protein of the nuclear receptor family of transcription factors. RORγ (RORγ1) and RORγt (RORγ2) are two isoforms, encoded by the same RORC gene.…
R-10015, a LIMK Inhibitor and a Broad-Spectrum Antiviral Drug, Inhibits HIV Infection
Human immunodeficiency virus (HIV) infection causes CD4 T cell depletion and immunodeficiency. Antiretroviral drugs target viral proteins, such as reverse transcriptase, protease, and integrase. Antiretroviral drugs effectively inhibit HIV. However,…
AS1517499, a STAT6 Inhibitor, Has Potential to Treat Asthma
Asthma is a common long-term inflammatory disease of the airways of the lungs. Asthma is a condition in which your airways narrow and swell and produce extra mucus. Airway hyperresponsiveness…
MS402, a BD1-Selective BET BRD Inhibitor, Blocks Th17 Cells Differentiation
T-helper 17 (Th17) cells is a unique CD4+ T-cell subset characterized by production of interleukin-17 (IL-17). Especially, IL-17 is a highly inflammatory cytokine with robust effects on stromal cells in…