immune response genes

ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with nanomolar binding affinities to the bromodomains (BDs) of BRD4, exhibiting IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

2'2'-cGAMP is a synthetic dinucleotide (CDN) that contains non-canonical 2'5'-phosphodiester bonds. It binds to the adapter protein stimulator of interferon genes , which is a component of the innate immune response that activates the type I interferon pathway when bound to cyclic dinucleotides. 2'2-cGAMP shows weaker binding to STING than 2'3'-cGAMP but binds more strongly than 3'3'-cGAMP , cyclic di-GMP , or 3'2'-cGAMP, which bind in the micromolar range (Kds = 1.04, 1.21, or 1.61 μM, respectively). Despite weaker binding, 2'2'-cGAMP induces IFN-β production in the same concentration range as 2'3'-cGAMP (EC50s = 15.8 and 19.4 nM, respectively, in L929 cells).

NFAT:AP-1 inhibitor-10 is a novel inhibitor of the NFAT:AP-1:DNA interaction on the ARRE-2 element, binding to DNA in a sequence-selective manner and inhibiting the transcription of the Il2 gene and several other cyclosporin A-sensitive cytokine genes important for the effector immune response.

Dexamethasone sodium succinate is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune response. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide......

CDN-A, a cyclic di-nucleotide, serves as a precursor for synthesizing antibody-drug conjugates (ADC) and acts as a potent stimulator of both innate and adaptive immune responses. In humans, these cyclic di-nucleotides, produced endogenously in response to foreign DNA or by bacterial pathogens, activate the innate immune system by inducing the expression of interferon genes [1] [2] [3].

Cyclic GMP is an endogenous second messenger that initiates interferon production in response to cytoplasmic DNA. It activates the stimulator of interferon genes (STING), triggering a signaling cascade that results in the production of type I interferons and other immune mediators. The conjugate of cyclic GMP and AMP, known as Cyclic-GMP-AMP, can induce the phosphorylation and nuclear translocation of IRF3, thereby enhancing antiviral immune responses. Additionally, Cyclic GMP may activate PDE to degrade cAMP, inhibit the myocardial calcium current ICa, and regulate cardiac contractility. The derivative 8-Br-cGMP exhibits antiplatelet activity, and Cyclic GMP is used in research related to antiviral immunity and cardiovascular diseases.

dCNP binds to NPR-B C receptors (NPR-B C receptor), initiating the cGMP signaling pathway and regulating vascular function. It exhibits anti-hypoxic effects by downregulating hypoxia-related genes such as HIF1α and HIF2α. Additionally, dCNP inhibits tumor stroma induction, demonstrating antifibrotic properties. It also enhances immune response by upregulating CTL, NK cells, and conventional type 1 dendritic cells in tumors.