immune response genes

ZL0420 是有效且选择性的 BET 溴结构域 4 (BRD4) 抑制剂，对 BRD4 的溴结构域 (BD) 具有纳摩尔结合亲和力。ZL0420 对 BRD4 BD1和 BRD4 BD2 的IC50分别为 27 nM 和 32 nM。

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为一种环二核苷酸，主要用于抗体-活性分子偶联物(ADC)的合成。作为先天免疫及适应性免疫反应的关键激活剂，环状二核苷酸能由内源性外来DNA或侵入性细菌病原体生成，在人体内通过促进干扰素基因表达激活先天免疫系统。

Cyclic GMP 是一种内源性第二信使，能诱导胞浆 DNA 反应引发干扰素的生成。它通过激活干扰素基因刺激因子 (STING)，触发产生 I 型干扰素及其他免疫介质的信号级联。Cyclic GMP 与 Cyclic-AMP 的结合物 Cyclic-GMP-AMP 会促进 IRF3 磷酸化和核转位，从而增强抗病毒免疫反应。此外，Cyclic GMP 可能通过激活 PDE 降解 cAMP 来抑制心肌细胞钙电流 ICa，从而调节心肌收缩。其衍生物 8-Br-cGMP 具有抗血小板活性。Cyclic GMP 被用于研究抗病毒免疫和心血管疾病。

dCNP 结合 NPR-B C 受体 (NPR-B C receptor)，激活 cGMP 信号通路以调节血管功能。通过下调 HIF1α、HIF2α 等基因，dCNP 发挥抗缺氧作用，并抑制肿瘤基质诱导，体现其抗纤维化效能。同时，dCNP 上调肿瘤中的 CTL、NK 细胞和常规 1 型树突状细胞，增强免疫反应。