killer,cells

Loxoribine (RWJ 21757) 是一种鸟苷类似物，是一种口服生物可利用的选择性 Toll 样受体 (TLR) 7 激动剂。 具有抗病毒和抗肿瘤活性。它是一种新型的强效免疫刺激剂，具有较广谱的免疫生物学活性。

Amivantamab (JNJ-61186372) 是一种人源可识别表皮生长因子受体 （EGFR） 和 MET 原癌基因 （MET）的抗体，具有抗癌抗肿瘤活性，可防止配体与 EGFR 和 MET 结合以及抑制下游信号转导的受体二聚化。Amivantamab 可诱导巨噬细胞的 Fc 依赖性胞吞作用和自然杀伤细胞的抗体依赖性细胞毒性，可用于研究转移性非小细胞肺癌。

CP-31398 在具有p53突变或野生型的癌症细胞中通过稳定p53的活性构象，并且促进p53活性。它还能上调p53的目标基因，包括p21WAF1 Cip1和KILLER DR5，从而发挥抑制肿瘤生长的功能。

Adenanthin, a natural inhibitor of thiol-dependent antioxidant enzymes, impairs the effector functions of human natural killer cells.

C8 Galactosylceramide is a synthetic C8 short-chain derivative of known membrane microdomain-forming sphingolipids. It increases the amount delivered and toxicity of doxorubicin in cancerous but not non-cancerous cells when incorporated into the nanoliposomal membrane of nanoliposomal-doxorubicin. C8 Galactosylceramide induces proliferation and cytokine production by splenocytes in vitro at concentrations ranging from 100-1,000 ng ml but has no effect on natural killer T cell production in vivo. It also activates NF-κB production in C6 glioma cells when used at a concentration of 10 μM.

C12 Galactosylceramide is a bioactive sphingolipid. It inhibits IL-4 production by 53.84% in EL4 T cells when used at a concentration of 10 μM. C12 Galactosylceramide reduces the growth of human papillomavirus type 16-associated tumors in mice and reduces tumor recurrence following surgical removal or chemotherapy. It also reduces natural killer T cell activity, delays the onset of proteinuria, and improves survival in a mouse model of systemic lupus.

H-Leu-Leu-OMe HBr (L-Leucyl-L-Leucine methyl ester HBr) 是 L-亮氨酸甲酯的二肽缩合产物，是对自然杀伤 T 细胞有毒性的肽，具有免疫抑制活性，可消除混合淋巴细胞群中的所有自然杀伤细胞 （NK） 功能。

Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.

NZ28, also known as NSC134754, is potent HSF1 inhibitor, which induced inhibition of HSF1, SP1 and NF-κB triggers the loss of the natural killer cell-activating ligands MICA B on human tumor cells. Heat-shock transcription factor HSF1 has a critical role in human epidermal growth factor receptor-2-induced cellular transformation and tumorigenesis.

NLG802 is an orally bioavailable prodrug of indoximod, a methylated tryptophan, with immune checkpoint inhibitory and antineoplastic activities. Upon oral administration, the indoximod prodrug NLG802 is converted to indoximod. Indoximod targets, binds to and inhibits the enzyme indoleamine 2,3-dioxygenase (IDO; IDO1), which converts the essential amino acid tryptophan into the immunosuppressive metabolite kynurenine. By increasing tryptophan levels and decreasing kynurenine levels, indoximod restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs).

ANA773 is a Toll-like Receptor 7 (TLR7) agonist prodrug with potential immunostimulating activity. Upon oral administration, ANA773 is metabolized into its active form that binds to and activates TLR7, thereby stimulating dendritic cells (DCs) and enhancing natural killer cell (NK) cytotoxicity. This activation results in the production of proinflammatory cytokines, including interferon alpha, and enhanced antibody-dependent cellular cytotoxicity (ADCC). TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.

αGalCer-RBD 是一种佐剂脂蛋白结合物。αGalCer-RBD 可诱导对 SARS-CoV-2及其变异毒株的有效免疫。αGalCer-RBD 结合物诱导 RBD 特异性、产生细胞因子的 T 细胞发育。αGalCer-RBD 有望成为一种有效的 COVID-19 疫苗候选化合物。α-Galactosylceramide (αGalCer) 是一种有效的不变自然杀伤 T 细胞 (iNKT) 激动剂。

Mezagitamab (TAK-079) 是一种全人源抗 CD38 的IgG1λ 单克隆抗体，对表达CD38的细胞（包括浆母细胞、浆细胞、自然杀伤细胞）具有高亲和力，通过抗体和补体依赖性细胞毒性耗尽表达 CD38 的肿瘤细胞。Mezagitamab 可用于研究复发/难治性多发性骨髓瘤 (RRMM) 和原发性血小板减少性紫癜 (ITP)。

Urelumab(BMS-66513) 是一种人源化的 IgG4 单克隆抗体，常被当作 CD137 激动剂使用。Urelumab 具有潜在的抗肿瘤活性，可增强 T 细胞和自然杀伤细胞对肿瘤细胞的杀伤作用，并增强 Rituximab 的细胞毒性。Urelumab 可用于研究弥漫性大B细胞淋巴瘤 (DLBCL)合滤泡性淋巴瘤 (FL) 等实体瘤相关疾病。

Lirilumab (IPH2102) 是一种针对杀伤性免疫球蛋白样受体抗体 KIR2D 的抗体，具有抗肿瘤活性，通过 Vav1 依赖性 NF-κB 去抑制增强自然杀伤细胞的抗 HPV+ 宫颈癌活性，可用于研究白血病、头颈部鳞状细胞癌 (SCCHN)。

Ilaprazole sodium hydrate (IY-81149 sodium hydrate) 是一种具有口服活性的质子泵抑制剂，具有潜在的抗病毒活性，抑制 H+ K+-ATPase，可阻断培养物中 Vero 细胞的传染性单纯疱疹病毒 （HSV）-1 2 释放，阻断 HSV 颗粒的转运。

Peptide A5K acetate 是 INF7-TAT 衍生物，专用于 CRISPR RNP 传递到 T 细胞。该化合物有效增强 Cas9 RNP 传递到自然杀伤 (NK) 细胞的能力。

Lorukafusp alfa（14.18 mAb; hu14.18-IL2）是一种由人源化14.18抗GD2抗体和IL210连接而成的免疫细胞因子。该化合物通过其hu14.18-IL2与肿瘤细胞表面的GD2结合，激活抗体依赖性细胞毒性（ADCC）和补体依赖性细胞毒性，以及与效应细胞上Fc受体结合并激活NK和T细胞的活性，从而显现出抗肿瘤效果。

Euphoscopin C, 一种自Euphorbia helioscopia分离得到的二萜类化合物，可显著增强NK细胞对H1299-luci细胞和A549-luci细胞的杀伤活性。

Euphoheliosnoid A (Compound 24) 为二萜类化合物，以 2.5 μM 浓度显著提升 NK 细胞针对 H1299-luci 及 A549-luci 细胞的杀伤效率。

Deacetylasperulosidic Acid 是海巴戟果实的主要植物化学成分。它能够防止体外 4-硝基喹啉1-氧化物诱导的 DNA 损伤，抑制 IL-2的产生以及自然杀伤细胞的活化。它具有抗原活性，抑制仓鼠卵巢细胞和小鼠中染色体畸变的诱导。它可增加超氧化物歧化酶活性，从而具有抗氧化活性。

MTX-3937作为一种Siglec-9抑制剂，其Kd值达到3.15 μM。该化合物能够增强自然杀伤(NK)细胞的功能与稳定性，并显著提升NK细胞在体内对抗肝癌的抗肿瘤效果。

GCS-12 作为一种 Th1 2 平衡的磺酰胺糖脂,主要通过增强与CD1d的相互作用来发挥作用.该化合物能激活自然杀伤 T 细胞 (NKT cell),诱导它们分泌细胞因子IFN-γ和IL-4,进而在小鼠体内展示出显著的免疫调节和抗肿瘤活性.

GCS-11 是一种高效的 NKT 细胞激动剂,特别选择性地促进 IFN-γ 的产生,同时也能增加 IL-4 的分泌.该化合物展现了显著的抗癌活性,并可能作为癌症免疫治疗或疫苗开发中的有前途佐剂.