Immunology/Inflammation

Immunology/Inflammation(免疫及炎症)

The immune and inflammation-related pathway including the Toll-like receptors pathway, the B cell receptor signaling pathway, the T cell receptor signaling pathway, etc.

Toll-like receptors (TLRs) play a central role in host cell recognition and responses to microbial pathogens. TLR4 initially recruits TIRAP and MyD88. MyD88 then recruits IRAKs, TRAF6, and the TAK1 complex, leading to early-stage activation of NF-κB and MAP kinases [1]. TLR4 is endocytosed and delivered to intracellular vesicles and forms a complex with TRAM and TRIF, which then recruits TRAF3 and the protein kinases TBK1 and IKKi. TBK1 and IKKi catalyze the phosphorylation of IRF3, leading to the expression of type I IFN [2].

BCR signaling is initiated through ligation of mIg under conditions that induce phosphorylation of the ITAMs in CD79, leading to the activation of Syk. Once Syk is activated, the BCR signal is transmitted via a series of proteins associated with the adaptor protein B-cell linker (Blnk, SLP-65). Blnk binds CD79a via non-ITAM tyrosines and is phosphorylated by Syk. Phospho-Blnk acts as a scaffold for the assembly of the other components, including Bruton’s tyrosine kinase (Btk), Vav 1, and phospholipase C-gamma 2 (PLCγ2) [3]. Following the assembly of the BCR-signalosome, GRB2 binds and activates the Ras-guanine exchange factor SOS, which in turn activates the small GTPase RAS. The original RAS signal is transmitted and amplified through the mitogen-activated protein kinase (MAPK) pathway, which including the serine/threonine-specific protein kinase RAF followed by MEK and extracellular signal related kinases ERK 1 and 2 [4]. After stimulation of BCR, CD19 is phosphorylated by Lyn. Phosphorylated CD19 activates PI3K by binding to the p85 subunit of PI3K and produce phosphatidylinositol-3,4,5-trisphosphate (PIP3) from PIP2, and PIP3 transmits signals downstream [5].

Central process of T cells responding to specific antigens is the binding of the T-cell receptor (TCR) to specific peptides bound to the major histocompatibility complex which expressed on antigen-presenting cells (APCs). Once TCR connected with its ligand, the ζ-chain–associated protein kinase 70 molecules (Zap-70) are recruited to the TCR-CD3 site and activated, resulting in an initiation of several signaling cascades. Once stimulation, Zap-70 forms complexes with several molecules including SLP-76; and a sequential protein kinase cascade is initiated, consisting of MAP kinase kinase kinase (MAP3K), MAP kinase kinase (MAPKK), and MAP kinase (MAPK) [6]. Two MAPK kinases, MKK4 and MKK7, have been reported to be the primary activators of JNK. MKK3, MKK4, and MKK6 are activators of P38 MAP kinase [7]. MAP kinase pathways are major pathways induced by TCR stimulation, and they play a key role in T-cell responses.

Phosphoinositide 3-kinase (PI3K) binds to the cytosolic domain of CD28, leading to conversion of PIP2 to PIP3, activation of PKB (Akt) and phosphoinositide-dependent kinase 1 (PDK1), and subsequent signaling transduction [8].

 

References

[1] Kawai T, Akira S. The role of pattern-recognition receptors in innate immunity: update on Toll-like receptors[J]. Nature immunology, 2010, 11(5): 373-384.

[2] Kawai T, Akira S. Toll-like receptors and their crosstalk with other innate receptors in infection and immunity[J]. Immunity, 2011, 34(5): 637-650.

[3] Packard T A, Cambier J C. B lymphocyte antigen receptor signaling: initiation, amplification, and regulation[J]. F1000Prime Rep, 2013, 5(40.10): 12703.

[4] Zhong Y, Byrd J C, Dubovsky J A. The B-cell receptor pathway: a critical component of healthy and malignant immune biology[C]//Seminars in hematology. WB Saunders, 2014, 51(3): 206-218.

[5] Baba Y, Matsumoto M, Kurosaki T. Calcium signaling in B cells: regulation of cytosolic Ca 2+ increase and its sensor molecules, STIM1 and STIM2[J]. Molecular immunology, 2014, 62(2): 339-343.

[6] Adachi K, Davis M M. T-cell receptor ligation induces distinct signaling pathways in naive vs. antigen-experienced T cells[J]. Proceedings of the National Academy of Sciences, 2011, 108(4): 1549-1554.

[7] Rincón M, Flavell R A, Davis R A. The Jnk and P38 MAP kinase signaling pathways in T cell–mediated immune responses[J]. Free Radical Biology and Medicine, 2000, 28(9): 1328-1337.

[8] Bashour K T, Gondarenko A, Chen H, et al. CD28 and CD3 have complementary roles in T-cell traction forces[J]. Proceedings of the National Academy of Sciences, 2014, 111(6): 2241-2246.

研究方向

Immunology/Inflammation 相关产品(4245)

  • GC64456 structure
    GC64456Stepharine
    CAS: 2810-21-1
    纯度: >98.00%

    Stepharine 是天然的生物碱,可直接靶向 TLR4 (TLR4 抑制剂),结合 TLR4/MD2 复合体。Stepharine 具有抗衰老、抗病毒和抗高血压等活性。

  • GC64482 structure
    GC64482SP4206
    CAS: 515846-21-6

    SP4206 是一种 IL-2/IL-2Rα 相互作用抑制剂,SP4206 高亲和力结合到 IL-2 (Kd=70 nM) ,且阻断 IL-2 与其受体 IL-2Rα 结合 (Kd=10 nM)。

  • GC64485 structure
    GC64485HXR9 hydrochloride
    纯度: >99.00%

    HXR9 hydrochloride 是一种细胞渗透性肽,是 HOX/PBX 相互作用 (HOX/PBX interaction) 的竞争性拮抗剂。HXR9 hydrochloride 拮抗 HOX 与第二转录因子 (PBX) 之间的相互作用,PBX 与旁系同源基因组 1 至 8 中的 HOX 蛋白结合。HXR9 hydrochloride 选择性地减少细胞增殖并促进 HOXA/PBX3 基因高水平表达的细胞,例如 MLL 重排的白血病细胞中的细胞凋亡 (apoptosis)。

  • GC64486 structure
    GC64486Pepinh-TRIF TFA
    纯度: >99.00%

    Pepinh-TRIF (TFA) 是一种 30 aa 肽,通过干扰 TLR-TRIF 的相互作用 (TLR-TRIF interaction ) 来阻断 TRIF 信号。

  • GC64526 structure
    GC64526CL097
    CAS: 1026249-18-2

    CL097 是一种有效的 TLR7/8 激动剂,可在巨噬细胞中诱导促炎细胞因子。CL097 诱导 NADPH 氧化酶启动活性,导致 fMLF 刺激的 ROS 产生增加。

  • GC64552 structure
    GC64552XJB-5-131
    CAS: 866404-31-1
    纯度: >98.00%

    XJB-5-131 是一种靶向线粒体的 ROS 和电子清除剂。XJB-5-131 是双功能抗氧化剂,包含自由基清除剂。XJB-5-131 是针对线粒体的合成抗氧化剂。XJB-5-131 是有效的脐带血单核细胞 (CB MNC) 电离辐射保护剂和缓和剂。

  • GC64595 structure
    GC64595HKSOX-1 (5/6-mixture)
    纯度: >98.50% / >98.00%

    HKSOX-1 是一种荧光探针,用于成像和检测活细胞以及体内的内源性超氧化物。 HKSOX-1 对超氧阴离子自由基具有极好的选择性和敏感性。

  • GC64619 structure
    GC64619β-Ionone
    CAS: 14901-07-6
    纯度: >99.00%

    β-Ionone 可有效诱导胃腺癌细胞 SGC7901 凋亡 (apoptosis)。具有抗肿瘤活性。

  • GC64630 structure
    GC646303-O-Acetyl-α-boswellic acid
    CAS: 89913-60-0

    A pentacyclic triterpene

  • GC64645 structure
    GC64645Sappanchalcone
    CAS: 94344-54-4
    纯度: >99.00%

    Sappanchalcone 从 Caesalpinia sappan L. 中提取的黄酮类化合物,诱导人结肠癌细胞凋亡 (apoptosis)。

  • GC64662 structure
    GC64662Helichrysetin
    CAS: 62014-87-3
    纯度: >99.00%

    Helichrysetin,分离于 Helichrysum odoratissimum 的花朵中, 是一种ID2 (DNA 结合抑制剂 2) 抑制剂,可抑制DCIS (原位导管癌) 的形成。Helichrysetin 对细胞生长具有很强的抑制作用,并且能够诱导 A549 细胞凋亡 (apoptosis)。

  • GC64663 structure
    GC64663Galloylpaeoniflorin
    CAS: 122965-41-7
    纯度: >98.00%

    Galloylpaeoniflorin 是 NF-κB 抑制剂。并且 Galloylpaeoniflorin 是一种DNA裂解的抑制剂。

  • GC64739 structure
    GC647392-Aminoquinoline
    CAS: 580-22-3
    纯度: >97.00%

    2-Aminoquinoline 是一种很有前途的化合物,可用作生物可利用的 nNOS 抑制剂,但对人类 nNOS 的抑制作用较低,与人类 eNOS 相比选择性较低,并且与其他 CNS 靶点有显着结合。2-Aminoquinoline 具有研究抗神经退行性疾病的潜力。

  • GC64748 structure
    GC64748Pristane
    CAS: 1921-70-6
    纯度: >98.00% / >99.00% / >99.50%

    Pristane是一种无色无味的液体,主要从鲨鱼肝油等天然来源提取,也作为微量成分存在于各种植物和海洋生物中。

  • GC64762 structure
    GC647623,6-Dihydroxyflavone
    CAS: 108238-41-1
    纯度: >98.00%

    3,6-Dihydroxyflavone 是一种抗癌剂。3,6-Dihydroxyflavone 剂量和时间依赖性地降低细胞活力并通过激活半胱天冬酶级联、切割聚 (ADP-核糖) 聚合酶 (PARP) 诱导 apoptosis。3,6-Dihydroxyflavone 增加细胞内氧化应激和脂质过氧化。

  • GC64786 structure
    GC64786Hellebrigenin
    CAS: 465-90-7

    Hellebrigenin,属于心脏活性类固醇的丁二烯内酯之一,从中药中分离出来。Hellebrigenin 诱导 DNA 损伤和细胞周期 G2/M 阻滞。 Hellebrigenin 触发线粒体介导的细胞凋亡。

  • GC64796 structure
    GC64796Eculizumab
    CAS: 219685-50-4
    纯度: >95.00%

    Eculizumab (Anti-Human C5, Humanized Antibody) 是一种针对补体 C5 (complement C5) 的长效人源化单克隆抗体。Eculizumab 抑制 C5 裂解为 C5a 和 C5b,因此抑制末端补体系统的部署,包括膜攻击复合物 (MAC) 的形成。Eculizumab 具有用于溶血研究的潜力。

  • GC64799 structure
    GC64799Cycloartenyl ferulate
    CAS: 21238-33-5

    Cycloartenyl ferulate (Cycloartenol ferulate) 是一种典型的三萜醇,具有抗氧化活性、抗过敏活性、抗炎活性和抗癌活性等多种生物活性。

  • GC64862 structure
    GC64862Tricetin
    CAS: 520-31-0

    Tricetin 是一种有效的竞争性 Keap1-Nrf2 蛋白相互作用 (PPI) 抑制剂。Tricetin 作用于帕金森病模型,通过激活 Nrf2/HO-1 信号通路和阻止线粒体依赖性细胞凋亡 (apoptosis) 通路来保护 6-OHDA 诱导的神经毒性。

  • GC64878 structure
    GC64878Factor D inhibitor 6
    CAS: 1386455-51-1
    纯度: >99.00%

    Factor D inhibitor 6 是一种有效的,高选择性,具有口服活性的因子 D (factor D) 抑制剂,IC50 为 30 nM,Kd 为 6 nM。Factor D inhibitor 6 对因子 B,激肽和凝集素补体途径激活以及广泛的受体,离子通道,激酶和蛋白酶等无活性。

  • GC64892 structure
    GC64892Factor B-IN-1
    CAS: 1481631-75-7

    Factor B-IN-1 是一种 Factor B 抑制剂,详细信息请参见专利 WO2013164802A1,Example 24。

  • GC64898 structure
    GC64898L-Kynurenine-d4-1
    CAS: 194546-33-3

    L-Kynurenine-d4-1 是 L-Kynurenine 氘代物。L-Kynurenine是L-色氨酸的代谢物。它是一种芳香烃受体 (aryl hydrocarbon receptor) 激动剂。

  • GC64901 structure
    GC64901TLR7 agonist 4
    CAS: 2413016-42-7

    TLR7 agonist 4 (Compound 1.2) 是一种 TLR7 激动剂,EC50 为 4.3 nM。

  • GC64936 structure
    GC64936TD52 dihydrochloride
    纯度: >98.00%

    A derivative of erlotinib