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)

  • GC62196 structure
    GC62196Nisoldipine-d7
    CAS: 1189718-34-0

    Nisoldipine-d7 是 Nisoldipine 的氘代物。Nisoldipine(BAY-k 5552)是高效特异的 L 型 Cav1.2 通道阻断剂,IC50 为 10 nM。

  • GC62198 structure
    GC62198c-di-AMP sodium
    CAS: 2734909-87-4
    纯度: >99.50% / >98.00% / >95.00%

    C-di-AMP是STING(刺激内质网的蛋白)的激动剂,通过与该跨膜蛋白结合,激活TBK3-IRF3信号通路,进而引发I型IFN和TNF的产生。

  • GC62203 structure
    GC62203Falcarindiol
    CAS: 55297-87-5
    纯度: >99.00% / >98.00%

    Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules.

  • GC62222 structure
    GC62222DB2313
    CAS: 2170606-74-1
    纯度: >98.00%

    DB2313是一种强效的转录因子PU.1抑制剂,IC 50 为14nM。

  • GC62224 structure
    GC62224Ixekizumab
    CAS: 1143503-69-8

    Ixekizumab 是一种人源化 IgG4 单克隆抗体,可选择性结合和中和白细胞介素 IL-17A (KD<3 pM)。Ixekizumab 直接阻断 IL-17A 与 IL-17RA 的结合,但不与其他 IL-17 家族成员结合。Ixekizumab 用于中重度斑块型银屑病的研究。

  • GC62242 structure
    GC62242Sideroxylin
    CAS: 3122-87-0

    Sideroxylin 是一种从 Callistemon lanceolatus 中分离的 C-甲基化黄酮,对金黄色葡萄球菌具有抗菌活性。Sideroxylin 可抑制卵巢癌细胞增殖并诱导凋亡 (apoptosis),导致 DNA 断裂,线粒体膜去极化,产生活性氧 (ROS)。

  • GC62246 structure
    GC62246G5-7
    CAS: 939681-36-4
    纯度: >99.50%

    G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2.

  • GC62252 structure
    GC62252Mefuparib hydrochloride
    CAS: 1449746-00-2
    纯度: >98.00%

    Mefuparib hydrochloride (MPH) 是一种具有口服活性的,底物竞争性和选择性的 PARP1/2 抑制剂,IC50 分别为 3.2 nM 和 1.9 nM。Mefuparib hydrochloride 诱导细胞凋亡 (apoptosis),并在体内外具有显着的抗癌活性。

  • GC62269 structure
    GC62269RRD-251
    CAS: 72214-67-6
    纯度: >99.50%

    RRD-251 是一种视网膜母细胞瘤肿瘤抑制蛋白 (Rb)-Raf-1相互作用 (Rb-Raf-1 interaction) 的抑制剂,具有高效的抗增殖、抗血管生成和抗肿瘤活性。

  • GC62273 structure
    GC62273JR14a
    CAS: 2411440-41-8
    纯度: >98.50%

    JR14a, a selective and potent human Complement C3a receptor antagonist, which is assessed by inhibition of intracellular calcium release (IC50=10 nM) induced in human monocyte-derived macrophages by C3a, inhibition of β-hexosaminidase secretion (IC50=8 nM) from human LAD2 mast cells degranulated by C3a, and selectivity for human C3aR over C5aR.

  • GC62300 structure
    GC62300JC124
    CAS: 1638611-48-9

    JC124 是一种特异性的 NLRP3 炎症小体抑制剂。JC124 具有抗炎和神经保护作用。

  • GC62317 structure
    GC62317NX-13
    CAS: 2389235-01-0
    纯度: >98.00%

    NX-13是一种一流的,具有口服活性的肠道限制剂,选择性靶向并激活 NLRX1 通路,诱导免疫代谢改变。NX-13 可降低炎症性肠病的炎症反应。NX-13 可用于克罗恩病和溃疡性结肠炎的研究。

  • GC62319 structure
    GC62319Samuraciclib trihydrochloride
    纯度: >99.00%

    Samuraciclib (CT7001) trihydrochloride 是一种有效的,具有选择性,ATP 竞争性和口服活性的 CDK7 抑制剂,IC50 为 41 nM。Samuraciclib trihydrochloride 对 CDK7 的选择性分别是 CDK1,CDK2 (IC50 为 578 nM),CDK5 和 CDK9 的 45 倍,15 倍,230 倍和 30 倍。Samuraciclib trihydrochloride 以 GI50 值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长,具有有效的抗肿瘤作用。

  • GC62331 structure
    GC62331CD73-IN-3
    CAS: 2375815-63-5
    纯度: >99.50%

    LY-3475070 is a potent, selective and orally bioavailable inhibitor of the ectoenzyme CD73 (cluster of differentiation 73, 5'-ecto-nucleotidase, 5'-NT, ecto-5'-nucleotidase).

  • GC62334 structure
    GC62334AT791
    CAS: 1219962-49-8
    纯度: >98.50%

    AT791 是一种有效的口服生物利用 TLR7 和 TLR9 抑制剂。AT791 抑制多种人类和小鼠细胞类型的 TLR7 和 TLR9 信号传导,并在体外抑制 DNA-TLR9 相互作用。

  • GC62338 structure
    GC62338GSK-3&#946; inhibitor 3
    CAS: 1448990-73-5
    纯度: >98.00%

    GSK-3β inhibitor 3 是一种有效,选择性,不可逆和共价的糖原合酶激酶 3β (GSK-3β) 抑制剂,IC50 值为 6.6 μM。GSK-3β inhibitor 3 可用于急性早幼粒细胞白血病的研究。

  • GC62347 structure
    GC62347CMC2.24
    CAS: 1255639-43-0
    纯度: >96.00%

    CMC2.24 (TRB-N0224) 是一种口服活性三羰基甲烷制剂,通过抑制 Ras 及其下游效应子 ERK1/2 途径对小鼠胰腺肿瘤有效。CMC2.24 也是一种有效的锌依赖性 MMPs 抑制剂,IC50 范围为 2.0-69 μM。CMC2.24 通过恢复软骨内稳态和通过NF-κB/HIF-2α 轴抑制软骨细胞凋亡来减轻骨关节炎的进展。

  • GC62370 structure
    GC62370Sodium thiocyanate
    CAS: 540-72-7

    Sodium Thiocyanate (NaSCN, Sodium rhodanide, Sodium sulfocyanate, Sodium rhodanate), one of the main sources of the thiocyanate anion, is used as a precursor for the synthesis of pharmaceuticals and other specialty chemicals. Sodium thiocyanate (NaSCN) reduces IL-6, whereas increases IL-10 levels. Sodium thiocyanate also reduces ROS.

  • GC62372 structure
    GC62372Cyclic-di-GMP sodium
    纯度: >99.00% / >99.50% / >98.50%

    A bacterial second messenger and cyclic dinucleotide

  • GC62388 structure
    GC62388YUM70
    CAS: 423145-35-1
    纯度: >98.00%

    YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.Although YUM70 inhibits GRP78 enzymatic activity, it increases the expression of GRP78 by increasing the chaperone translation mechanism.

  • GC62395 structure
    GC62395TLR7/8 agonist 3
    CAS: 642473-95-8
    纯度: >99.00%

    TLR7/8 agonist 3 是一种有效的 TLR7/8 激动剂,源于专利文献 WO2016057618,化合物 II。

  • GC62399 structure
    GC62399RA375

    RA375 是 RPN13 (26S 蛋白酶体亚基) 抑制剂。RA375 激活 UPR 信号、ROS 产生和凋亡。RA375 的抗肿瘤活性是 RA190的 10 倍。

  • GC62406 structure
    GC62406Moracin O
    CAS: 123702-97-6
    纯度: >98.00%

    Moracin O是一种从 Morus alba Linn.中分离出来的,具有显著抗炎和抗氧化活性的缺氧诱导因子(HIF-1)抑制剂。

  • GC62411 structure
    GC62411QTX125
    CAS: 1279698-31-5

    QTX125 是一种有效且高度选择性的 HDAC6 抑制剂。与其他 HDAC 相比,QTX125 对 HDAC6 具有出色的选择性。QTX125 具有抗肿瘤作用。