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)

  • GC33076 structure
    GC33076Telratolimod (MEDI 9197)
    CAS: 1359993-59-1
    纯度: >99.00%

    Telratolimod (MEDI 9197)是一种有效的toll-like receptor 7(TLR-7)和toll-like receptor 8(TLR-8)的激动剂。

  • GC33092 structure
    GC33092Hesperin
    CAS: 4430-35-7
    纯度: >98.00%

    An isothiocyanate with diverse biological activities

  • GC33134 structure
    GC33134Bufotalin
    CAS: 471-95-4
    纯度: 98.46%

    Bufotalin是一种天然的强心类固醇,来源于蟾蜍分泌物。

  • GC33150 structure
    GC33150DHMEQ racemate (rel-DHMEQ)
    CAS: 287194-38-1

    DHMEQ 消旋体 (rel-DHMEQ) 是一种 NF-κB 抑制剂。 DHMEQ 消旋体 (rel-DHMEQ) 的活性低于 (-)-DHMEQ。

  • GC33200 structure
    GC33200Target Protein-binding moiety 13
    CAS: 1092369-24-8
    纯度: >98.50%

    Target Protein-binding moiety 13 (PROTAC FKBP12-binding moiety 1) 是 FKBP (SLF) 的合成配体。目标蛋白结合部分 13(PROTAC FKBP12 结合部分 1)可用于 PROTAC 的合成。

  • GC33306 structure
    GC33306IMD-0560
    CAS: 439144-66-8
    纯度: >99.50%

    IMD-0560 is an Inhibitor of nuclear factor kappa-B kinase (IKK) which can suppress the production of inflammatory cytokines and chemokines.

  • GC33314 structure
    GC333141,4-Chrysenequinone (Chrysene-1,4-dione)
    CAS: 100900-16-1

    1,4-Chrysenequinone (Chrysene-1,4-dione) 是一种多环芳香族醌,可作为芳烃受体 (AhR) 的激活剂。

  • GC33330 structure
    GC33330Cynaropicrin
    CAS: 35730-78-0
    纯度: >98.00%

    A sesquiterpene lactone

  • GC33405 structure
    GC33405Neoseptin 3
    CAS: 1622863-21-1
    纯度: >98.00% / >99.50%

    Neoseptin3是Toll样受体4/髓样分化因子2(mTLR4/MD-2)的激动剂,其EC50值为18.5μM。

  • GC33426 structure
    GC33426Rocaglamide (Rocaglamide A)
    CAS: 84573-16-0
    纯度: >98.50%

    Rocaglamide (Rocaglamide A) 是从 Aglaia 属(楝科)中分离出来的。

  • GC33444 structure
    GC33444Octahydrocurcumin (Hexahydrobisdemethoxycurcumin)
    CAS: 36062-07-4
    纯度: >98.00%

    An active metabolite of curcumin with diverse biological activities

  • GC33479 structure
    GC33479Hexaconazole ((-)-Hexaconazol)
    CAS: 79983-71-4

    A triazole fungicide

  • GC33606 structure
    GC33606D-(+)-Glucono-1,5-lactone (Gluconic acid lactone)
    CAS: 90-80-2
    纯度: >99.00%

    Gluconolactone is a naturally occurring polyhydroxy acid with metal chelating, moisturizing and antioxidant activity.

  • GC33632 structure
    GC33632Veratric acid (3,4-Dimethoxybenzoic acid)
    CAS: 93-07-2

    Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.

  • GC33699 structure
    GC33699SAFit1
    CAS: 1643125-32-9
    纯度: >99.50% / >98.00%

    SAFit1 是一种 FK506 结合蛋白 51(FKBP51)特异性抑制剂,其 K i 值为 4 ± 0.3nM。

  • GC33717 structure
    GC33717Flaconitine (Acetylaconitine)
    CAS: 77181-26-1
    纯度: >98.50%

    A diterpene alkaloid with diverse biological activities

  • GC33779 structure
    GC33779Cysteamine (β-Mercaptoethylamine)
    CAS: 60-23-1
    纯度: >95.00%

    2-Aminoethanethiol (cysteamine, β-Mercaptoethylamine, 2-Mercaptoethylamine, Thioethanolamine, Mercaptamine) is a radiation-protective agent that oxidizes in air to form cystamine.

  • GC33815 structure
    GC338154-Hydroxyphenylacetic acid
    CAS: 156-38-7
    纯度: >99.00%

    A phenolic acid with anti-inflammatory and anti-steatotic activities

  • GC33816 structure
    GC33816Ertiprotafib (PTP 112)
    CAS: 251303-04-5

    Ertiprotafib (PTP 112) 是 PTP1B,IkB 激酶 β 的抑制剂; (IKK-β) 和双 PPARα;和 PPARβ;激动剂,IC50 为 1.6 μ;M 代表 PTP1B,400 nM 代表 IKK-β;EC50 约为 1 μ;M 代表 PPARα;/PPAR`;

  • GC33820 structure
    GC33820C29
    CAS: 363600-92-4
    纯度: >98.00%

    C29 是一种 Toll 样受体 2 (TLR2) 抑制剂。

  • GC33823 structure
    GC33823C-176 (STING inhibitor 1)
    CAS: 314054-00-7
    纯度: >99.00% / >98.00%

    C-176(STING 抑制剂 1)强烈降低 STING 介导的,但不降低 RIG-I 或 TBK1 介导的 IFNβ 报告基因活性。

  • GC33827 structure
    GC33827Uric acid
    CAS: 69-93-2
    纯度: >99.00% / >98.00%

    Uric Acid (2,6,8-Trioxypurine, 2,6,8-Trihydroxypurine, 2,6,8-Trioxopurine), a normal component of urine, is a product of the metabolic breakdown of purine nucleotides.

  • GC33828 structure
    GC33828E6446 dihydrochloride (E-6446 dihydrochloride)
    CAS: 1345675-25-3
    纯度: >99.50%

    E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.

  • GC33831 structure
    GC33831Lidocaine hydrochloride (Lignocaine hydrochloride)
    CAS: 73-78-9
    纯度: >99.50% / >98.00%

    Lidocaine hydrochloride (Lignocaine hydrochloride)是一种氨基酰胺类局部麻醉剂,可抑制voltage-insensitive ‘flicker’ K + channel,IC 50 值为220μM。