GLPBio

Immunology/Inflammation

Read More about this category

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.

Research Areas

Products Related to Immunology/Inflammation(4922)

  • GC73210 structure
    GC73210MTR-106
    CAS: 1639357-93-9
    Purity: >99.00%

    MTR-106 ist ein potenter und oral aktiver G-Quadruplex-Stabilisator und RNA-Polymerase-I-Inhibitor.

  • GC73212 structure
    GC73212TH-6
    CAS: 3031349-25-1
    Purity: >95.00%

    TH-6 ist ein potenter HDAC-Inhibitor mit IC50s von 0.115, 0.135, 0.242, 0.138, 2.120 µM für HDAC1, HDAC2, HDAC3, HDAC6, HDAC8.

  • GC73225 structure
    GC73225ROS-generating agent 1
    CAS: 2369030-41-9
    Purity: >99.00%

    ROS-generating agent 1 (Verbindung 2c) modifiziert kovalent den Sec-498-Rückstand von TrxR, um ROS zu erzeugen.

  • GC73232 structure
    GC73232PRDX1-IN-1
    Purity: >98.00%

    PRDX1-IN-1 ist ein selektiver Inhibtor von PRDX1 mit einem IC50-Wert von 0,164 μM.

  • GC73234 structure
    GC73234MY-673
    CAS: 2944459-96-3
    Purity: >98.00%

    MY-673 ist ein Colchicinbindungsstelle-Inhibitor (CBSI), der die Tubulinpolymerisation hemmt.

  • GC73237 structure
    GC73237BWA-522
    CAS: 3042820-12-9
    Purity: >99.00%

    BWA-522 ist eine oral verfügbare kleinmolekulare Protein-Targeting Chimäre (PROTAC) mit signifikantem Abbaueffekt auf AR-FL und AR-V7.

  • GC73243 structure
    GC73243Nrf2-IN-3
    CAS: 6325-13-9
    Purity: >99.00%

    Nrf2-IN-3 (Verbindung R16) ist ein Nrf2-Hemmer.

  • GC73268 structure
    GC73268PH14
    Purity: >99.00%

    PH14 ist ein dualer PI3K/HDAC-Inhibitor mit IC50-Werten von 20,3 nM und 24,5 nM für PI3Kα bzw. HDAC3.

  • GC73269 structure
    GC73269ABBV-467
    CAS: 2287186-66-5
    Purity: >99.00%

    ABBV-467 ist ein selektiver MCL-1-Inhibitor (Ki: <0,01 nM).

  • GC73272 structure
    GC73272PARP-1-IN-3
    CAS: 2976342-33-1
    Purity: >99.00%

    PARP-1-IN-3, ein Benzamidderivat, ist ein potenter PARP-1 Inhibitor mit IC50 Werten von 0,25 nM und 2,34 nM für PARP-1 bzw. PARP-2.

  • GC73274 structure
    GC73274EGFR T790M/L858R-IN-2
    CAS: 2955607-40-4
    Purity: >99.00%

    EGFR T790M/L858R-IN-2 ist ein potenter und selektiver EGFRT790M/L858R-Inhibitor mit IC50-Werten von 3,5, 1290 nM für EGFRT790M/L858R bzw. EGFR WT.

  • GC73288 structure
    GC73288CDK8-IN-13
    CAS: 918523-75-8
    Purity: >98.00%

    CDK8-IN-13 ist ein potenter, selektiver und oral aktiver CDK8-Inhibitor mit einem IC50-Wert von 51,9 nM.

  • GC73294 structure
    GC73294F5446
    CAS: 2304465-89-0
    Purity: >99.00%

    F5446 (Compound 1) ist ein selektiver kleinmolekularer Inhibitor der SUV39H1 Metltransferase.

  • GC73301 structure
    GC733015-Aminosalicylic acid-d3
    CAS: 1309283-32-6
    Purity: >99.00%

    5-Aminosalicylic acid-d3 ist die mit Deuterium markierte 5-Aminosalicylsäure.

  • GC73309 structure
    GC73309Anti-melanoma agent 1
    CAS: 2418579-17-4
    Purity: >99.00%

    Anti-melanoma agent 1 (Verbindung 5m) ist ein Anti-Melanom-Mittel und induziert Zellapoptose.

  • GC73311 structure
    GC73311STAT3-IN-13
    CAS: 2248552-86-3
    Purity: >99.00%

    STAT3-IN-13 (Verbindung 6f) ist ein starker STAT3-Hemmer.

  • GC73313 structure
    GC73313PI3Kα-IN-9
    CAS: 2715287-67-3
    Purity: >99.00%

    PI3Kα-IN-9 (Verbindung 27) ist ein selektiver, langwirkender und oral aktiver PI3Kα-Inhibitor mit IC50-Werten von 4,4, 128, 146 und 153 nM für PI3Kα, PI3Kγ, PI3Kδ und PI3Kβ.

  • GC73317 structure
    GC73317ODN 1585 sodium
    Purity: >93.00%

    ODN 1585 sodium ist ein starker Induktor der IFN- und TNFα-Produktion.

  • GC73319 structure
    GC73319FITC-labeled ODN 2216 sodium
    Purity: >97.00%

    FITC-labeled ODN 2216 sodium ist ein humanspezifischer TLR9-Toll-ähnlicher Rezeptor-9-Ligand oder -Agonist.

  • GC73326 structure
    GC73326ODN D-SL03 sodium
    Purity: >99.00%

    ODN D-SL03 sodium ist ein CpG-Oligonukleotid der C-Klasse und kann PBMCs zur Produktion von hohem IFN-α anregen.

  • GC73355 structure
    GC73355STAT3-SH2 domain inhibitor 1
    CAS: 2816059-41-1
    Purity: >98.50%

    STAT3-SH2 domain inhibitor 1 ist ein potenter Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 Domain) Inhibitor mit einem Kd Wert von 1,57 μM.

  • GC73371 structure
    GC73371Enpp/Carbonic anhydrase-IN-2
    CAS: 2883495-39-2
    Purity: >99.00%

    Enpp/Carbonic anhydrase-IN-2 ist ein potenter Enpp- und Carbonandrase-Inhibitor mit IC50s von 1.13, 1.07, 0.74, 0.33, 0.68 für NPP1, NPP2, NPP3, CA-IX, CA-XII.

  • GC73396 structure
    GC73396PRMT6-IN-3
    CAS: 2890765-10-1
    Purity: >99.00%

    PRMT6-IN-3 (Verbindung 25) ist ein selektiver PRMT6-Inhibitor mit einem IC50-Wert von 192 nM.

  • GC73407 structure
    GC73407STING agonist-26
    CAS: 2868261-48-5
    Purity: >99.00%

    STING agonist-26 (CF508) ist ein Nichtnukleotid-kleinmolekularer STING-Agonist.