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)

  • GC73413 structure
    GC73413ARC186 sodium
    Purity: >94.00%

    ARC186 sodium es un aptámero no conjude de 40KDa PEG con una secuencia idéntica a 0 Avacincaptad pegol ARC1905 sódico.

  • GC73417 structure
    GC73417CASP8-IN-1
    CAS: 1956368-39-0
    Purity: >98.00%

    CASP8-IN-1 (compuesto 63-R) es un inhibiselectivo de la caspasa 8 (CASP8), con una IC50 de 0,7 μM.

  • GC73424 structure
    GC73424PRT062607 acetate
    CAS: 1370261-98-5
    Purity: >99.00%

    PRT062607 acetate es un inhibidor de Syk disponible por vía oral (IC50: 1 nM) que inhila la inflamación y la Apoptosis por inducción.

  • GC73428 structure
    GC73428CWI1-2 hydrochloride
    CAS: 2408590-37-2
    Purity: >98.00%

    CWI1-2 hydrochloride es un inhibidor de IGF2BP2 que se une a IGF2BP2 e inhisu interacción con los transcritos objetivo m6a modificados, induce apoptosis y diferenciación.

  • GC73441 structure
    GC73441EAPB 02303
    CAS: 1958290-51-1
    Purity: >99.00%

    EAPB 02303 es un agente disrupde microtúbulos e inhibidor.

  • GC73452 structure
    GC73452CCT374705
    CAS: 2640647-90-9
    Purity: >99.00%

    CCT374705 es un inhibidor de BCL6 activo por vía oral con potentes efectos antiproliferativos in vitro.

  • GC73469 structure
    GC73469Cereblon inhibitor 2
    CAS: 2639380-62-2
    Purity: >98.00%

    Cereblon inhibitor 2 (compuesto 8) es un inhibidor de Cereblon útil en la investigación de tumores sólidos, especialmente cáncer de mama.

  • GC73476 structure
    GC73476MYC-RIBOTAC
    Purity: >98.00%

    MYC-RIBOTAC es una quimribonucleasa (RIBOTAC) dirigida a MYC Internal ribosome entry site (IRES).

  • GC73491 structure
    GC73491RapaBlock
    CAS: 2474076-02-1
    Purity: >98.00%

    RapaBlock es un potente ligando FKBP12, no inmunosuprese e impermeal cerebro.

  • GC73494 structure
    GC73494MSU-42011
    CAS: 2456434-36-7
    Purity: >98.00%

    MSU-42011 es un agonista oral activo del receptor retinox (RXR).

  • GC73501 structure
    GC73501Wu-5
    CAS: 2630378-05-9
    Purity: >98.00%

    Wu-5 es un inhibidor de USP10 que puede inhibir las vías FLT3 y AMPK, inducir degradación FLT3-ITD e inducir apoptosis.

  • GC73541 structure
    GC73541PRMT5-IN-31
    Purity: >99.00%

    PRMT5-IN-31 (compuesto 3m) es un inhibidor selectivo de PRMT5 (IC50: 0.31 μM).

  • GC73543 structure
    GC73543FC-116
    CAS: 2417298-29-2
    Purity: >98.00%

    FC-116 es un inhibidor de la tubulina que inhieficazmente el crecimiento tumoral en ratones.

  • GC73552 structure
    GC73552TIM-3-IN-2
    CAS: 1113126-49-0
    Purity: >99.00%

    TIM-3-IN-2 (compuesto A-41) es un inhibidor de Tim3 (KD: 0.61 μM).

  • GC73555 structure
    GC73555PI3Kδ-IN-16
    CAS: 2766437-35-6
    Purity: >99.00%

    PI3Kδ-IN-16 es un potente y selectivo inhibidor del PI3Kδ.

  • GC73561 structure
    GC73561YS-363
    CAS: 2470908-90-6
    Purity: >99.00%

    YS-363 es un potente inhibidor del EGFR, con IC50s de 0,96 nM y 0,67 nM para las formas mutantes de EGFR de tipo salvaje y L858R, respectivamente.

  • GC73567 structure
    GC73567Os30
    CAS: 2998928-68-8
    Purity: >98.00%

    Os30, un potente inhibidor de EGFR de cuarta generación, es un potente inhibidor de EGFRC797S-TK con valores de IC50 de 18 nM y 113 nM para EGFRDel19/T790M/C797S TK y EGFRL858R/T790M/C797S TK, respectivamente.

  • GC73569 structure
    GC73569MY-1076
    CAS: 3008262-76-5
    Purity: >99.00%

    MY-1076 es un inhibidor de YAP.

  • GC73571 structure
    GC73571Tubulin polymerization-IN-56
    CAS: 2966790-98-5
    Purity: >99.00%

    Tubulin polymerization-IN-56, un derivado del indazol, es un potente inhibide la polimeride de tubulina a través de la interacción con el sitio de colchicina, lo que resulta en la detención del ciclo celular y la apoptosis celular.

  • GC73572 structure
    GC73572PP5-IN-1
    CAS: 1022417-69-1
    Purity: >99.00%

    PP5-IN-1 (compuesto P053) es un inhibicompetitivo de la proteína serina/treonina fosfatasa-5 (PP5) que se une a su dominio catalítico y causa apoptosis en el cáncer renal.

  • GC73576 structure
    GC73576Enpp-1-IN-19
    CAS: 2738583-25-8
    Purity: >99.00%

    Enpp-1-IN-19 (compuesto 29f) es un inhibidor de ENPP1 activo por vía oral que inhila la hidrólidel cGAMP por ENPP1 (IC50=68 nM).

  • GC73579 structure
    GC73579DDO-2728
    CAS: 3029515-97-4
    Purity: >98.50%

    DDO-2728 (compuesto 19) es un inhibiselectivo AlkB homologue 5 (ALKBH5) con una IC50 de 2,97 μM.

  • GC73594 structure
    GC73594KH16
    Purity: >98.00%

    KH16 es un potente y bajo nanomolar inhibidor de HDAC.

  • GC73599 structure
    GC73599TH9619
    CAS: 2379556-22-4
    Purity: >99.00%

    TH9619 es un potente inhibidor de las actividades de la dedrogenasa y la ciclodrolasa tanto en MTHFD1 como en MTHFD2 con un valor de IC50 de 47 nM, y destruye selectivamente las células cancerosas.