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(4794)

  • GC73644 structure
    GC73644NT-0796
    CAS: 2272917-13-0
    Purity: >99.00%

    NT-0796 هو مثبط للالتهاب نشط عن طريق الفم و انتقائي و مخترق للجهاز العصبي المركزي NLRP3.

  • GC73647 structure
    GC73647STING-IN-7
    CAS: 899947-07-0
    Purity: >98.00%

    STING-IN-7 (مركب 21) هو مثبط قوي من STING مع IC50 من 11.5 نانومتر.

  • GC73678 structure
    GC73678RMC-4998
    CAS: 2642037-07-6
    Purity: >96.00%

    RMC-4998 هو مثبط نشط عن طريق الفم يستهدف الحالة النشطة أو المرتبطة GTP من الطافرة KRASG12C.

  • GC73688 structure
    GC73688Hydroxy-PP-Me
    CAS: 833481-77-9
    Purity: >99.00%

    Hydroxy-PP-Me هو مثبط قوي ومحدد CBR1 مع IC50 من 759 نانومتر. "دروكسي بي بي مي" يمنع موت الخلايا المبرمج الناجم عن انسحاب المصل.

  • GC73697 structure
    GC73697STM3006
    CAS: 2499664-52-5
    Purity: >97.00%

    STM3006 هو مثبط عالي الفعالية، انتقائي ونشيط فمويا METTL3 (IC50: 5 نانومتر).

  • GC73702 structure
    GC73702NSC 689534
    CAS: 907958-80-9
    Purity: >96.00%

    NSC 689534 يمكن أن تشكل مخلبات النحاس مع Cu2+.

  • GC73730 structure
    GC73730RL-6-Me-7-OH
    CAS: 2184-54-5
    Purity: >96.00%

    ينشط RL-6-Me-7-OH خلايا MAIT البشرية والفأرية (EC50=25µM).

  • GC73740 structure
    GC73740DCZ5418
    CAS: 2883709-99-5
    Purity: >99.00%

    DCZ5418 هو مثبط لـ TRIP13.

  • GC73744 structure
    GC73744JAB-2485
    CAS: 2899209-55-1
    Purity: >98.00%

    JAB-2485 هو مثبط قوي وانتقائي لأنزيم أورورا كيناز أ (AURKA)، مع IC50 من 0.33 نانومتر.

  • GC73750 structure
    GC73750GLPG3312
    CAS: 2340388-72-7
    Purity: >98.00%

    GLPG3312 (المركب 28) هو مثبط انتقائي pan-SIK مع قيم IC50 من 2.0 نانومتر و 0.7 نانومتر و 0.6 نانومتر لكل من SIK1 و SIK2 و SIK3 على التوالي.

  • GC73760 structure
    GC73760Trilexium
    CAS: 1983180-82-0
    Purity: >99.00%

    (ديسمبر 2018) Trilexium (TRX-E-009-1) هو الجيل الثالث من البنزوبيران المرتبط ببنية TRX-E-002-1.

  • GC73767 structure
    GC73767PKM2-IN-6
    CAS: 771467-00-6
    Purity: >98.00%

    PKM2-IN-6 (المركب 7d) هو مثبط فعال وفعال عن طريق الفم PKM2 مع قيمة IC50 من 23 نانومتر.

  • GC73773 structure
    GC73773PLK1/BRD4-IN-5
    Purity: >99.00%

    PLK1/BRD4-IN-5 (مركب SC10) هو مثبط PLK1 و BRD4 نشط عن طريق الفم مع قيم IC50 من 0.3 من نانومتر و 60.8 من نانومتر، على التوالي.

  • GC73774 structure
    GC73774YCH2823
    Purity: >99.00%

    YCH2823 مثبط لـ USP7 (IC50 = 49.6 نانومتر ؛ Kd = 0.117 ميكرومتر).

  • GC73786 structure
    GC73786ARV-393
    CAS: 2851885-95-3
    Purity: >98.00%

    ARV-393 هو بروتاك (PROTAC) نشط عن طريق الفم يستخدم نظام يوبيكتين البروتيني لاستهداف تحلل BCL6.

  • GC73793 structure
    GC73793PSMA binder-1
    CAS: 2170653-14-0
    Purity: >98.00%

    PSMA binder-1 هو ربيطة لـ PSMA ويمكن استخدامه لتجميع Ac-PSMA-trillium.

  • GC73794 structure
    GC73794PSMA binder-2
    CAS: 2149567-00-8
    Purity: >97.00%

    PSMA binder-2 هو ربيطة لـ PSMA ويمكن استخدامه لتجميع Ac-PSMA-trillium.

  • GC73795 structure
    GC73795T-1-PMPA
    CAS: 1323883-62-0
    Purity: >99.00%

    T-1-PMPA هو مثبط قوي EGFR مع خصائص الاستماتة.

  • GC73796 structure
    GC73796CVN293
    CAS: 2815296-08-1
    Purity: >99.00%

    CVN293 هو مثبط انتقائي ونفاذ للدماغ لأيون البوتاسيوم قناة KCNK13 مع IC50s من 41 نانومتر و 28 نانومتر ل hKCNK13 و mKCNK13 على التوالي.

  • GC73808 structure
    GC73808Glutor
    CAS: 2561471-22-3
    Purity: >99.00%

    Glutor هو مثبط انتقائي من GLUT 1/2/3 يمكن أن يقمع امتصاص الجلوكوز.

  • GC73813 structure
    GC73813IOX5
    Purity: >99.00%

    IOX5 هو مثبط انتقائي لبرول دروكسيلاز (PHD).

  • GC73822 structure
    GC73822GNE-900
    CAS: 1200126-26-6
    Purity: >99.00%

    يعتبر GNE-900 مثبط ChK1 تنافسي ال ATP-، انتقائي، ونشيط عن طريق الفم مع IC50s من 0.0011، 1.5 µM ل ChKl، ChK2، على التوالي.

  • GC73865 structure
    GC73865SNX281
    CAS: 2332803-84-4
    Purity: >99.00%

    SNX281 هو ناهض STING نشط جهازيًا يرتبط بالبروتين STING، ويعزز نقل الإشارة من مسار cGAS-STING، ويزيد من الاستجابات الخلوية لخلايا الورم.

  • GC73867 structure
    GC73867Balinatunfib (SAR-441566)
    CAS: 2248726-53-4
    Purity: >98.00%

    TNFα activity modulator 3 (مثال 6) هو مُعدل لنشاط TNF الذي يثبط تنشيط NF κB المستحث بواسطة TNFα، ويمكن استخدامه في الأبحاث ذات الصلة.