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.
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Immunology/Inflammation 相关产品(4245)
- GC73996PROTAC AR/AR-V7 degrader-1CAS: 2841308-96-9纯度: >98.00%
PROTAC AR/AR-V7 degrader-1(27c)是一种基于PROTAC的双AR AR-V7降解器,AR和AR-V7的DC50值分别为2.67和2.64μM。
- GC74013FOSL1 degrader 1纯度: 不显示
FOSL1 degrader 1(4)是一种T-5224-PROTAC,能有效降解FOSL1 (AP-1),抑制HNSCC中癌干性基因的表达。
- GC74029ASCT2-IN-1CAS: 3032651-18-3纯度: >98.00%
ASCT2-IN-1(化合物20k)是一种ASCT2抑制剂,在A549和HEK293细胞中的IC50值分别为5.6 μM和3.5 μM。
- GC74050PROTAC CDK4/6 degrader 1CAS: 3025082-14-5纯度: >98.00%
PROTAC CDK4/6 degrader 1(化合物7f)是CDK4和CDK6的双重降解剂,DC50分别为10.5和2.5 nM。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC73996 | PROTAC AR/AR-V7 degrader-1 | 2841308-96-9 | >98.00% | |
PROTAC AR/AR-V7 degrader-1(27c)是一种基于PROTAC的双AR AR-V7降解器,AR和AR-V7的DC50值分别为2.67和2.64μM。 | ||||
| GC74001 | TS-24 | 1563260-97-8 | >98.00% | |
TS-24是组织蛋白酶S的抑制剂,IC50为4.3μM。 | ||||
| GC74005 | AK59 | - | >98.00% | |
AK59是一种通过HERC4(一种HECT结构域E3连接酶)发挥作用的STING降解剂。 | ||||
| GC74007 | SelSA | 1225038-92-5 | >99.00% | |
SelSA是一种选择性的口服活性组蛋白去乙酰化酶6 (HDAC6)抑制剂,IC50为56.9 nM。 | ||||
| GC74013 | FOSL1 degrader 1 | - | 不显示 | |
FOSL1 degrader 1(4)是一种T-5224-PROTAC,能有效降解FOSL1 (AP-1),抑制HNSCC中癌干性基因的表达。 | ||||
| GC74024 | BPU | - | >99.00% | |
BPU在亚g1期阻止细胞周期进程。 | ||||
| GC74029 | ASCT2-IN-1 | 3032651-18-3 | >98.00% | |
ASCT2-IN-1(化合物20k)是一种ASCT2抑制剂,在A549和HEK293细胞中的IC50值分别为5.6 μM和3.5 μM。 | ||||
| GC74030 | ASCT2-IN-2 | - | >99.00% | |
ASCT2-IN-2(化合物25e)是一种ASCT2抑制剂,IC50为5.14μM。 | ||||
| GC74032 | Enpp-1-IN-20 | - | >98.00% | |
Enpp-1-IN-20(化合物31)是一种外核苷酸焦磷酸酶/磷酸二酯酶1 (ENPP1)抑制剂,IC50为0.09 nM。 | ||||
| GC74042 | SpiD3 | 3033533-25-1 | >98.00% | |
SpiD3是一种新型的螺环二聚体。 | ||||
| GC74045 | Zoracopan | 2243483-63-6 | >99.00% | |
Zoracopan是一种选择性补体因子D(CFD)抑制剂。 | ||||
| GC74047 | UR778Br | 866127-80-2 | >99.00% | |
UR778Br靶向IQGAP1蛋白的GTP酶激活蛋白相关结构域(GRD结构域)。 | ||||
| GC74050 | PROTAC CDK4/6 degrader 1 | 3025082-14-5 | >98.00% | |
PROTAC CDK4/6 degrader 1(化合物7f)是CDK4和CDK6的双重降解剂,DC50分别为10.5和2.5 nM。 | ||||
| GC74070 | INF 195 | 1211379-56-4 | >99.00% | |
INF 195是一种NLRP3抑制剂。 | ||||
| GC74072 | FT-FAPI-12_9 | 2883407-81-4 | >95.00% | |
FT-FAPI-12_9其可用于合成FAP靶向放射性示踪剂FAPI-46。 | ||||
| GC74073 | FT-FAPI-12_9 TFA | - | >99.00% | |
FT-FAPI-12_9 TFA是一种FAP配体,可用于合成靶向FAP的放射性示踪剂FAPI-46。 | ||||
| GC74075 | SC428 | 1898232-70-6 | >98.00% | |
SC428是一种靶向N-末端结构域的雄激素受体(AR)抑制剂。 | ||||
| GC74077 | HEI3090 | 2377167-56-9 | >99.00% | |
HEI3090是P2X7R激活剂。 | ||||
| GC74090 | Dimethyl fumarate-d2 | 23057-98-9 | >99.00% | |
Dimethyl fumarate-d2是氘标记的富马酸二甲酯。 | ||||
| GC74102 | Apomine | 126411-13-0 | >99.00% | |
Apomine (SR-45023A)是一种抑制胆固醇合成中甲羟戊酸/类异戊二烯途径的抗肿瘤药物。 | ||||
| GC74157 | EN450 | 793719-01-4 | >99.00% | |
EN450是一种针对NF-κB的半胱氨酸反应性共价分子胶降解剂。 | ||||
| GC74159 | MK-0731 | 845256-65-7 | >99.00% | |
MK-0731是一种选择性、非竞争性和变构驱动蛋白纺锤体蛋白(KSP)抑制剂,IC50为2.2 nM,pKa为7.6。 | ||||
| GC74164 | 25-Hydroxytachysterol3 | 39932-44-0 | >98.00% | |
25-Hydroxytachysterol3是维生素D3的代谢物 | ||||
| GC74187 | Salicylic acid-13C6 | 1189678-81-6 | >97.00% | |
Salicylic acid-13C6是13c标记的水杨酸。 | ||||
