靶向先天免疫 cGAS - STING - TBK1 信号通路的小分子。
关键词: ABZI, amidobenzimidazole ACMA, 9-amino-6-chloro-2-methoxyacridine AMP, adenosine monophosphate ATP, adenosine triphosphate Anti-tumor BNBC, 6-bromo-N-(naphthalen-1-yl)benzo[d][1,3]dioxole-5-carboxamide CBD, cyclic dinucleotide-binding domain CDA, cyclic diadenosine monophosphate (c-di-AMP) CDG, cyclic diguanosine monophosphate (c-di-GMP) CDN, cyclic dinucleotide CMA, 10-carboxymethyl-9-acridanone CTD, C-terminal domain CTLA-4, cytotoxic T lymphocyte associated protein 4 CTT, C-terminal tail CXCL, chemokine (C-X-C motif) ligand DC50, concentration for 50% degradation DCs, dendritic cells DMXAA, 5,6-dimethylxanthenone-4-acetic acid DSDP, dispiro diketopiperzine EM, cryo-electron microscopy ENPP1, ecto-nucleotide pyrophosphatase/phosphodiesterase ER, endoplasmic reticulum FAA, flavone-8-acetic acid FDA, U.S. Food and Drug Administration FP, fluorescence polarization GMP, guanosine monophosphate GTP, guanosine triphosphate HCQ, hydrochloroquine HTS, high throughput screening ICI, immune checkpoint inhibitor IKK, IκB kinase IO, immune-oncology IRF3, interferon regulatory factor 3 ISG, interferon stimulated gene ITC, isothermal titration calorimetry Immunotherapy KD, kinase domain LBD, ligand-binding domain MDCK, Madin–Darby canine kidney MG, Mangostin MI, maximum induction MLK, mixed lineage kinase MinEC5×, minimum effective concentration for inducing 5-fold luciferase activity NF-κB, nuclear factor-κB Ntase, nucleotidyl transferase PBMCs, peripheral-blood mononuclear cells PD-1, programmed death receptor 1 PD-L1, programmed death ligand 1 PDE, phosphodiesterases PDK1, 3-phosphoinositide-dependent protein kinase 1 PPi, pyrophosphoric acid PROTACs, proteolysis targeting chimeras PRRs, pattern recognition receptors QC, quinacrine SAR, structure–activity relationship SDD, scaffold and dimerization domain STAT, signal transducer and activator of transcription STING STING, stimulator of interferon genes Small molecule modulators TBK1 TBK1, TANK-binding kinase 1 THIQCs, tetrahydroisoquinolone acetic acids TNFRSF, tumor necrosis factor receptor superfamily ULD, ubiquitin-like domain VHL, von Hippel–Lindau cAIMP, cyclic adenosine-inosine monophosphate cGAMP, cyclic guanosine monophosphate-adenosine monophosphate cGAS cGAS, cyclic guanosine monophosphate-adenosine monophosphate synthase dsDNA, double-stranded DNA i.t., intratumoral
来 源:
DOI:10.1016/j.apsb.2020.03.001
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