Immunology & Inflammation
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CXCR4 抑制剂
MSX-122是口服可生物利用的CXCR4抑制剂（IC50 =?10 nM），具有潜在的抗肿瘤和抗病毒活性。CXCR4抑制剂MSX-122与趋化因子受体CXCR4结合，阻止基质衍生因子-1（SDF-1）与CXCR4受体和受体激活结合，这可能导致肿瘤细胞增殖和迁移减少。
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CXCR4 拮抗剂
AMD 3465 Hexahydrobromide是一种有效的选择性CXCR4拮抗剂。
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- Kentaro Suzuki, .et al. C-terminal-modifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
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CXCR4 激动剂
ATI-2341是针对C-X-C趋化因子受体4型（CXCR4）（EC50 = 194 nM）的pepducin，是一种变构激动剂，可激活抑制性异三聚体G蛋白（Gi），从而促进cAMP生成的抑制并诱导钙动员。
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CXCR4 拮抗剂
Plerixafor 8HCl (DB06809)是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性， IC50分别为44 nM和5.7 nM。
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- Mei Zheng, .et al. CXCL12 inhibits hair growth through CXCR4, Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. Bone marrow cell homing to sites of acute tibial fracture: 89Zr-oxine cell labeling with positron emission tomographic imaging in a mouse model, EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. Bone marrow cell trafficking analyzed by 89Zr-oxine positron emission tomography in a murine transplantation model, Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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CXCR4 拮抗剂
AMD3100 (Plerixafor)是用于增殖造血干细胞的免疫刺激剂，并且是用于动员造血干细胞进行移植的趋化因子受体-4拮抗剂。
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- Hitoshi Maeda, .et al. Cell-penetrating albumin enhances the sublingual delivery of antigens through macropinocytosis, Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. Brain vascular damage-induced lymphatic ingrowth is directed by Cxcl12b/Cxcr4a, Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. Effects of local vs systemic administration of CXCR4 inhibitor AMD3100 on orthodontic tooth movement in rats, Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. Positive effects of selenium supplementation on selenoprotein S expression and cytokine status in a murine model of acute liver injury, J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. Stromal cell-derived factor 1 (SDF1) attenuates platelet-derived growth factor-B (PDGF-B)-induced vascular remodeling for adipose tissue expansion in obesity, Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. Role of Prx1-expressing skeletal cells and Prx1-expression in fracture repair, Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. C-terminal?Cmodifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. Cell-penetrating mechanism of intracellular targeting albumin: Contribution of macropinocytosis induction and endosomal escape, J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. LPS-induced CXCR7 expression promotes gastric Cancer proliferation and migration via the TLR4/MD-2 pathway, Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. The role of conventional antibodies targeting the CD4 binding site and CD4-induced epitopes in the control of HIV-1 CRF01_AE viruses, Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. Microbe-dependent lymphatic migration of neutrophils modulates lymphocyte proliferation in lymph nodes, Nat Commun, 2015, 6: 7139 PMID: 25972253
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CXCR4 拮抗剂
USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
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CXCR4 拮抗剂
WZ811是4型C-X-C趋化因子受体（CXCR4）拮抗剂（EC50 = 0.3 nM）。在体外抑制CXCR4/基质细胞衍生因子1（SDF-1）介导的cAMP调节（EC50 = 1.2 nM）。
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CXCR4 receptor modulator
NSC-23026是CXCR4受体调节剂。
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CXCR4 拮抗剂
AMD 070是CXCR4趋化因子受体拮抗剂。
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- Uchida D, .et al. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells, Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. Enhancement of the CXCL12/CXCR4 axis due to acquisition of resistance in pancreatic cancer: effect of CXCR4 antagonists, BMC Cancer, 2016, 16: 305 PMID: 27175473
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CXCR4 拮抗剂
在CXCR4 125I-SDF抑制结合试验中，AMD-070 HCl是一种有效的选择性CXCR4拮抗剂，IC50值为13 nM，抑制T-4型HIV-1（NL4.3株）在MT-4细胞中的复制和PBMC。
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