VUF11207 fumarate is a highly potent chemokine receptor CXCR7 agonist (pKi=8.1). VUF11207 fumarate effectively induces the recruitment of CXCR7 and its downstream effector protein β-arrestin2 (pEC50=8.8) and promotes receptor internalization (pEC50=7.9)[1, 2]. CXCR7 is highly expressed in various malignant tumors, promoting tumor growth, angiogenesis, and metastasis[3]. VUF11207 fumarate can increase the thickness of the pleura and collagen deposition in the aorta in angiotensin II-induced hypertensive mouse model[4]. VUF11207 fumarate can prolong the antitumor effect of anti-PD-L1 antibody in glioblastoma-carrying mice[5].
References:
[1] Wijtmans M, Maussang D, Sirci F, et al. Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists[J]. European journal of medicinal chemistry, 2012, 51: 184-192.
[2] Nugraha A P, Kitaura H, Ohori F, et al. CXC receptor 7 agonist acts as a CXC motif chemokine ligand 12 inhibitor to ameliorate osteoclastogenesis and bone resorption[J]. Molecular Medicine Reports, 2022, 25(3): 78.
[3] Fan H, Wang W, Yan J, et al. Prognostic significance of CXCR7 in cancer patients: a meta-analysis[J]. Cancer cell international, 2018, 18(1): 212.
[4] Song B, Chen D, Liu Z, et al. Stromal cell-derived factor-1 exerts opposing roles through CXCR4 and CXCR7 in angiotensin II-induced adventitial remodeling[J]. Biochemical and biophysical research communications, 2022, 594: 38-45.
[5] Liu C C, Yang W B, Chien C H, et al. CXCR7 activation evokes the anti-PD-L1 antibody against glioblastoma by remodeling CXCL12-mediated immunity[J]. Cell Death & Disease, 2024, 15(6): 434.
VUF11207 fumarate是一种高效的趋化因子受体CXCR7激动剂（pKi=8.1），VUF11207 fumarate能够有效诱导CXCR7与其下游效应蛋白β-arrestin2的募集（pEC50=8.8），并促进受体的内化过程（pEC50=7.9）[1, 2]。CXCR7在多种恶性肿瘤中高表达，促进肿瘤生长、血管生成和转移[3]。VUF11207 fumarate能够增加由血管紧张素II诱导的高血压小鼠模型的胸膜外膜厚度和主动脉胶原沉积[4]。VUF11207 fumarate能够延长抗 PD-L1抗体在胶质母细胞瘤携带小鼠中的抗肿瘤效果[5]。