Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands.
Bioorg Med Chem. 2010 Jan 15;18(2):675-88. doi: 10.1016/j.bmc.2009.11.060. Epub 2009 Dec 6.
Human cytomegalovirus (HCMV) is a widespread human pathogen, possessing onco-modulatory properties. Constitutive signaling of the HCMV-encoded chemokine receptor US28 and its ability to bind a broad spectrum of chemokines might facilitate HCMV-associated tumor progression. Novel nonpeptidergic chemotypes were identified as neutral antagonists or inverse agonists on US28, that allosterically inhibit chemokine binding to US28.
人巨细胞病毒(HCMV)是一种广泛存在的人类病原体,具有致癌调节特性。HCMV 编码的趋化因子受体 US28 的组成性信号转导及其与广泛谱的趋化因子结合的能力可能促进 HCMV 相关的肿瘤进展。新型非肽类化学型被鉴定为 US28 的中性拮抗剂或反向激动剂,它们变构抑制趋化因子与 US28 的结合。