Department of Biochemistry, Faculty of Science, Charles University Prague, Czech Republic.
Bioorg Med Chem. 2010 Feb 15;18(4):1434-40. doi: 10.1016/j.bmc.2010.01.015. Epub 2010 Jan 11.
We have recently identified a new class of high affinity ligands for CD69 leukocyte membrane receptor, carboxylated calixarenes. Of the three compounds investigated here, thiacalix[4]arene had the highest affinity for CD69 in direct binding assays, and proved to be the most specific inhibitor of CD69 identified so far in receptor precipitation and cellular activation experiments. Carboxylated calixarenes also proved effective at protection of CD69(high) lymphocytes from apoptosis triggered by a multivalent ligand or antibody. Thus, carboxylated calixarenes set a new paradigm for noncarbohydrate ligands for CD69 making them attractive for protection of killer cells in combined animal tumor therapies.
我们最近发现了一类新的高亲和力配体，用于 CD69 白细胞膜受体，即羧基化杯芳烃。在研究的三种化合物中，噻吩杯[4]芳烃在直接结合测定中对 CD69 具有最高的亲和力，并被证明是迄今为止在受体沉淀和细胞激活实验中鉴定的最特异的 CD69 抑制剂。羧基化杯芳烃还能有效保护 CD69(高)淋巴细胞免受多价配体或抗体触发的细胞凋亡。因此，羧基化杯芳烃为 CD69 的非碳水化合物配体开创了一个新的范例，使其成为联合动物肿瘤治疗中保护杀伤细胞的有吸引力的配体。
