Laboratory of Cell Biology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
Proc Natl Acad Sci U S A. 2013 Jan 15;110(3):1065-70. doi: 10.1073/pnas.1212431110. Epub 2012 Dec 31.
The pH 6 antigen (Psa) of Yersinia pestis consists of fimbriae that bind to two receptors: β1-linked galactosyl residues in glycosphingolipids and the phosphocholine group in phospholipids. Despite the ubiquitous presence of either moiety on the surface of many mammalian cells, Y. pestis appears to prefer interacting with certain types of human cells, such as macrophages and alveolar epithelial cells of the lung. The molecular mechanism of this apparent selectivity is not clear. Site-directed mutagenesis of the consensus choline-binding motif in the sequence of PsaA, the subunit of the Psa fimbrial homopolymer, identified residues that abolish galactosylceramide binding, phosphatidylcholine binding, or both. The crystal structure of PsaA in complex with both galactose and phosphocholine reveals separate receptor binding sites that share a common structural motif, thus suggesting a potential interaction between the two sites. Mutagenesis of this shared structural motif identified Tyr126, which is part of the choline-binding consensus sequence but is found in direct contact with the galactose in the structure of PsaA, important for both receptor binding. Thus, this structure depicts a fimbrial subunit that forms a polymeric adhesin with a unique arrangement of dual receptor binding sites. These findings move the field forward by providing insights into unique types of multiple receptor-ligand interactions and should steer research into the synthesis of dual receptor inhibitor molecules to slow down the rapid progression of plague.
鼠疫耶尔森氏菌的 pH6 抗原(Psa)由菌毛组成,可与两种受体结合:糖脂中的β1 连接半乳糖基残基和磷脂中的磷酸胆碱基团。尽管这两种物质在许多哺乳动物细胞表面普遍存在,但鼠疫耶尔森氏菌似乎更倾向于与某些类型的人类细胞相互作用,如巨噬细胞和肺的肺泡上皮细胞。这种明显选择性的分子机制尚不清楚。对 Psa 菌毛同聚体亚单位 PsaA 序列中胆碱结合模体的定点突变,确定了破坏半乳糖神经酰胺结合、磷脂酰胆碱结合或两者的残基。PsaA 与半乳糖和磷酸胆碱复合物的晶体结构揭示了共享共同结构模体的单独受体结合位点,从而表明两个位点之间可能存在相互作用。对这个共享结构模体的突变鉴定出了 Tyr126,它是胆碱结合共识序列的一部分,但在 PsaA 的结构中与半乳糖直接接触,对两种受体的结合都很重要。因此,该结构描绘了一个带有独特排列的双重受体结合位点的菌毛亚单位,形成了一种聚合性黏附素。这些发现通过提供对独特类型的多种受体-配体相互作用的深入了解,推动了该领域的发展,并应引导研究合成双重受体抑制剂分子,以减缓鼠疫的快速发展。