Pucci Michael J, Dougherty Thomas J
Achillion Pharmaceuticals, New Haven, CT, USA.
Methods Mol Med. 2008;142:131-41. doi: 10.1007/978-1-59745-246-5_11.
Key enzymes that assemble the bacterial cell wall are also the target of the Beta-lactam class of antibiotics. The covalent binding of labeled penicillin to these proteins has been used in numerous studies in drug discovery, antibiotic mechanisms of action and resistance, and cell wall physiology. Methods to label and measure penicillin binding proteins in two prototypical organisms, a Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus), are described. The methods discussed include identifying penicillin-binding proteins in both intact cells (in vivo measurements) and isolated cell membranes.
组装细菌细胞壁的关键酶也是β-内酰胺类抗生素的作用靶点。标记青霉素与这些蛋白质的共价结合已被广泛应用于药物发现、抗生素作用机制与耐药性以及细胞壁生理学等众多研究中。本文描述了在两种典型生物体中标记和测量青霉素结合蛋白的方法,这两种生物体分别是革兰氏阴性菌(大肠杆菌)和革兰氏阳性菌(金黄色葡萄球菌)。所讨论的方法包括在完整细胞(体内测量)和分离的细胞膜中鉴定青霉素结合蛋白。