Department of Organic and Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100, Gliwice, Poland; Biotechnology Center of Silesian University of Technology, B. Krzywoustego 8, 44-100, Gliwice, Poland.
Department of Organic and Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100, Gliwice, Poland; Biotechnology Center of Silesian University of Technology, B. Krzywoustego 8, 44-100, Gliwice, Poland.
Eur J Pharmacol. 2020 Jan 5;866:172773. doi: 10.1016/j.ejphar.2019.172773. Epub 2019 Nov 6.
α,α-Bisphosphonates (BPs) are well established in the treatment of bone diseases such as osteoporosis and Paget's disease. Their successful application originates from their high affinity to hydroxyapatite. While the initially appreciated features of BPs are already beneficial to many patients, recent developments have further expanded their pleiotropic applications. This review describes the background of the interactions of BPs with bone cells that form the basis of the classical treatment. A better understanding of the mechanism behind their interactions allows for the parallel application of BPs against bone cancer and metastases followed by palliative pain relief. Targeted therapy with bone-seeking BPs coupled with a diagnostic agent in one particle resulted in theranostics which is also described here. For example, in such a system, BP moieties are bound to contrast agents used in magnetic resonance imaging or radionuclides used in positron emission tomography. In addition, another example of the pleiotropic function of BPs which involves targeting the imaging agents to bone tissues accompanied by pain reduction is presented in this work.
α,α-双膦酸盐（BPs）在骨质疏松症和 Pagets 病等骨骼疾病的治疗中已得到广泛应用。它们的成功应用源于其与羟磷灰石的高亲和力。虽然最初被认可的 BPs 的特性已经对许多患者有益，但最近的发展进一步扩展了它们的多效性应用。本综述描述了 BPs 与骨细胞相互作用的背景，这是经典治疗的基础。更好地了解其相互作用的机制，可以使 BPs 能够平行应用于骨癌和转移，并随后进行姑息性疼痛缓解。靶向治疗与骨靶向 BPs 结合在一个粒子中的诊断剂导致了治疗学，本文也对此进行了描述。例如，在这样的系统中，BP 部分与磁共振成像中使用的造影剂或正电子发射断层扫描中使用的放射性核素结合。此外，本文还介绍了 BPs 的另一种多效性功能的例子，即通过将成像剂靶向骨组织并同时减轻疼痛来实现。
