Serafin Pawel, Kleczkowska Patrycja
Military Institute of Hygiene and Epidemiology, 01-163 Warsaw, Poland.
Maria Sklodowska-Curie, Medical Academy in Warsaw, Solidarnosci 12 Str., 03-411 Warsaw, Poland.
Pharmaceutics. 2023 Nov 7;15(11):2597. doi: 10.3390/pharmaceutics15112597.
Recently, bombesin (BN) and its analogs have attracted much attention as excellent anticancer agents because they interact with specific receptors widely distributed on the surface of various cancer cells. However, their biological properties proceed far beyond this, given a broad spectrum of activity. Bombesin receptor ligands are effective drugs for the treatment of rheumatoid arthritis or gastrointestinal diseases. However, most diseases are complex, and the use of polytherapy may lead to pharmacokinetic and pharmacodynamic drug-drug interactions, resulting in side effects. Therefore, there is a need to develop effective compounds that also contain BN or its analogs, which are combined with other structural entities, thus generating a so-called hybrid drug. Hybrid drugs that contain bombesin pharmacophore(s) may be proposed as a solution to the problem of polytherapy or the lack of an effective cure. Such structures have now demonstrated the desired efficacy, though information on these aforementioned compounds is relatively scarce. Therefore, our paper aims to encourage researchers to focus on bombesins. Herein, we indicate that the hybrid approach should also be firmly applied to bombesins and the BN receptor family. This paper's structure is divided into two main sections demonstrating bombesins and their properties, as well as recent data on bombesin-based hybrid compounds and their potential usefulness in medicine. Overall, it refers to the discovery and synthesis of modified bombesin-based hybrid compounds.
最近,蛙皮素(BN)及其类似物作为优秀的抗癌药物备受关注,因为它们能与广泛分布于各种癌细胞表面的特定受体相互作用。然而,鉴于其广泛的活性谱,它们的生物学特性远不止于此。蛙皮素受体配体是治疗类风湿性关节炎或胃肠道疾病的有效药物。然而,大多数疾病都很复杂,联合治疗可能会导致药代动力学和药效学方面的药物相互作用,从而产生副作用。因此,有必要开发同时含有BN或其类似物且与其他结构实体相结合的有效化合物,即所谓的杂合药物。含有蛙皮素药效团的杂合药物可能是解决联合治疗问题或缺乏有效治疗方法的一种方案。这类结构现已显示出预期的疗效,不过关于上述化合物的信息相对较少。因此,我们的论文旨在鼓励研究人员关注蛙皮素。在此,我们指出杂合方法也应坚定地应用于蛙皮素和BN受体家族。本文结构分为两个主要部分,分别展示蛙皮素及其特性,以及基于蛙皮素的杂合化合物的最新数据及其在医学上的潜在用途。总体而言,本文涉及基于修饰蛙皮素的杂合化合物的发现与合成。