Institute of Parasitology, Vetsuisse Faculty, University of Bern, Länggass-Strasse 122, 3012 Bern, Switzerland.
Proteomics and Mass Spectrometry Core Facility, Department for BioMedical Research (DBMR), University of Bern, Länggass-Strasse 122, 3012 Bern, Switzerland.
Int J Mol Sci. 2024 Jun 24;25(13):6903. doi: 10.3390/ijms25136903.
Identification of drug targets and biochemical investigations on mechanisms of action are major issues in modern drug development. The present article is a critical review of the classical "one drug"-"one target" paradigm. In fact, novel methods for target deconvolution and for investigation of resistant strains based on protein mass spectrometry have shown that multiple gene products and adaptation mechanisms are involved in the responses of pathogens to xenobiotics rather than one single gene or gene product. Resistance to drugs may be linked to differential expression of other proteins than those interacting with the drug in protein binding studies and result in complex cell physiological adaptation. Consequently, the unraveling of mechanisms of action needs approaches beyond proteomics. This review is focused on protozoan pathogens. The conclusions can, however, be extended to chemotherapies against other pathogens or cancer.
药物靶点的鉴定和作用机制的生化研究是现代药物开发的主要问题。本文对经典的“一种药物-一种靶点”范式进行了批判性的回顾。事实上,基于蛋白质质谱的新型靶标去卷积和耐药株研究方法表明,多种基因产物和适应机制参与了病原体对异生物的反应,而不是单一的基因或基因产物。药物耐药性可能与药物结合研究中与药物相互作用的蛋白质不同的其他蛋白质的差异表达有关,并导致复杂的细胞生理适应。因此,作用机制的阐明需要超越蛋白质组学的方法。本综述重点介绍了原生动物病原体。然而,这些结论可以扩展到针对其他病原体或癌症的化疗。