Dubianok Yuliya, Kumar Anand, Rak Alexey
Sanofi R&D, Bio Structure and Biophysics at Integrated Drug Discovery, Vitry-sur-Seine, France.
Methods Mol Biol. 2025;2905:17-49. doi: 10.1007/978-1-0716-4418-8_2.
Structural biology is catalyzing a paradigm shift in drug discovery towards rational approaches in target identification and validation. Leveraging structural insights obtained through cryo-EM or X-ray crystallography not only enhances the efficiency of drug discovery projects in terms of time and cost, but also significantly improves the likelihood of achieving market approval.Initiating a successful project necessitates more than just a robust package for target credentialing; it demands a comprehensive strategy for the identification and optimization of potential drugs. The critical evaluation of target druggability is markedly enhanced when supported by experimentally derived structural information. This nuanced approach ensures a more thorough understanding of the technical feasibility of drug development from the project's inception.
结构生物学正在推动药物发现领域的范式转变,朝着在靶点识别和验证中采用合理方法的方向发展。利用通过冷冻电镜或X射线晶体学获得的结构见解,不仅能在时间和成本方面提高药物发现项目的效率,还能显著提高获得市场批准的可能性。启动一个成功的项目不仅需要一个强有力的靶点认证方案,还需要一个全面的潜在药物识别和优化策略。当有实验得出的结构信息支持时,对靶点可成药性的关键评估会显著增强。这种细致入微的方法可确保从项目启动之初就能更全面地了解药物开发的技术可行性。