Department of Pharmacy, Shree Dev Bhoomi Institute of Education, Science and Technology, Veer Madho Singh Bhandari Uttarakhand Technical University, Dehradun, Uttarakhand, India.
Department of Pharmacy, School of Medical and Allied Sciences, Galgotias University, Greater Noida, Uttar Pradesh, India.
Curr Protein Pept Sci. 2024;25(3):226-243. doi: 10.2174/0113892037268777231013154850.
Bioconjugation techniques have emerged as powerful tools for enhancing the stability and targeting efficiency of protein and peptide therapeutics. This review provides a comprehensive analysis of the various bioconjugation strategies employed in the field. The introduction highlights the significance of bioconjugation techniques in addressing stability and targeting challenges associated with protein and peptide-based drugs. Chemical and enzymatic bioconjugation methods are discussed, along with crosslinking strategies for covalent attachment and site-specific conjugation approaches. The role of bioconjugation in improving stability profiles is explored, showcasing case studies that demonstrate successful stability enhancement. Furthermore, bioconjugation techniques for ligand attachment and targeting are presented, accompanied by examples of targeted protein and peptide therapeutics. The review also covers bioconjugation approaches for prolonging circulation and controlled release, focusing on strategies to extend half-life, reduce clearance, and design-controlled release systems. Analytical characterization techniques for bioconjugates, including the evaluation of conjugation efficiency, stability, and assessment of biological activity and targeting efficiency, are thoroughly examined. considerations and clinical applications of bioconjugated protein and peptide therapeutics, including pharmacokinetic and pharmacodynamic considerations, as well as preclinical and clinical developments, are discussed. Finally, the review concludes with an overview of future perspectives, emphasizing the potential for novel conjugation methods and advanced targeting strategies to further enhance the stability and targeting efficiency of protein and peptide therapeutics.
生物缀合技术已成为增强蛋白质和肽类治疗药物稳定性和靶向效率的有力工具。本文对该领域中使用的各种生物缀合策略进行了全面分析。引言部分强调了生物缀合技术在解决与蛋白质和肽类药物相关的稳定性和靶向挑战方面的重要性。本文讨论了化学和酶促生物缀合方法，以及用于共价连接的交联策略和定点缀合方法。探讨了生物缀合在改善稳定性方面的作用，展示了成功增强稳定性的案例研究。此外，还介绍了用于配体连接和靶向的生物缀合技术，并提供了靶向蛋白质和肽类治疗药物的实例。本文还涵盖了用于延长循环和控制释放的生物缀合方法，重点介绍了延长半衰期、减少清除率和设计控制释放系统的策略。深入研究了生物缀合物的分析表征技术，包括缀合效率、稳定性以及生物活性和靶向效率评估。讨论了生物缀合蛋白和肽类治疗药物的考虑因素和临床应用，包括药代动力学和药效学考虑因素，以及临床前和临床开发情况。最后，本文总结了未来展望，强调了新型缀合方法和先进靶向策略的潜力，以进一步提高蛋白质和肽类治疗药物的稳定性和靶向效率。
