European Journal of Medicinal Chemistry Reports (Dec 2024)

Advancements, challenges, and future frontiers in covalent inhibitors and covalent drugs: A review

  • Muhammad Salman Hameed,
  • Hongxuan Cao,
  • Li Guo,
  • Lei Zeng,
  • Yanliang Ren

Journal volume & issue
Vol. 12
p. 100217

Abstract

Read online

Recent progress in the realm of covalent inhibitors and covalent drugs, placing a distinct emphasis on precisely defining the scope and outlining key objectives. The scope of this review encompasses a broad examination of various classes of covalent inhibitors and drugs, with a focus on their mechanisms, applications, and limitations. Specifically, we discuss the chemical principles underlying covalent interactions in drug design and delve into the structural features that render these compounds effective in their respective targets. Our objectives include summarizing recent research progress in the development and application of covalent inhibitors and drugs, identifying key challenges faced by researchers and clinicians, and proposing future directions for advancing the field. By synthesizing current knowledge and addressing emerging trends, this review aims to contribute to a deeper understanding of covalent inhibitors and drugs and to inspire further research efforts towards their development and optimization.

Keywords