Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

Emerging variants of SARS‐CoV‐2 and potential novel epidemic coronaviruses underline
the importance of investigating various viral proteins as potential drug targets. The papain …

The SARS-CoV-2 pandemic has triggered global efforts to develop therapeutics. The main
protease of SARS-CoV-2 (Mpro), critical for viral replication, is a key target for therapeutic …

The concept of functional groups (FGs), sets of connected atoms that can determine the
intrinsic reactivity of the parent molecule and in part are responsible for the overall …

Glutathione peroxidase 4 (GPX4) is a promising target to induce ferroptosis for the treatment
of triple-negative breast cancer (TNBC). We designed and synthesized a novel series of …

Covalent inhibition has become more accepted in the past two decades, as illustrated by the
clinical approval of several irreversible inhibitors designed to covalently modify their target …

Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …

The covalent inhibition of a target protein has gained widespread attention in the field of
drug discovery. Most of the current covalent drugs utilize the high reactivity of cysteines …

Covalent drugs have experienced significant renewed interest in drug discovery. This
resurgence has been accompanied by a better understanding of the reactivity relationships …

Molecules that possess the ability to form irreversible covalent bonds with their targets are
well established in drug development with various examples clinically approved, 1, 2 and …