There is a resurging interest in compounds that engage their target through covalent
interactions. Cysteine's thiol is endowed with enhanced reactivity, making it the nucleophile …

Covalent protein inhibitors have found considerable utility in medicinal chemistry and
chemical biology. Chemical probes and drugs have been rationally designed and fine-tuned …

Over the past decade targeted covalent inhibitors have undergone a renaissance due to the
clinical validation and regulatory approval of several small molecule therapeutics that are …

Covalent inhibitors are widely used in drug discovery and chemical biology. Although
covalent inhibitors are frequently designed to react with noncatalytic cysteines, many ligand …

Targeted covalent inhibitors have become an integral part of a number of therapeutic
protocols and are the subject of intense research. The mechanism of action of these …

Covalent inhibition is a rapidly growing discipline within drug discovery. Many historical
covalent inhibitors were discovered by serendipity, with such a mechanism of action often …

Covalent inhibitors are experiencing a growing resurgence in drug design and are an
increasingly useful tool in molecular biology. The ability to attach inhibitors to their targets by …

In contrast to the traditional mechanism of drug action that relies on the reversible,
noncovalent interaction of a ligand with its biological target, a targeted covalent inhibitor …

Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

Targeted covalent enzyme inhibition is experiencing resurgence as a medicinal chemistry
design strategy. Targeted covalent inhibitors exhibit slow target offset, increased binding …