Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

In recent years, the development of targeted covalent inhibitors has gained popularity
around the world. Specific groups (electrophilic warheads) form irreversible bonds with the …

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 …

Introduction Covalent drugs have been used for more than hundred years, but gathered
larger interest in the last two decades. There are currently over a 100 different electrophilic …

Covalent drugs exert potent and durable activity by chemical modification of the
endogenous target protein in vivo. To maximize the pharmacological efficacy while …

The reactive functionalities of drugs that engage in covalent interactions with the
enzyme/receptor residue in either a reversible or an irreversible manner are …

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 …

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

There has been tremendous progress in covalent inhibitors as evidenced by the ascent of
innovative electrophilic warheads with suppressed non‐specific reactivity but enhanced …