Interactions among biomacromolecules, predominantly noncovalent, underpin biological
processes. However, recent advancements in biospecific chemistry have enabled the …

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

Binding via reversible covalent bond formation presents a novel and powerful mechanism to
enhance the potency of synthetic inhibitors for therapeutically important proteins. Work on …

Electrophilic small molecules that can reversibly modify proteins are of growing interest in
drug discovery. However, the ability to study reversible covalent probes in live cells can be …

Natural products perennially serve as prolific sources of drug leads and chemical probes,
fueling the development of numerous therapeutics. Despite their scarcity, natural products …

Besides vaccines, the development of antiviral drugs targeting SARS-CoV-2 is critical for
preventing future COVID outbreaks. The SARS-CoV-2 main protease (Mpro), a cysteine …

Small molecule drugs that covalently bind irreversibly to their target proteins have several
advantages over conventional reversible inhibitors. They include increased duration of …

Click chemistry has been proven to be very useful in drug delivery. Due to the availability of
a large number of click reactions with a various characteristics, selection of appropriate …

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 …

Fragment based drug discovery has long been used for the identification of new ligands and
interest in targeted covalent inhibitors has continued to grow in recent years, with high …