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 …

Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …

The epidermal growth factor receptor (EGFR) belongs to the ERBB family of tyrosine kinase
receptors. EGFR signaling cascade is a key regulator in cell proliferation, differentiation …

Fluoroorganic chemistry has become essential in the evolution of many different but
interconnected research fields. These include the development of new materials with a …

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 …

Although covalent inhibitors have been used as therapeutics for more than a century, there
has been general resistance in the pharmaceutical industry against their further …

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 …

The clinical and commercial success of covalent drugs has prompted a renewed and more
deliberate pursuit of covalent and irreversible mechanisms within drug discovery. A covalent …

Introduction: Cancer is a devastating disease; however, several therapeutic advances have
recently been made, wherein EGFR and its family members have emerged as useful …

Protein kinases are a large family of approximately 530 highly conserved enzymes that
transfer a γ-phosphate group from ATP to a variety of amino acid residues, such as tyrosine …