Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

Abstract The United States Food and Drug Administration (US FDA) has always been a
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …

The majority of therapies that target individual proteins rely on specific activity-modulating
interactions with the target protein—for example, enzyme inhibition or ligand blocking …

Most current therapies that target plasma membrane receptors function by antagonizing
ligand binding or enzymatic activities. However, typical mammalian proteins comprise …

Targeted protein degradation has emerged as a new paradigm to manipulate cellular
proteostasis. Proteolysis-targeting chimeras (PROTACs) are bifunctional small molecules …

Protein knockdown using the auxin-inducible degron (AID) technology is useful to study
protein function in living cells because it induces rapid depletion, which makes it possible to …

The high selectivity and affinity of antibodies toward their antigens have made them a highly
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …

Selective protein degradation platforms have afforded new development opportunities for
therapeutics and tools for biological inquiry. The first lysosome-targeting chimeras (LYTACs) …

Protein silencing represents an essential tool in biomedical research. Targeted protein
degradation (TPD) strategies exemplified by PROTACs are rapidly emerging as modalities …

New biological tools provide new techniques to probe fundamental biological processes.
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …