Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …

Thalidomide and its derivatives are powerful cancer therapeutics that are among the best-
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …

Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …

Proteolysis targeting chimeras (PROTACs) are bifunctional compounds that recruit an E3
ligase to a target protein to induce ubiquitination and degradation of the target. Rational …

Conditional protein degradation tags (degrons) are usually> 100 amino acids long or are
triggered by small molecules with substantial off-target effects, thwarting their use as specific …

Bruton tyrosine kinase (BTK) is an important signaling hub that activates the B-cell receptor
(BCR) signaling cascade. BCR activation can contribute to the growth and survival of B-cell …

Targeted protein degradation (TPD) is an emerging pharmacologic strategy. It relies on
small-molecule “degraders” that induce proximity of a component of an E3 ubiquitin ligase …

HDAC8 can mediate signals by using its enzymatic or nonenzymatic functions, which are
expected to be critical for various types of cancer. Herein, we employed proteolysis targeting …

BRD9 is a pivotal epigenetic factor involved in cancers and inflammatory diseases. Still, the
limited selectivity and poor phenotypic activity of targeted agents make it an atypically …

The precise and safe treatment of bioorthogonal prodrug system is hindered by separate
administration of prodrug and its activator, which often results in poor therapeutic effects and …