Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …

Proteomics is the field of study that includes the analysis of proteins, from either a basic
science prospective or a clinical one. Proteins can be investigated for their abundance …

Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-
dependent degradation of proteins. TPD is of interest in drug development, as it can address …

Privileged structures have been widely used as an effective template in medicinal chemistry
for drug discovery. Chalcone is a common simple scaffold found in many naturally occurring …

Abstract Cyclin-dependent kinase 9 (CDK9), an important regulator of transcriptional
elongation, is a promising target for cancer therapy, particularly for cancers driven by …

Most human proteins lack chemical probes, and several large-scale and generalizable small-
molecule binding assays have been introduced to address this problem. How compounds …

Despite advances in genetic and proteomic techniques, a complete portrait of the proteome
and its complement of dynamic interactions and modifications remains a lofty, and as of yet …

Heterobifunctional molecules that recruit E3 ubiquitin ligases, such as cereblon, for targeted
protein degradation represent an emerging pharmacological strategy. A major unanswered …

Nucleophilic amino acids make important contributions to protein function, including
performing key roles in catalysis and serving as sites for post-translational modification …

The ubiquitin system has become synonymous with the modification of lysine residues.
However, the substrate scope and diversity of the conjugation machinery have been …