The transcriptional upregulation of oncogenes is a driving force behind the progression of
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …

Rheumatoid arthritis (RA) is a chronic immune-mediated disease that primarily affects the
synovium of diarthrodial joints. During the course of RA, the synovium transforms into a …

Epigenetic alternations concern heritable yet reversible changes in histone or DNA
modifications that regulate gene activity beyond the underlying sequence. Epigenetic …

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 …

The epigenetic modifications of histones are versatile marks that are intimately connected to
development and disease pathogenesis including human cancers. In this review, we will …

The two tandem bromodomains of the BET (bromodomain and extraterminal domain)
proteins enable chromatin binding to facilitate transcription. Drugs that inhibit both …

Proteins of the bromodomain and extra-terminal (BET) domain family are epigenetic readers
that bind acetylated histones through their bromodomains to regulate gene transcription …

Innate immunity serves as the rapid and first-line defense against invading pathogens, and
this process can be regulated at various levels, including epigenetic mechanisms. The …

Many drugs, or their antecedents, were discovered through observation of their effects on
normal or disease physiology. For the past generation, this phenotypic drug discovery …

Sulfoximines have been largely disregarded in medicinal chemistry for a long time.
However, recently, they have risen to the apparent level of stardom on the drug discovery …