Oestrogens and their receptors contribute broadly to physiology and diseases. In
premenopausal women, endogenous oestrogens protect against cardiovascular, metabolic …

Small-molecule drug discovery has traditionally focused on occupancy of a binding site that
directly affects protein function, and this approach typically precludes targeting proteins that …

Estrogen receptor alpha (ERα) is a well-established therapeutic target for the treatment of
ER-positive (ER+) breast cancers. Despite the tremendous successes achieved with …

The actions of estrogens and related estrogenic molecules are complex and multifaceted in
both sexes. A wide array of natural, synthetic, and therapeutic molecules target pathways …

KRAS is the most frequently mutated oncogene found in pancreatic, colorectal, and lung
cancers. Although it has been challenging to identify targeted therapies for cancers …

There are several challenges towards the development and clinical use of small molecule
inhibitors, which are currently the main type of targeted therapies towards intracellular …

The current inhibitor‐based approach to therapeutics has inherent limitations owing to its
occupancy‐based model: 1) there is a need to maintain high systemic exposure to ensure …

Defects in the functions of RNA binding proteins (RBPs) are at the origin of many diseases;
however, targeting RBPs with conventional drugs has proven difficult. PROTACs are a new …

Traditional pharmaceutical drug discovery is almost exclusively focused on directly
controlling protein activity to cure diseases. Modulators of protein activity, especially …

Selective degradation of proteins by proteolysis targeting chimeras (PROTACs) offers a
promising potential alternative to protein inhibition for therapeutic intervention. Current …