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

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 …

Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …

Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been
developed for inducing the protein degradation by a targeting molecule. This technology …

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for
targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly …

CARM1 is amplified or overexpressed in many cancer types, and its overexpression
correlates with poor prognosis. Potent small-molecule inhibitors for CARM1 have been …

Highlights•Degraders are an emerging modality which fall into the 'beyond rule of
5'space.•Poor permeability and solubility are critical features limiting oral absorption.• …

Glioma is a primary aggressive brain tumor with high recurrence rate. The poor efficiency of
chemotherapeutic drugs crossing the blood‒brain barrier (BBB) is well-known as one of the …

Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that
utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI) …

Heterobifunctional proteolysis-targeting chimeric compounds leverage the activity of E3
ligases to induce degradation of target oncoproteins and exhibit potent preclinical antitumor …