Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …

A total of 378 novel drugs and 27 biosimilars approved by the US Food and Drug
Administration (FDA) between 2010 and 2019 were evaluated according to approval …

Abstract RAS mutations (HRAS, NRAS, and KRAS) are among the most common
oncogenes, and around 19% of patients with cancer harbor RAS mutations. Cells harboring …

With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …

Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …

The ability to regulate membrane protein abundance offers great opportunities for
developing therapeutic sites for various diseases. Herein, we describe a platform for the …

Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique
for new drug discovery and development. Currently, the largest challenge in the molecular …

Hydrophobic tagging (HyT) is a potential therapeutic strategy for targeted protein
degradation (TPD). Norbornene was discovered as an unprecedented hydrophobic tag in …