Progress in strategies aimed at breaking down therapeutic target proteins has led to a
paradigm shift in drug discovery. Thalidomide and its derivatives are the only protein …

In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …

A platform to accelerate optimization of proteolysis targeting chimeras (PROTACs) has been
developed using a direct-to-biology (D2B) approach with a focus on linker effects. A large …

ABSTRACT Introduction: Proteolysis–targeting chimeras (PROTACs) have emerged as a
new modality with the potential to revolutionize drug discovery. PROTACs are …

Ubiquitination is a key post-translational modification of proteins, affecting the regulation of
multiple cellular processes. Cells are equipped with over 600 ubiquitin orchestrators, called …

Thalidomide, originally developed as a sedative drug, causes multiple defects due to severe
teratogenicity, but it has been re-purposed for treating multiple myeloma, and derivatives …

Eleven novel benzoxazole/benzothiazole‐based thalidomide analogs were designed and
synthesized to obtain new effective antitumor immunomodulatory agents. The synthesized …

Succinimides are well recognized heterocyclic compounds in drug discovery which produce
diverse therapeutically related applications in pharmacological practices. Researches in …

Glutarimides such as thalidomide, pomalidomide, and lenalidomide are the most frequently
used ligands to recruit E3 ubiquitin ligase cereblon (CRBN) for the development of …

Cereblon (CRBN) is a ubiquitously expressed E3 ligase substrate receptor and a key player
in pharmaceutical targeted protein degradation. Despite substantial insight gained into its …