We report the discovery of ARD-2051 as a potent and orally efficacious androgen receptor
(AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM …

Targeted protein degradation via small-molecule modulation of cereblon offers vast potential
for the development of new therapeutics. Cereblon-binding therapeutics carry the safety …

Target-protein degradation is an emerging field in drug discovery and development. In
particular, the substrate-receptor proteins of the cullin–ubiquitin ligase system play a key …

Importance Myelodysplastic neoplasms (MDS), formerly known as myelodysplastic
syndromes, are clonal hematopoietic malignancies that cause morphologic bone marrow …

Abstract “Molecular glue”(MG) is a term coined to describe the mechanism of action of the
plant hormone auxin and subsequently used to characterize synthetic small molecule …

Molecular glue degraders are small, drug-like compounds that induce interactions between
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …

Control of protein levels by nucleic-acid-based technologies has proven to be a useful
research tool but lacks the advantages of small molecules with respect to cell permeability …

The drugs lenalidomide and pomalidomide bind to the protein cereblon, directing the CRL4–
CRBN E3 ligase toward the transcription factors Ikaros and Aiolos to cause their …

Sickle cell disease (SCD) is a prevalent, life-threatening condition attributable to a heritable
mutation in β-hemoglobin. Therapeutic induction of fetal hemoglobin (HbF) can ameliorate …

Purpose: Estrogen receptor (ER) alpha signaling is a known driver of ER-positive
(ER+)/human epidermal growth factor receptor 2 negative (HER2−) breast cancer …