Targeted protein degradation refers to the use of small molecules to induce the selective degradation of proteins. In its most common form, this degradation is achieved through …
PY Ting, S Borikar, JR Kerrigan, NM Thomsen… - Science, 2024 - science.org
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 …
S Yamanaka, H Furihata, Y Yanagihara, A Taya… - Nature …, 2023 - nature.com
Lenalidomide, an immunomodulatory drug (IMiD), is commonly used as a first-line therapy in many haematological cancers, such as multiple myeloma (MM) and 5q myelodysplastic …
H Yoon, JC Rutter, YD Li… - The Journal of Clinical …, 2024 - Am Soc Clin Investig
The concept of induced protein degradation by small molecules has emerged as a promising therapeutic strategy that is particularly effective in targeting proteins previously …
NR Kong, LH Jones - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Targeted protein degradation (TPD) has emerged as a potentially transformational therapeutic modality with considerable promise. Molecular glue degraders remodel the …
Y Chen, H Xue, J Jin - Journal of Biological Chemistry, 2024 - Elsevier
The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …
R Stevens, JDF Thompson, JCL Fournier… - Chemical Society …, 2024 - pubs.rsc.org
Targeted protein degraders such as PROTACs and molecular glues are a rapidly emerging therapeutic modality within industry and academia. Degraders possess unique mechanisms …
A Kroupova, VA Spiteri, ZJ Rutter, H Furihata… - Nature …, 2024 - nature.com
The ubiquitin E3 ligase cereblon (CRBN) is the target of therapeutic drugs thalidomide and lenalidomide and is recruited by most targeted protein degraders (PROTACs and molecular …
Small-molecule chemical “probes” complement the use of molecular biology techniques to explore, validate, and generate hypotheses on the function of proteins in diseases such as …