Homo-PROTACs for the chemical knockdown of cereblon
C Steinebach, S Lindner, ND Udeshi… - ACS chemical …, 2018 - ACS Publications
The immunomodulatory drugs (IMiDs) thalidomide, lenalidomide, and pomalidomide, all
approved for the treatment of multiple myeloma, induce targeted ubiquitination and …
approved for the treatment of multiple myeloma, induce targeted ubiquitination and …
Genetic predisposition to MDS: clinical features and clonal evolution
AL Kennedy, A Shimamura - … Journal of the American Society of …, 2019 - ashpublications.org
Myelodysplastic syndrome (MDS) typically presents in older adults with the acquisition of
age-related somatic mutations, whereas MDS presenting in children and younger adults is …
age-related somatic mutations, whereas MDS presenting in children and younger adults is …
[HTML][HTML] PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective
Abstract Mouse double minute 2 (MDM2) is an E3 ubiquitin ligase which effectively
degrades tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt …
degrades tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt …
[HTML][HTML] Advancing targeted protein degradation for metabolic diseases therapy
QQ Zhou, HT Xiao, F Yang, YD Wang, P Li… - Pharmacological …, 2023 - Elsevier
The development and application of traditional drugs represented by small molecule
chemical drugs and biological agents, especially inhibitors, have become the mainstream …
chemical drugs and biological agents, especially inhibitors, have become the mainstream …
Specific knockdown of endogenous tau protein by peptide-directed ubiquitin-proteasome degradation
TT Chu, N Gao, QQ Li, PG Chen, XF Yang, YX Chen… - Cell chemical …, 2016 - cell.com
Tau, an important pathological protein of Alzheimer's disease (AD), can mediate the toxicity
of amyloid β (Aβ). Thus, reduction of Tau with chemical molecules may offer a novel strategy …
of amyloid β (Aβ). Thus, reduction of Tau with chemical molecules may offer a novel strategy …
Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders
Cyclin-dependent kinase 6 (CDK6) is an important regulator of the cell cycle. Together with
CDK4, it phosphorylates and inactivates retinoblastoma (Rb) protein. In tumour cells, CDK6 …
CDK4, it phosphorylates and inactivates retinoblastoma (Rb) protein. In tumour cells, CDK6 …
Selective CK1α degraders exert antiproliferative activity against a broad range of human cancer cell lines
G Nishiguchi, LG Mascibroda, SM Young… - Nature …, 2024 - nature.com
Molecular-glue degraders are small molecules that induce a specific interaction between an
E3 ligase and a target protein, resulting in the target proteolysis. The discovery of molecular …
E3 ligase and a target protein, resulting in the target proteolysis. The discovery of molecular …
Reversible dual-covalent molecular locking of the 14-3-3/ERRγ protein–protein interaction as a molecular glue drug discovery approach
BA Somsen, RJC Schellekens… - Journal of the …, 2023 - ACS Publications
Molecules that stabilize protein–protein interactions (PPIs) are invaluable as tool
compounds for biophysics and (structural) biology, and as starting points for molecular glue …
compounds for biophysics and (structural) biology, and as starting points for molecular glue …
[HTML][HTML] Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs
Abstract The von Hippel-Lindau (VHL) and cereblon (CRBN) proteins are substrate
recognition subunits of two ubiquitously expressed and biologically important Cullin RING …
recognition subunits of two ubiquitously expressed and biologically important Cullin RING …
Targeted protein degradation: current and future challenges
Traditional approaches in the development of small-molecule drugs typically aim to inhibit
the biochemical activity of functional protein domains. In contrast, targeted protein …
the biochemical activity of functional protein domains. In contrast, targeted protein …