Covalent fragment-based ligand screening approaches for identification of novel ubiquitin proteasome system modulators
EM Rothweiler, PE Brennan, KVM Huber - Biological Chemistry, 2022 - degruyter.com
Ubiquitination is a key regulatory mechanism vital for maintenance of cellular homeostasis.
Protein degradation is induced by E3 ligases via attachment of ubiquitin chains to …
Protein degradation is induced by E3 ligases via attachment of ubiquitin chains to …
Targeted protein degradation as an antiviral approach
A Chakravarty, PL Yang - Antiviral research, 2023 - Elsevier
Targeted protein degradation (TPD) has emerged as a new modality in drug discovery. In
this approach, small molecules are used to drive degradation of the target protein of interest …
this approach, small molecules are used to drive degradation of the target protein of interest …
The application of ubiquitin ligases in the PROTAC drug design
Y Chen, J Jin - Acta Biochimica et Biophysica Sinica, 2020 - academic.oup.com
Protein ubiquitylation plays important roles in many biological activities. Protein
ubiquitylation is a unique process that is mainly controlled by ubiquitin ligases. The ubiquitin …
ubiquitylation is a unique process that is mainly controlled by ubiquitin ligases. The ubiquitin …
The genetics of myelodysplastic syndromes and the opportunities for tailored treatments
CN Kontandreopoulou, K Kalopisis, NA Viniou… - Frontiers in …, 2022 - frontiersin.org
Genomic instability, microenvironmental aberrations, and somatic mutations contribute to the
phenotype of myelodysplastic syndrome and the risk for transformation to AML. Genes …
phenotype of myelodysplastic syndrome and the risk for transformation to AML. Genes …
Unlocking DCAFs To Catalyze Degrader Development: An Arena for Innovative Approaches
Chemically induced proximity-based targeted protein degradation (TPD) has become a
prominent paradigm in drug discovery. With the clinical benefit demonstrated by certain …
prominent paradigm in drug discovery. With the clinical benefit demonstrated by certain …
Chemical modulation of pre-mRNA splicing in mammalian systems
RE Boer, ZR Torrey, JS Schneekloth Jr - ACS Chemical Biology, 2020 - ACS Publications
RNA splicing is a key component of gene expression and proteomic diversity in humans.
The spliceosome assembles on and processes individual nascent pre-mRNA transcripts into …
The spliceosome assembles on and processes individual nascent pre-mRNA transcripts into …
An updated patent review of BRD4 degraders
Introduction Bromodomain-containing protein 4 (BRD4), an important epigenetic reader, is
closely associated with the pathogenesis and development of many diseases, including …
closely associated with the pathogenesis and development of many diseases, including …
Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders
SCC Lucas, A Ahmed, SN Ashraf… - Journal of Medicinal …, 2024 - ACS Publications
Unlocking novel E3 ligases for use in heterobifunctional PROTAC degraders is of high
importance to the pharmaceutical industry. Over-reliance on the current suite of ligands used …
importance to the pharmaceutical industry. Over-reliance on the current suite of ligands used …
Targeted protein degradation in CNS disorders: a promising route to novel therapeutics?
S Kuemper, AG Cairns, K Birchall, Z Yao… - Frontiers in Molecular …, 2024 - frontiersin.org
Targeted protein degradation (TPD) is a rapidly expanding field, with various PROTACs
(proteolysis-targeting chimeras) in clinical trials and molecular glues such as …
(proteolysis-targeting chimeras) in clinical trials and molecular glues such as …
Targeted protein degradation via intramolecular bivalent glues
O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - bioRxiv, 2023 - biorxiv.org
Targeted protein degradation is a drug modality represented by compounds that recruit a
target to an E3 ubiquitin ligase to promote target ubiquitination and proteasomal …
target to an E3 ubiquitin ligase to promote target ubiquitination and proteasomal …