Protein degraders-from thalidomide to new PROTACs
T Ito - The Journal of Biochemistry, 2024 - academic.oup.com
Recently, the development of protein degraders (protein-degrading compounds) has
prominently progressed. There are two remarkable classes of protein degraders: proteolysis …
prominently progressed. There are two remarkable classes of protein degraders: proteolysis …
Human IGF2 Gene Epigenetic and Transcriptional Regulation: At the Core of Developmental Growth and Tumorigenic Behavior
P Scalia, SJ Williams, Y Fujita-Yamaguchi - Biomedicines, 2023 - mdpi.com
Regulation of the human IGF2 gene displays multiple layers of control, which secures a
genetically and epigenetically predetermined gene expression pattern throughout …
genetically and epigenetically predetermined gene expression pattern throughout …
Epigenomic signatures of sarcomatoid differentiation to guide the treatment of renal cell carcinoma
Renal cell carcinoma with sarcomatoid differentiation (sRCC) is associated with poor
survival and a heightened response to immune checkpoint inhibitors (ICIs). Two major …
survival and a heightened response to immune checkpoint inhibitors (ICIs). Two major …
Discovery and Characterization of a Novel Cereblon-Recruiting PRC1 Bridged PROTAC Degrader
Bridged PROTAC is a novel protein complex degrader strategy that exploits the target
protein's binding partner to degrade undruggable proteins by inducing proximity to an E3 …
protein's binding partner to degrade undruggable proteins by inducing proximity to an E3 …
[HTML][HTML] Current status of oligonucleotide-based protein degraders
Transcription factors (TFs) and RNA-binding proteins (RBPs) have long been considered
undruggable, mainly because they lack ligand-binding sites and are equipped with flat and …
undruggable, mainly because they lack ligand-binding sites and are equipped with flat and …
Taming transcription factors with TRAFTACs
Transcription factors play central roles in numerous diseases yet are notoriously challenging
targets for drug development. In this issue of Cell Chemical Biology, Samarasinghe et …
targets for drug development. In this issue of Cell Chemical Biology, Samarasinghe et …
In vivo synthetic chemistry of proteolysis targeting chimeras (PROTACs)
S Tomoshige, M Ishikawa - Bioorganic & Medicinal Chemistry, 2021 - Elsevier
Chemical knockdown of therapeutic targets using proteolysis targeting chimeras (PROTACs)
is a rapidly developing field in drug discovery, but PROTACs are bifunctional molecules that …
is a rapidly developing field in drug discovery, but PROTACs are bifunctional molecules that …
Emerging target discovery and drug repurposing opportunities in chordoma
DM Freed, J Sommer, N Punturi - Frontiers in Oncology, 2022 - frontiersin.org
The development of effective and personalized treatment options for patients with rare
cancers like chordoma is hampered by numerous challenges. Biomarker-guided …
cancers like chordoma is hampered by numerous challenges. Biomarker-guided …
[HTML][HTML] Expanding the horizons of targeted protein degradation: A non-small molecule perspective
X Huang, F Wu, J Ye, L Wang, X Wang, X Li… - … Pharmaceutica Sinica B, 2024 - Elsevier
Targeted protein degradation (TPD) represented by proteolysis targeting chimeras
(PROTACs) marks a significant stride in drug discovery. A plethora of innovative …
(PROTACs) marks a significant stride in drug discovery. A plethora of innovative …
Two in one: the emerging concept of bifunctional antibodies
K Rhee, X Zhou - Current Opinion in Biotechnology, 2024 - Elsevier
Highlights•Traditional antibodies block ligand binding or drive Fc effector
functions.•Bifunctional antibodies function through an induced proximity …
functions.•Bifunctional antibodies function through an induced proximity …