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 …
[HTML][HTML] 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 …
[HTML][HTML] 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 …
The emerging role of targeted protein degradation to treat and study cancer
MH Brodermann, EK Henderson… - The Journal of …, 2024 - Wiley Online Library
The evolution of cancer treatment has provided increasingly targeted strategies both in the
upfront and relapsed disease settings. Small‐molecule inhibitors and immunotherapy have …
upfront and relapsed disease settings. Small‐molecule inhibitors and immunotherapy have …
[HTML][HTML] On the identification of differentially-active transcription factors from ATAC-seq data
F Gerbaldo, E Sonder, V Fischer, S Frei, J Wang… - bioRxiv, 2024 - ncbi.nlm.nih.gov
ATAC-seq has emerged as a rich epigenome profiling technique, and is commonly used to
identify Transcription Factors (TFs) underlying given phenomena. A number of methods can …
identify Transcription Factors (TFs) underlying given phenomena. A number of methods can …
Novel design strategies to enhance the efficiency of proteolysis targeting chimeras
C Zhao, FJ Dekker - ACS Pharmacology & Translational Science, 2022 - ACS Publications
Despite the success of drug discovery over the past decades, many potential drug targets
still remain intractable for small molecule modulation. The development of proteolysis …
still remain intractable for small molecule modulation. The development of proteolysis …