Discovery and Characterization of a Novel Cereblon-Recruiting PRC1 Bridged PROTAC Degrader

M Kabir, L Qin, K Luo, Y Xiong, RA Sidi… - Journal of Medicinal …, 2024 - ACS Publications
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 …

[HTML][HTML] Current status of oligonucleotide-based protein degraders

PC Shih, M Naganuma, Y Demizu, M Naito - Pharmaceutics, 2023 - mdpi.com
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 …

[HTML][HTML] Taming transcription factors with TRAFTACs

CSC Ng, SM Banik - Cell chemical biology, 2021 - cell.com
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 …

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 …

[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 …

[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 …

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 …

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 …

[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 …

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 …