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 …

Targeted protein degradation: An important tool for drug discovery for “Undruggable” tumor transcription factors

M Dai, S Radhakrishnan, R Li, R Tan… - … in Cancer Research …, 2022 - journals.sagepub.com
Conventional small-molecule drugs (SMDs) are compounds characterized by low molecular
weight, high cell permeability, and high selectivity. In clinical translation, SMDs are regarded …

Antitumor Effect of Anti‐c‐Myc Aptamer‐Based PROTAC for Degradation of the c‐Myc Protein

Y Wang, G Yang, X Zhang, R Bai, D Yuan… - Advanced …, 2024 - Wiley Online Library
Targeting “undruggable” targets with intrinsically disordered structures is of great
significance for the treatment of disease. The transcription factor c‐Myc controls global gene …

[HTML][HTML] NFIC mediates m6A mRNA methylation to orchestrate transcriptional and post-transcriptional regulation to represses malignant phenotype of non-small cell …

K Shi, Y Chen, R Liu, X Fu, H Guo, T Gao… - Cancer Cell …, 2024 - Springer
Background Multiple genetic and epigenetic regulatory mechanisms are crucial in the
development and tumorigenesis process. Transcriptional regulation often involves intricate …

[HTML][HTML] Targeted protein degradation: A promising approach for cancer treatment

MZI Khan, A Nazli, I Naz, D Khan, I Haq… - Journal of Pharmaceutical …, 2023 - Elsevier
Targeted protein degradation (TPD) is a promising approach that has the ability to address
disease-causing proteins. Compared to traditional inhibition, proteolysis targeting chimera …

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

X Zhao, Y Chen, H Su, L Zhang - Interdisciplinary Medicine, 2023 - Wiley Online Library
Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD)
technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells. A …

Selective Proteolysis of Activated Transcriptional Factor by NIR‐Responsive Palindromic DNA Thalidomide Conjugate Inhibits the Canonical Smad Pathway

M Hou, R Guo, T Ren, T Wang, JH Jiang, J He - Small, 2023 - Wiley Online Library
Dysfunctional transcription factors that activate abnormal expressions of specific proteins are
often associated with the progression of various diseases. Despite being attractive drug …

[HTML][HTML] Protocol for the generation and purification of high-molecular-weight covalent RNA-DNA hybrids with T4 RNA ligase

O Laguía, G Bosso, J Martínez-Torrecuadrada… - STAR protocols, 2024 - Elsevier
RNA-DNA covalent hybrids (RDHs) are widely employed in biology. Although RDHs can be
manufactured, the synthesis of molecules longer than 120 nucleotides is challenging. Here …