Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X **e, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

Ongoing clinical trials of nonviral siRNA therapeutics

EA Narasipura, R VanKeulen-Miller, Y Ma… - Bioconjugate …, 2023 - ACS Publications
Short interfering RNAs (siRNA) are a powerful class of genetic medicines whose clinical
translation can be hindered by their suboptimal delivery properties in vivo. Here, we provide …

Systems approaches to investigate the role of NF-κB signaling in aging

M Haga, M Okada - Biochemical Journal, 2022 - portlandpress.com
The nuclear factor-κB (NF-κB) signaling pathway is one of the most well-studied pathways
related to inflammation, and its involvement in aging has attracted considerable attention. As …

Targeting key proteins involved in transcriptional regulation for cancer therapy: Current strategies and future prospective

H Pei, W Guo, Y Peng, H **ong… - Medicinal Research …, 2022 - Wiley Online Library
The key proteins involved in transcriptional regulation play convergent roles in cellular
homeostasis, and their dysfunction mediates aberrant gene expressions that underline the …

Regulating protein–RNA interactions: advances in targeting the LIN28/Let-7 pathway

GK Oyejobi, X Yan, P Sliz, L Wang - International Journal of Molecular …, 2024 - mdpi.com
Originally discovered in C. elegans, LIN28 is an evolutionarily conserved zinc finger RNA-
binding protein (RBP) that post-transcriptionally regulates genes involved in developmental …

A split intein and split luciferase-coupled system for detecting protein-protein interactions

Z Yao, J Kim, B Geng, J Chen, V Wong… - Molecular Systems …, 2024 - embopress.org
Elucidation of protein-protein interactions (PPIs) represents one of the most important
methods in biomedical research. Recently, PPIs have started to be exploited for drug …

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 …

USP7 deubiquitinates KRAS and promotes non-small cell lung cancer

B Huang, D Cao, X Yuan, Y **ong, B Chen, Y Wang… - Cell Reports, 2024 - cell.com
RAS oncogenic mutations are pivotal drivers of tumorigenesis. Ubiquitination modulates
RAS functions, including activation, stability, and localization. While several E3 ligases …

Design and validation of a reporter mouse to study the dynamic regulation of TFEB and TFE3 activity through in vivo imaging techniques

E Brunialti, N Rizzi, R Pinto-Costa, A Villa, A Panzeri… - Autophagy, 2024 - Taylor & Francis
ABSTRACT TFEB and TFE3 belong to the MiT/TFE family of transcription factors that bind
identical DNA responsive elements in the regulatory regions of target genes. They are …