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

X Xie, 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 …

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 …

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 …

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

H Pei, W Guo, Y Peng, H Xiong… - 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 …

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 …

RNA‐Selective Small‐Molecule Ligands: Recent Advances in Live‐Cell Imaging and Drug Discovery

KH Chan, Y Wang, BX Zheng, W Long, X Feng… - …, 2023 - Wiley Online Library
RNA structures, including those formed from coding and noncoding RNAs, alternative to
protein‐based drug targets, could be a promising target of small molecules for drug …

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 …

Precision oncology revolution: CRISPR-Cas9 and PROTAC technologies unleashed

K Kanbar, R El Darzi, DE Jaalouk - Frontiers in Genetics, 2024 - frontiersin.org
Cancer continues to present a substantial global health challenge, with its incidence and
mortality rates persistently reflecting its significant impact. The emergence of precision …

Bifunctional robots inducing targeted protein degradation

ME Sobhia, H Kumar, S Kumari - European Journal of Medicinal Chemistry, 2023 - Elsevier
The gaining importance of Targeted Protein Degradation (TPD) and PROTACs (PROteolysis-
TArgeting Chimeras) have drawn the scientific community's attention. PROTACs are …

[HTML][HTML] D154Q mutation does not alter KRAS dimerization

I Grozavu, S Stuart, A Lyakisheva, Z Yao… - Journal of molecular …, 2022 - Elsevier
KRAS is one of the most frequently mutated oncogenes in human cancers. Despite nearly
40 years of research, KRAS remains largely undruggable, in part due to an incomplete …