Recent advances of degradation technologies based on PROTAC mechanism

M Xiao, J Zhao, Q Wang, J Liu, L Ma - Biomolecules, 2022 - mdpi.com
PROTAC (proteolysis-targeting chimeras), which selectively degrades target proteins, has
become the most popular technology for drug development in recent years. Here, we …

Systematic potency and property assessment of VHL ligands and implications on PROTAC design

J Krieger, FJ Sorrell, AA Wegener, B Leuthner… - …, 2023 - Wiley Online Library
Herein, we describe a systematic SAR‐and SPR‐investigation of the peptidomimetic
hydroxy‐proline based VHL‐ligand VH032, from which most to‐date published VHL …

Pervasive transcriptome interactions of protein-targeted drugs

L Fang, WA Velema, Y Lee, L Xiao, MG Mohsen… - Nature Chemistry, 2023 - nature.com
The off-target toxicity of drugs targeted to proteins imparts substantial health and economic
costs. Proteome interaction studies can reveal off-target effects with unintended proteins; …

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

Y Zhong, F Chi, H Wu, Y Liu, Z Xie, W Huang… - European journal of …, 2022 - Elsevier
Targeted protein degradation technology has evolved a brand-new therapeutic modality
from an innovative drug discovery perspective. Though the classical PROTACs has …

Targeted miR-34a delivery with PD1 displayed bacterial outer membrane vesicles-coated zeolitic imidazolate framework nanoparticles for enhanced tumor therapy

C Cui, Q He, J Wang, J Kang, W Ma, Y Nian… - International Journal of …, 2023 - Elsevier
MicroRNA (miRNA) has been widely used as an effective gene drug for tumor therapy, but
its chemical instability limited its therapeutic application in vivo. In this research, we fabricate …

Targeting the epigenome to reinvigorate T cells for cancer immunotherapy

D Xiong, L Zhang, ZJ Sun - Military Medical Research, 2023 - Springer
Cancer immunotherapy using immune-checkpoint inhibitors (ICIs) has revolutionized the
field of cancer treatment; however, ICI efficacy is constrained by progressive dysfunction of …

A hybrid structure determination approach to investigate the druggability of the nucleocapsid protein of SARS-CoV-2

G Padroni, M Bikaki, M Novakovic… - Nucleic Acids …, 2023 - academic.oup.com
The pandemic caused by SARS-CoV-2 has called for concerted efforts to generate new
insights into the biology of betacoronaviruses to inform drug screening and development …

Targeting ribonucleases with small molecules and bifunctional molecules

L Borgelt, P Wu - ACS Chemical Biology, 2023 - ACS Publications
Ribonucleases (RNases) cleave and process RNAs, thereby regulating the biogenesis,
metabolism, and degradation of coding and noncoding RNAs. Thus, small molecules …

Fragment-based approaches to identify RNA binders

BM Suresh, A Taghavi, JL Childs-Disney… - Journal of medicinal …, 2023 - ACS Publications
Although fragment-based drug discovery (FBDD) has been successfully implemented and
well-explored for protein targets, its feasibility for RNA targets is emerging. Despite the …

Discovery of RNA-targeted small molecules through the merging of experimental and computational technologies

EC Morishita - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
Introduction The field of RNA-targeted small molecules is rapidly evolving, owing to the
advances in experimental and computational technologies. With the identification of several …