[HTML][HTML] Principles for targeting RNA with drug-like small molecules

KD Warner, CE Hajdin, KM Weeks - Nature reviews Drug discovery, 2018 - nature.com
RNA molecules are essential for cellular information transfer and gene regulation, and
RNAs have been implicated in many human diseases. Messenger and non-coding RNAs …

Targeting mRNA processing as an anticancer strategy

J Desterro, P Bak-Gordon… - Nature Reviews Drug …, 2020 - nature.com
Discoveries in the past decade have highlighted the potential of mRNA as a therapeutic
target for cancer. Specifically, RNA sequencing revealed that, in addition to gene mutations …

Functional carbon quantum dots as medical countermeasures to human coronavirus

A Łoczechin, K Séron, A Barras… - … applied materials & …, 2019 - ACS Publications
Therapeutic options for the highly pathogenic human coronavirus (HCoV) infections are
urgently needed. Anticoronavirus therapy is however challenging, as coronaviruses are …

1, 2, 3‐Triazole hybrids with anti‐HIV‐1 activity

LS Feng, MJ Zheng, F Zhao, D Liu - Archiv der Pharmazie, 2021 - Wiley Online Library
The human immunodeficiency virus type 1 (HIV‐1) is the major etiological agent responsible
for the acquired immunodeficiency syndrome (AIDS), which is a serious infectious disease …

Transcriptome-Wide Mapping of Small-Molecule RNA-Binding Sites in Cells Informs an Isoform-Specific Degrader of QSOX1 mRNA

Y Tong, QMR Gibaut, W Rouse… - Journal of the …, 2022 - ACS Publications
The interactions between cellular RNAs in MDA-MB-231 triple negative breast cancer cells
and a panel of small molecules appended with a diazirine cross-linking moiety and an …

Structural dynamics of single SARS-CoV-2 pseudoknot molecules reveal topologically distinct conformers

K Neupane, M Zhao, A Lyons, S Munshi… - Nature …, 2021 - nature.com
The RNA pseudoknot that stimulates programmed ribosomal frameshifting in SARS-CoV-2
is a possible drug target. To understand how it responds to mechanical tension applied by …

Small molecule–RNA targeting: starting with the fundamentals

AE Hargrove - Chemical Communications, 2020 - pubs.rsc.org
The structural and regulatory elements in therapeutically relevant RNAs offer many
opportunities for targeting by small molecules, yet fundamental understanding of what drives …

Application of triazoles as bioisosteres and linkers in the development of microtubule targeting agents

MS Malik, SA Ahmed, II Althagafi, MA Ansari… - RSC Medicinal …, 2020 - pubs.rsc.org
The triazole ring system has emerged as an exciting prospect in the optimization studies of
promising lead molecules in the quest for new drugs for clinical usage. Several marketed …

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 …

Anti-frameshifting ligand active against SARS coronavirus-2 is resistant to natural mutations of the frameshift-stimulatory pseudoknot

K Neupane, S Munshi, M Zhao, DB Ritchie… - Journal of molecular …, 2020 - Elsevier
Abstract SARS-CoV-2 uses− 1 programmed ribosomal frameshifting (− 1 PRF) to control
expression of key viral proteins. Because modulating− 1 PRF can attenuate the virus …