Fragment-to-lead medicinal chemistry publications in 2021

L Walsh, DA Erlanson, IJP de Esch… - Journal of medicinal …, 2023 - ACS Publications
This Perspective is the seventh in an annual series that summarizes successful Fragment-to-
Lead (F2L) case studies published in a given year. A tabulated summary of relevant articles …

Riboswitches as drug targets for antibiotics

V Panchal, R Brenk - Antibiotics, 2021 - mdpi.com
Riboswitches reside in the untranslated region of RNA and regulate genes involved in the
biosynthesis of essential metabolites through binding of small molecules. Since their …

Exploring the Druggability of Conserved RNA Regulatory Elements in the SARS‐CoV‐2 Genome

S Sreeramulu, C Richter, H Berg… - Angewandte …, 2021 - Wiley Online Library
SARS‐CoV‐2 contains a positive single‐stranded RNA genome of approximately 30 000
nucleotides. Within this genome, 15 RNA elements were identified as conserved between …

Brief report: Gender identity differences in autistic adults: Associations with perceptual and socio-cognitive profiles

RJ Walsh, L Krabbendam, J Dewinter… - Journal of autism and …, 2018 - Springer
Prior research has shown an elevation in autism traits and diagnoses in individuals seen for
gender related consultation and in participants self-identifying as transgender. To …

19 F NMR viewed through two different lenses: ligand-observed and protein-observed 19 F NMR applications for fragment-based drug discovery

CR Buchholz, WCK Pomerantz - RSC chemical biology, 2021 - pubs.rsc.org
19F NMR has emerged as a powerful tool in drug discovery, particularly in fragment-based
screens. The favorable magnetic resonance properties of the fluorine-19 nucleus, the …

Contemporary progress and opportunities in RNA-targeted drug discovery

AL Garner - ACS Medicinal Chemistry Letters, 2023 - ACS Publications
The surprising discovery that RNAs are the predominant gene products to emerge from the
human genome catalyzed a renaissance in RNA biology. It is now well-understood that …

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 …

Low-molecular weight small molecules can potently bind RNA and affect oncogenic pathways in cells

BM Suresh, Y Akahori, A Taghavi… - Journal of the …, 2022 - ACS Publications
RNA is challenging to target with bioactive small molecules, particularly those of low
molecular weight that bind with sufficient affinity and specificity. In this report, we developed …

Applications of solution NMR in drug discovery

L Shi, N Zhang - Molecules, 2021 - mdpi.com
During the past decades, solution nuclear magnetic resonance (NMR) spectroscopy has
demonstrated itself as a promising tool in drug discovery. Especially, fragment-based drug …

Fragment‐Based Drug Discovery for RNA Targets

KP Lundquist, V Panchal, CH Gotfredsen… - …, 2021 - Wiley Online Library
Rapid development within the fields of both fragment‐based drug discovery (FBDD) and
medicinal targeting of RNA provides possibilities for combining technologies and methods in …