Ronald J. Quinn
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View article: Democratized Discovery of Microsclerodermin F as an Immunophilin Ligand
Democratized Discovery of Microsclerodermin F as an Immunophilin Ligand Open
While immunophilins are well-recognized therapeutic targets, several members of this family of peptidyl-proline isomerases (PPIases) have yet to be subjected to ligand discovery efforts. In this study, we demonstrate a cost-effective means…
View article: The value of universally available raw NMR data for transparency, reproducibility, and integrity in natural product research
The value of universally available raw NMR data for transparency, reproducibility, and integrity in natural product research Open
Covering: up to 2018With contributions from the global natural product (NP) research community, and continuing the Raw Data Initiative, this review collects a comprehensive demonstration of the immense scientific value of disseminating raw…
View article: Correction: The value of universally available raw NMR data for transparency, reproducibility, and integrity in natural product research
Correction: The value of universally available raw NMR data for transparency, reproducibility, and integrity in natural product research Open
Correction for 'The value of universally available raw NMR data for transparency, reproducibility, and integrity in natural product research'
Inner-mitochondrial membrane protein <i>Pf</i>MPV17 is linked to <i>P. falciparum in vitro</i> resistance to the indoloquinolizidine alkaloid alstonine Open
Background There are an estimated 260 million malaria cases and ∼600 000 deaths annually. Challenges to malaria eradication include the lack of highly effective and broadly applicable vaccines and parasite drug resistance. This is driving …
View article: New sesquiterpenoids with anti-inflammatory effects from phytopathogenic fungus Bipolaris sorokiniana 11134
New sesquiterpenoids with anti-inflammatory effects from phytopathogenic fungus Bipolaris sorokiniana 11134 Open
Sesquiterpenoids represent a structurally diverse class of natural products widely recognized for their ecological significance and pharmacological potential, including antimicrobial, anti-inflammatory, and anticancer properties. As part o…
Discovery of Lithospermate B as a Potential Ligand for the Malarial E2 Ubiquitin-Conjugating Enzyme via Multiplexed Native Mass Spectrometry Open
There is an urgent need for novel therapeutics to combat Plasmodium falciparum, especially in light of increasing drug resistance. Here, we present a multiplexed native mass spectrometry (MS) platform capable of simultaneously screening mu…
dFLASH; dual FLuorescent transcription factor activity sensor for histone integrated live-cell reporting and high-content screening Open
Live-cell transcription factor (TF) activity reporting is crucial for synthetic biology, drug discovery and functional genomics. Here we present dFLASH (dual FLuorescent transcription factor Activity Sensor for Histone-integrated live-cell…
Nuclear Magnetic Resonance Fingerprinting and Principal Component Analysis Strategies Lead to Anti-Tuberculosis Natural Product Discovery from Actinomycetes Open
Background: The increasing prevalence of drug-resistant tuberculosis (TB) underscores the urgent need for novel antimicrobial agents. Methods: This study integrates cultivation optimization, nuclear magnetic resonance (NMR) fingerprinting,…
Natural Product Graveoline Modulates Kirsten Rat Sarcoma Viral Oncogene Homologue (KRAS) Membrane Association: Insights from Advanced Spectroscopic Studies Open
The KRAS gene plays a pivotal role in numerous cancers by encoding a GTPase that upon association with the plasma membrane activates the MAPK pathway, promoting cellular proliferation. In our study, we investigated small molecules that dis…
Rapid Discovery of Antimicrobial and Antimalarial Agents from Natural Product Fragments Open
Fragment-based drug discovery (FBDD) focuses on small compounds, known as fragments, typically with a molecular weight of less than 300 Da. This study highlights the benefits of employing a pure natural product library for FBDD, contrastin…
A Screening of 10,240 NatureBank Fractions Identifies Nematicidal Activity in Agelasine-Containing Extracts from Sponges Open
Nematode infections affect a fifth of the human population, livestock, and crops worldwide, imposing a burden to global public health and economies, particularly in developing nations. Resistance to commercial anthelmintics has increased o…
Advancing Kir4.2 Channel Ligand Identification through Collision-Induced Affinity Selection Mass Spectrometry Open
The inwardly rectifying potassium Kir4.2 channel plays a crucial role in regulating membrane potentials and maintaining potassium homeostasis. Kir4.2 has been implicated in various physiological processes, including insulin secretion, gast…
Identification of Ligands for Ion Channels: TRPM2 Open
Transient receptor potential melastatin 2 (TRPM2) is a calcium‐permeable, nonselective cation channel with a widespread distribution throughout the body. It is involved in many pathological and physiological processes, making it a potentia…
dFLASH; dual FLuorescent transcription factor Activity Sensor for Histone integrated live-cell reporting and high-content screening Open
Live-cell reporting of regulated transcription factor (TF) activity has a wide variety of applications in synthetic biology, drug discovery, and functional genomics. As a result, there is high value in the generation of versatile, sensitiv…
Dereplication of the Termite Gut-associated Actinomycete Metabolome as a Source of Bioactive Secondary Metabolites Open
Natural products (NPs) and their derivatives have historically played a vital role in drug discovery by serving as invaluable sources of therapeutic agents and potential drug leads. Among the established sources of NPs, microorganisms have…
dFLASH; dual FLuorescent transcription factor Activity Sensor for Histone integrated live-cell reporting and high-content screening Open
Live-cell reporting of regulated transcription factor (TF) activity has a wide variety of applications in synthetic biology, drug discovery, and functional genomics. As a result, there is high value in the generation of versatile, sensitiv…
Discovery of Anti-SARS-CoV-2 Nsp9 Binders from Natural Products by a Native Mass Spectrometry Approach Open
The search for effective antiviral agents against SARS-CoV-2 remains a critical global endeavor. In this study, we focused on the viral nucleocapsid protein Nsp9, which is a key player in viral RNA replication and an attractive drug target…
The mechanism of cleavage of Evans chiral auxiliaries by LiOOH: origins of the different regioselectivities obtained with LiOH, LiOOH, LiOBn and LiSBn Open
Oxazolidinones are widely used as chiral auxiliaries in asymmetric synthesis. The chiral auxiliary can be selectively removed using LiOOH, LiOBn or LiSBn, but not LiOH, which instead favours endocyclic cleavage with opening of the oxazolid…
Drug-Repurposing Screening Identifies a Gallic Acid Binding Site on SARS-CoV-2 Non-structural Protein 7 Open
SARS-CoV-2 is the agent responsible for acute respiratory disease COVID-19 and the global pandemic initiated in early 2020. While the record-breaking development of vaccines has assisted the control of COVID-19, there is still a pressing g…
Keynote Lecture “Anti-viral Drug Discovery for Severe Acute Respiratory Syndrome (SARS-CoV-2)” Open
Understanding molecular level interactions between the metabolome and proteome, two of the most important classes of molecules in biology, will generate deeper insight into the function of metabolites (natural products) which have a centra…
View article: The Time and Place for Nature in Drug Discovery
The Time and Place for Nature in Drug Discovery Open
The case for a renewed focus on Nature in drug discovery is reviewed; not in terms of natural product screening, but how and why biomimetic molecules, especially those produced by natural processes, should deliver in the age of artificial …
Metabolite-protein interactions: Native mass spectrometry and collision induced affinity selection mass spectrometry in natural product screening Open
Understanding molecular level interactions between the metabolome and proteome, two of the most important classes of molecules in biology, will generate deeper insight into the function of metabolites (natural products) which have a centra…
Meeting the Challenge 2: Identification of Potential Chemical Probes for Parkinson’s Disease from <i>Ligusticum chuanxiong</i> Hort Using Cytological Profiling Open
Traditional Chinese medicine (TCM) has been around for thousands of years and is increasingly gaining popularity in the Western world to treat various complex disorders including the incurable neurodegenerative condition, Parkinson's Disea…
A hnRNPA2B1 agonist effectively inhibits HBV and SARS-CoV-2 omicron<i>in vivo</i> Open
The twenty-first century has already recorded more than ten major epidemics or pandemics of viral disease, including the devastating COVID-19. Novel effective antivirals with broad-spectrum coverage are urgently needed. Herein, we reported…
Collision-Induced Affinity Selection Mass Spectrometry for Identification of Ligands Open
Hyphenated mass spectrometry has been used to identify ligands binding to proteins. It involves mixing protein and compounds, separation of protein-ligand complexes from unbound compounds, dissociation of the protein-ligand complex, separa…
View article: Identifying New Ligands for JNK3 by Fluorescence Thermal Shift Assays and Native Mass Spectrometry
Identifying New Ligands for JNK3 by Fluorescence Thermal Shift Assays and Native Mass Spectrometry Open
The c-Jun N-terminal kinases (JNKs) are evolutionary highly conserved serine/threonine kinases. Numerous findings suggest that JNK3 is involved in the pathogenesis of neurodegenerative diseases, so the inhibition of JNK3 may be a potential…
Binding Studies of the Prodrug HAO472 to SARS-Cov-2 Nsp9 and Variants Open
SARS-CoV-2 (COVID-19) has infected over 219 million people and caused the death of over 4.55 million worldwide. In a previous screen of a natural product library against purified SARS-CoV-2 Nsp9 using a native mass spectrometry-based appro…
Turning Metabolomics into Drug Discovery Open
Metabolomics is the "omics" that studies the whole metabolome. It has a wide range of applications, inter alia chemotaxonomy, environmental influences, agriculture, etc. Here we review the application of metabolomics in natural product res…