Jack R. Davison
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View article: Genomic Discovery and Structure–Activity Exploration of a Novel Family of Enzyme-Activated Covalent Cyclin-Dependent Kinase Inhibitors
Genomic Discovery and Structure–Activity Exploration of a Novel Family of Enzyme-Activated Covalent Cyclin-Dependent Kinase Inhibitors Open
Fungi have historically been the source of numerous important medicinal compounds, but full exploitation of their genetic potential for drug development has been hampered in traditional discovery paradigms. Here we describe a radically dif…
View article: The genome of antibiotic-producing colonies of the Pelagophyte alga Chrysophaeum taylorii reveals a diverse and non-canonical capacity for secondary metabolism
The genome of antibiotic-producing colonies of the Pelagophyte alga Chrysophaeum taylorii reveals a diverse and non-canonical capacity for secondary metabolism Open
Chrysophaeum taylorii is a member of an understudied clade of marine algae that can be responsible for harmful coastal blooms and is known to accumulate bioactive natural products including antibiotics of the chrysophaentin class. Whole ge…
View article: Fragment expansion with NUDELs - poised DNA-encoded libraries
Fragment expansion with NUDELs - poised DNA-encoded libraries Open
Optimisation of the affinity of lead compounds is a critical challenge in the identification of drug candidates and chemical probes. Fragment-based drug discovery has become established as one of the methods of choice for drug discovery st…
View article: Fragment expansion with NUDELs – poised DNA-encoded libraries
Fragment expansion with NUDELs – poised DNA-encoded libraries Open
Fragment growing using poised DNA-encoded libraries, which allow the coupling of a targeted active fragment, allows the optimisation of fragment hits to potent compounds in a single operation, illustrated by the discovery of a 51 nM BRD4 l…
View article: Lentzeacins A-E, New Bacterial-Derived 2,5- and 2,6-Disubstituted Pyrazines from a BGC-Rich Soil Bacterium Lentzea sp. GA3-008
Lentzeacins A-E, New Bacterial-Derived 2,5- and 2,6-Disubstituted Pyrazines from a BGC-Rich Soil Bacterium Lentzea sp. GA3-008 Open
Pyrazines (1,4-diazirines) are an important group of natural products that have tremendous monetary value in the food and fragrance industries and can exhibit a wide range of biological effects including antineoplastic, antidiabetic and an…
View article: Vertirhodins A–F, C-Linked Pyrrolidine-Iminosugar-Containing Pyranonaphthoquinones from <i>Streptomyces</i> sp. B15-008
Vertirhodins A–F, C-Linked Pyrrolidine-Iminosugar-Containing Pyranonaphthoquinones from <i>Streptomyces</i> sp. B15-008 Open
Six novel pyranonaphthoquinones, vertirhodins A-F (1-6), were discovered from a soil-derived Streptomyces sp. B15-008. Their chemical structures and absolute configurations were determined using nuclear magnetic resonance and comparison of…
View article: Antimicrobial Chrysophaentin Analogs Identified from Laboratory Cultures of the Marine Microalga <i>Chrysophaeum taylorii</i>
Antimicrobial Chrysophaentin Analogs Identified from Laboratory Cultures of the Marine Microalga <i>Chrysophaeum taylorii</i> Open
A laboratory culture of the colonial marine alga Chrysophaeum taylorii NIES-1699 yielded a set of new bioactive chrysophaentin analogs, and their structures were determined by HRESIMS and NMR spectroscopy. Differences in the metabolites id…
View article: A New Natural Product Analog of Blasticidin S Reveals Cellular Uptake Facilitated by the NorA Multidrug Transporter
A New Natural Product Analog of Blasticidin S Reveals Cellular Uptake Facilitated by the NorA Multidrug Transporter Open
The permeation of antibiotics through bacterial membranes to their target site is a crucial determinant of drug activity but in many cases remains poorly understood. During screening efforts to discover new broad-spectrum antibiotic compou…
View article: Insights from NMR Spectroscopy into the Conformational Properties of Man‐9 and Its Recognition by Two HIV Binding Proteins
Insights from NMR Spectroscopy into the Conformational Properties of Man‐9 and Its Recognition by Two HIV Binding Proteins Open
Man 9 GlcNAc 2 (Man‐9) present at the surface of HIV makes up the binding sites of several HIV‐neutralizing agents and the mammalian lectin DC‐SIGN, which is involved in cellular immunity and trans‐infections. We describe the conformationa…