David J. Mann
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View article: Synthesis and Functionalization of Sulfoximine‐Bicyclo[1.1.0]butanes: Functionalizable, Tuneable and Cysteine‐Selective Chiral Warheads
Synthesis and Functionalization of Sulfoximine‐Bicyclo[1.1.0]butanes: Functionalizable, Tuneable and Cysteine‐Selective Chiral Warheads Open
Electrophilic covalent warheads with appropriate reactivity and selectivity are crucial to the investigation of protein function and the discovery of therapeutics. Here we report the synthesis of sulfoximine bicyclo[1.1.0] butanes (BCBs) a…
View article: Synthesis and Functionalization of Sulfoximine‐Bicyclo[1.1.0]butanes: Functionalizable, Tuneable and Cysteine‐Selective Chiral Warheads
Synthesis and Functionalization of Sulfoximine‐Bicyclo[1.1.0]butanes: Functionalizable, Tuneable and Cysteine‐Selective Chiral Warheads Open
Electrophilic covalent warheads with appropriate reactivity and selectivity are crucial to the investigation of protein function and the discovery of therapeutics. Here we report the synthesis of sulfoximine bicyclo[1.1.0] butanes (BCBs) a…
View article: Synthesis and Functionalization of Sulfoximine-Bicyclo[1.1.0]butanes: Functionalizable, Tuneable and Cysteine-Selective Chiral Warheads
Synthesis and Functionalization of Sulfoximine-Bicyclo[1.1.0]butanes: Functionalizable, Tuneable and Cysteine-Selective Chiral Warheads Open
Electrophilic covalent warheads with appropriate reactivity and selectivity are crucial to the investigation of protein function and the discovery of therapeutics. Here we report the synthesis of sulfoximine bicyclo[1.1.0]butanes (BCBs) as…
View article: Supplementary Figures 1-6, Table 1 from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth
Supplementary Figures 1-6, Table 1 from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth Open
Supplementary Figures 1-6, Table 1 from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth
View article: Supplementary Figures 1-6, Table 1 from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth
Supplementary Figures 1-6, Table 1 from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth Open
Supplementary Figures 1-6, Table 1 from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth
View article: Data from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth
Data from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth Open
Progression of prostate cancer is highly dependent upon the androgen receptor pathway, such that knowledge of androgen-regulated proteins is vital to understand and combat this disease. Using a proteomic screen, we found the RNA-binding pr…
View article: Data from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth
Data from FUS/TLS Is a Novel Mediator of Androgen-Dependent Cell-Cycle Progression and Prostate Cancer Growth Open
Progression of prostate cancer is highly dependent upon the androgen receptor pathway, such that knowledge of androgen-regulated proteins is vital to understand and combat this disease. Using a proteomic screen, we found the RNA-binding pr…
View article: Identification of the first structurally validated covalent ligands of the small GTPase RAB27A
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A Open
A novel Rab27A construct enables elucidation of covalent ligand binding, paving the way for structure-guided approaches against this challenging target.
View article: Co-ordinated control of the Aurora B abscission checkpoint by PKCε complex assembly, midbody recruitment and retention
Co-ordinated control of the Aurora B abscission checkpoint by PKCε complex assembly, midbody recruitment and retention Open
A requirement for PKCε in exiting from the Aurora B dependent abscission checkpoint is associated with events at the midbody, however, the recruitment, retention and action of PKCε in this compartment are poorly understood. Here, the prere…
View article: Visualising G-quadruplex DNA dynamics in live cells by fluorescence lifetime imaging microscopy
Visualising G-quadruplex DNA dynamics in live cells by fluorescence lifetime imaging microscopy Open
Guanine rich regions of oligonucleotides fold into quadruple-stranded structures called G-quadruplexes (G4). Increasing evidence suggests that these G4 structures form in vivo and play a crucial role in cellular processes. However, their d…
View article: Quantitative Irreversible Tethering (qIT) for Target-directed Covalent Fragment Screening
Quantitative Irreversible Tethering (qIT) for Target-directed Covalent Fragment Screening Open
Small molecules that react to form covalent bonds with proteins are widely used as biological tools and therapeutic agents. Screening cysteine-reactive fragments against a protein target is an efficient way to identify chemical starting po…
View article: <i>N</i>-Myristoyltransferase Inhibition Induces ER-Stress, Cell Cycle Arrest, and Apoptosis in Cancer Cells
<i>N</i>-Myristoyltransferase Inhibition Induces ER-Stress, Cell Cycle Arrest, and Apoptosis in Cancer Cells Open
N-Myristoyltransferase (NMT) covalently attaches a C14 fatty acid to the N-terminal glycine of proteins and has been proposed as a therapeutic target in cancer. We have recently shown that selective NMT inhibition leads to dose-responsive …
View article: Cyclin D type does not influence cell cycle response to <scp>DNA</scp> damage caused by ionizing radiation in multiple myeloma tumours
Cyclin D type does not influence cell cycle response to <span>DNA</span> damage caused by ionizing radiation in multiple myeloma tumours Open
Summary Multiple myeloma ( MM ) is characterized by over‐expression of cyclin D1 ( CCND 1) or D2 ( CCND 2), which control G1 phase cell‐cycle progression. Proteolytic degradation of CCND 1 (but not CCND 2), resulting in G1 arrest, is repor…