Clinical Perspectives of Scrotal Ultrasound in Urology

Tang, Shou-Hung; Cha, Tai‐Lung; Sun, Guang‐Huan

doi:10.5772/27633

Cited by 1 publication

(1 citation statement)

References 7 publications

(7 reference statements)

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“…12,[23][24][25] Additionally, the ability of B cells to produce secretory IgM is potently inhibited by B-I09, leading to significantly decreased immunosuppressive functions of myeloid-derived suppressor cells and reactivation of antitumor CD8+ T cell functions in CLL and lung cancer mouse models. 26 Structural tailoring of IRE-1 inhibitors to investigate the influence of substituents on the drug stability and stimuli-specific release has not been explored.…”

Section: Introductionmentioning

confidence: 99%

Structural Tailoring of a Novel Fluorescent IRE-1 RNase Inhibitor to Precisely Control Its Activity

et al. 2019

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Activation of the IRE-1/XBP-1 pathway has been linked to many human diseases. We report a novel fluorescent tricyclic chromenone inhibitor, D-F07, in which we incorporated a 9-methoxy group onto the chromenone core to enhance its potency and masked the aldehyde to achieve longterm efficacy. Protection of the aldehyde as a 1,3-dioxane acetal led to strong fluorescence emitted by the coumarin chromophore, enabling D-F07 to be tracked inside the cell. We installed a photolabile structural cage on the hydroxy group of D-F07 to generate PC-D-F07. Such a modification significantly stabilized the 1,3-dioxane acetal protecting group, allowing for specific stimulusmediated control of inhibitory activity. Upon photo-activation, the re-exposed hydroxy group on D-F07 triggered the aldehyde-protecting 1,3-dioxane acetal to slowly decompose, leading to the inhibition of the RNase activity of IRE-1. Our novel findings will also allow for spatiotemporal control of the inhibitory effect of other salicylaldehyde-based compounds currently in development.

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Section: Introductionmentioning

confidence: 99%