Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 7 of 7 for “"ATP-competitive inhibitor"”.
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Small-Molecule Activation of Yap for Inner-Ear Regeneration – and Beyond
… identified a potent, non-toxic, and reversible inhibitor of Hippo signaling. An ATP-competitive inhibitor of Lats kinases, the compound causes Yap-dependent proliferation of murine supporting cells in the inner ear, murine cardiomyocytes, and human Müller glia in retinal organoids. The compound …
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Approaches to Study Small Molecule Inhibitors and Their Targets
… In this method, called Stable Isotope Labeled Inhibitors for Crosslinking (SILIC), structure-activity relationship data is used to design inhibitor analogs that incorporate a photo-crosslinking group along with either natural or heavy stable isotopes. An equimolar mixture of these inhibitor …
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Development of Non-Atp Competitive, Plk1-Selective Inhibitors
… tumor suppressors, it is imperative that a PLK1 inhibitor be exclusive for PLK1. By targeting the non-catalytic polo box domain (PBD) of PLK1, which modulates sub-cellular localization and mitotic functions of PLK1, we can obtain selective PLK1 inhibition, which can lead to mitotic arrest and …
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Studies toward the synthesis of celastrol and the late-stage hydroxylation of arenes mediated by 4,5-dichlorophthaloyl peroxide
… Relevant to cancer, celastrol functions as a non-ATP-competitive inhibitor of heat shock protein-90, providing a potential lead for the development of new inhibitors with improved pharmacology. A laboratory preparation of the small molecule was undertaken to provide access to the unnatural …
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Identification and Characterization of a Selective Inhibitor of the PIM-1 Kinase
… to identify and characterize a selective inhibitor of the PIM- 1 kinase. Such an inhibitor would have utility as a laboratory tool for the study of PIM-1 kinase function and as a template for the design of molecular therapeutics for diseases in which PIM-1 kinase activity is …
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Biochemical Context Drives Inhibitor Selectivity in Aurora A Kinase
… of human cancers that have driven a wealth of inhibitor development targeting Aurora activity, but no compounds have been FDA approved. Recently, Aurora A was shown to provide a non-catalytic stabilizing scaffold for N-Myc, the protein product of the MYCN gene, which is heavily amplified in …
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Interrogating novel functions of the I kappa B kinases via CRISPR-Cas9 gene editing and small molecule inhibition
… is a commercially available allosteric inhibitor of IKKβ that has been used extensively in numerous studies, including a report that proposed novel functions for IKKβ in mitotic cell cycle progression (Blazkova et al., 2007). Similar antiproliferative effects to those reported by …