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Targeting fibroblast growth factor receptors blocks PI3K/AKT signaling, induces apoptosis, and impairs mammary tumor outgrowth and metastasis.
Members of the fibroblast growth factor receptor (FGFR) family have essential roles in normal physiology and in cancer where they control diverse processes. FGFRs have been associated with breastExpand
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Exosomes surf on filopodia to enter cells at endocytic hot spots, traffic within endosomes, and are targeted to the ER
Heusermann et al. use a single-vesicle dye-tracing analysis in live cells showing that exosomes enter cells as intact vesicles, primarily at filopodia-active regions, and sort into endocytic vesicleExpand
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Protein Complex Interactor Analysis and Differential Activity of KDM3 Subfamily Members Towards H3K9 Methylation
Histone modifications play an important role in chromatin organization and gene regulation, and their interpretation is referred to as epigenetic control. The methylation levels of several lysineExpand
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Class I and IIa Histone Deacetylases Have Opposite Effects on Sclerostin Gene Regulation
Background: Gene regulation of the bone repressor sclerostin (SOST) is only poorly understood. Results: SOST gene suppression by parathyroid hormone is partially mediated by HDAC5 inhibiting MEF2,Expand
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Two Antagonistic MALT1 Auto-Cleavage Mechanisms Reveal a Role for TRAF6 to Unleash MALT1 Activation
The paracaspase MALT1 has arginine-directed proteolytic activity triggered by engagement of immune receptors. Recruitment of MALT1 into activation complexes is required for MALT1 proteolyticExpand
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Chemical genetic approach identifies microtubule affinity‐regulating kinase 1 as a leucine‐rich repeat kinase 2 substrate
Mutations in leucine‐rich repeat kinase 2 (LRRK2) are the most common cause of autosomal‐dominant forms of Parkinson's disease. LRRK2 is a modular, multidomain protein containing 2 enzymatic domains,Expand
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Characterization of kinase inhibitors using reverse phase protein arrays.
Using the reverse protein array platform in combination with planar waveguide technology, which allows detection of proteins in spotted cell lysates with high sensitivity in a 96-wellExpand
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Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.
A diverse range of selective FGFR4 inhibitor hit series were identified using unbiased screening approaches and by the modification of known kinase inhibitor scaffolds. In each case the origin of theExpand
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Systematic characterization of extracellular vesicle sorting domains and quantification at the single molecule – single vesicle level by fluorescence correlation spectroscopy and single particle
ABSTRACT Extracellular vesicles (EV) convey biological information by transmitting macromolecules between cells and tissues and are of great promise as pharmaceutical nanocarriers, and as therapeuticExpand
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Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
FGF19 signaling through the FGFR4/β-klotho receptor complex has been shown to be a key driver of growth and survival in a subset of hepatocellular carcinomas making selective FGFR4 inhibition anExpand