... interactions phosphorylation small-molecule inhibitor ULK kinase In addition to modulating the timing of membrane abscission, ULK3 was suggested to play a role in several signalling pathways. Though it is not required for autophagy induced by low nutrient levels, studies on the Drosophila ULK3...

... presenting an inhibition constant in the micromolar concentration range. Three of them inhibited tumour cell proliferation. The association of virtual screening and experimental assay thus proved successful for the discovery of the first small-molecule inhibitors of Pontin. 1 Correspondence may...

... peptidylprolyl isomerase small-molecule inhibitor X-ray crystallography Melioidosis is a community-acquired infection frequent in South-East Asia and Northern Australia [ 1 ]. Caused by the Gram-negative bacterium Burkholderia pseudomallei , the disease can range from a localized infection to an acute...

... To whom correspondence should be addressed (email [email protected] ). cystic fibrosis transmembrane conductance regulator (CFTR) type 2 lysophosphatidic acid receptor (LPA 2 ) Na + /H + exchanger regulatory factor-2 (NHEFR2) PDZ domain protein–protein interaction small-molecule inhibitor...

... interaction small-molecule inhibitor type 2 lysophosphatidic acid receptor (LPA 2 ) On the basis of the number and diversity of PDZ-domain-mediated interactions, we predict that the development of small-molecule compounds which specifically target a particular interaction will continue...

...-tagged PfPRMT1 and untagged PfPRMT1 were localized in both cellular compartments, with the majority in the cytoplasm. in vitro assays showed that PfPRMT1 could be inhibited by several small-molecule inhibitors, with IC 50 -values in the sub-micromolar range. Most of these compounds also effectively...

... phosphoinositide 3-kinase (PI3K) site-directed mutagenesis small-molecule inhibitor Enzymes of the PI3K (phosphoinositide 3-kinase) family are fundamental to numerous intracellular signalling cascades, catalysing phosphorylation at the 3-hydroxy function of phosphatidylinositols [ 1 , 2 ]. The 3...

...Christopher G. Proud Small-molecule inhibitors are now widely used to try to dissect regulatory signalling events. Many of these interfere with the function of protein kinases, often as part of signalling cascades. In addition to their utility as tools for the researcher, the long-term aspiration...