... conformational changes enzyme–substrate interactions phosphorylation small-molecule inhibitor ULK kinase Membrane abscission is the ultimate step in several physiologically important processes such as exosome budding and cytokinesis [ 1 ]. Any connection between two membrane substructures is cut...

... 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...

... 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...

... 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...

...-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...

[email protected] ). 6 3 2008 2 5 2008 20 5 2008 20 5 2008 © The Authors Journal compilation © 2008 Biochemical Society 2008 ATP-binding pocket phosphoinositide 3-kinase (PI3K) site-directed mutagenesis small-molecule inhibitor Enzymes of the PI3K (phosphoinositide 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...