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Adaptins: the final recount.
A survey for adaptins from sequenced genomes including those of man, mouse, the fruit fly Drosophila melanogaster, the nematode Caenorhabditis elegans, the plant Arabidopsis thaliana, and the yeasts, Saccharomyces cerevisiae and Schizosac charomyces pombe is reported.
Recognition of dileucine-based sorting signals from HIV-1 Nef and LIMP-II by the AP-1 γ–σ1 and AP-3 δ–σ3 hemicomplexes
A yeast three-hybrid assay is used to demonstrate that [DE]XXXL[LI]-type signals from the human immunodeficiency virus negative factor protein and the lysosomal integral membrane protein II interact with combinations of the γ/δ and σ subunits of AP-1 and AP-3.
Genetic analyses of adaptin function from yeast to mammals.
Rabenosyn-5 and EHD1 interact and sequentially regulate protein recycling to the plasma membrane.
The studies suggest that Rabenosyn-5 and EHD1 act sequentially in the transport of proteins from early endosomes to the endosomal recycling compartment and back to the plasma membrane.
Functional and physical interactions of the adaptor protein complex AP‐4 with ADP‐ribosylation factors (ARFs)
It is shown that the recruitment of endogenous AP‐4 to the TGN in vivo is regulated by the small GTP‐binding protein ARF1, and a direct interaction of the ϵ and μ4 subunits of AP‐ 4 with ARf1 is demonstrated.
Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials
The biologic properties of the 2-aminothiazole derivative NVP-BYL719, a selective inhibitor of PI3Kα and its most common oncogenic mutant forms, are reported and it is found that PIK3CA mutation was the foremost positive predictor of sensitivity while revealing additional positive and negative associations such as Pik3CA amplification and PTEN mutation, respectively.
Class I Histone Deacetylase Expression Has Independent Prognostic Impact in Human Colorectal Cancer: Specific Role of Class I Histone Deacetylases In vitro and In vivo
The finding that HDACs are differentially expressed in colorectal tumors suggest that the evaluation of HDAC expression in clinical trials for HDAC inhibitors might help to identify a patient subgroup who will exceptionally profit from such a treatment.
Signal-binding Specificity of the μ4 Subunit of the Adaptor Protein Complex AP-4*
The medium subunit μ4 of the recently described adaptor protein complex AP-4 recognized the tyrosine signal from the human lysosomal protein LAMP-2, HTGYEQF and the apparent dissociation constant for the μ4-YXXØ interaction was determined to be in the micromolar range.
Specific regulation of the adaptor protein complex AP-3 by the Arf GAP AGAP1.
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein…
Optimization of the core and aryl appendage improved oral absorption and culminated in the identification of indole acid, PF-06409577 (7), which was advanced to first-in-human trials for the treatment of diabetic nephropathy.