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Sequential Regulation of DOCK2 Dynamics by Two Phospholipids During Neutrophil Chemotaxis
During chemotaxis, activation of the small guanosine triphosphatase Rac is spatially regulated to organize the extension of membrane protrusions in the direction of migration. In neutrophils, Rac
Limited Brain Distribution of [3R,4R,5S]-4-Acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate Phosphate (Ro 64-0802), a Pharmacologically Active Form of Oseltamivir, by Active Efflux
It is suggested that Ro 64-0802 can cross the BBB from the blood, but its brain distribution is limited by its active efflux by Mrp4 and Oat3 across theBBB.
P-glycoprotein Restricts the Penetration of Oseltamivir Across the Blood-Brain Barrier
The results suggest that P-gp limits the brain uptake of oseltamivir at the blood-brain barrier (BBB) and that Ro 64-0802 itself barely crosses the BBB.
Blockade of inflammatory responses by a small-molecule inhibitor of the Rac activator DOCK2.
The identified 4-[3'-(2″-chlorophenyl)-2'-propen-1'-ylidene]-1-phenyl-3,5-pyrazolidinedione (CPYPP) as a small-molecule inhibitor of DOCK2 provides a rational of and a chemical scaffold for development of the Dock2-targeting immunosuppressant.
Control of multivalent interactions by binding epitope density.
This work studies the influence of multivalent ligand binding epitope density on the clustering of a model receptor, concanavalin A, and analyzes three aspects of receptor clustering: the stoichiometry of the complex, rate of cluster formation, and receptor proximity.
Probing Low Affinity and Multivalent Interactions with Surface Plasmon Resonance: Ligands for Concanavalin A
The affinities of the carbohydrate-binding protein concanavalin A (Con A) for mono- and multivalent ligands were measured by surface plasmon resonance (SPR) detection. Assessing protein−carbohydrate
Embryo Spacing and Implantation Timing Are Differentially Regulated by LPA3-Mediated Lysophosphatidic Acid Signaling in Mice1
The results suggest that LPA3 signaling controls embryo spacing via uterine contraction around E3.5, which is critical for embryo spacing.
Varying the Size of Multivalent Ligands: The Dependence of Concanavalin A Binding on Neoglycopolymer Length
Motomu Kanai, Kathleen H. Mortell, andLaura L. Kiessling*Department of ChemistryUniVersity of WisconsinsMadisonMadison, Wisconsin 53706ReceiVed June 24, 1997Carbohydrate-substituted polymers have
Second generation catalytic asymmetric synthesis of Tamiflu: allylic substitution route.
This second generation route of Tamiflu is more practical than the previously reported route and introduces an allylic oxygen function and C1 unit on the C=C double bond through cyanophosphorylation of enone and allylic substitution with an oxygen nucleophile.
Copper(I)-Catalyzed Enantioselective Addition of Enynes to Ketones.
A copper(I)-catalyzed enantioselective addition of enynes to ketones was developed. The method allows facile construction of enantiomerically enriched tertiary alcohols using skipped enynes as stable