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Competitive cAMP antagonists for cAMP-receptor proteins.
The two exocyclic oxygen atoms at phosphorus of cAMP have been replaced by a sulfur atom or by a dimethylamino group. These substitutions introduce chirality at the phosphorus atom; therefore, twoExpand
Drosophila SOCS Proteins
The current understanding of Drosophila SOCS proteins, their roles in vivo, and future approaches to elucidating their functions are reviewed. Expand
Inhibitory action of certain cyclophosphate derivatives of cAMP on cAMP-dependent protein kinases.
The present work using highly purified compounds suggests the absence of a charge interaction, since the uncharged analog (Sp)-cAMPN(CH3)2 activates the kinase effectively. Expand
Cryo-EM structure of the human α1β3γ2 GABAA receptor in a lipid bilayer
A high-resolution cryo-electron microscopy structure of the full-length human α1β3γ2L GABAA receptor, functionally reconstituted in lipid nanodiscs is reported and illustrates the molecular principles of heteromeric GAB AA receptor organization and provides a reference framework for future mechanistic investigations of GABAergic signalling and pharmacology. Expand
Mechanisms of coupling between DNA recognition specificity and catalysis in EcoRI endonuclease.
The results show the roles in catalysis of individual phosphoryl oxygens and of DNA distortion and suggest that a "crosstalk ring" in the complex couples recognition to catalysis and couples the two catalytic sites to each other. Expand
Comparative metabolism of 2-[bis(2-chloroethyl)amino]tetrahydro-2-H-1,3,2-oxazaphosphorine-2-oxide (cyclophosphamide) and its enantiomers in humans.
There is little reason to predict that the enantiomers will differ from each other or from the racemate in their therapeutic effects in humans, but there are other factors, e.g., stereoselective uptake of the intermediary 4-hydroxylated metabolites by neoplastic cells, which could elicit such differences. Expand
Novel route to oligo(deoxyribonucleoside phosphorothioates). Stereocontrolled synthesis of P-chiral oligo(deoxyribonucleoside phosphorothioates).
The synthesis and separation of diastereoisomerically pure 5'-O-DMT-nucleoside 3'-O-(2-thio-1,3,2-oxathiaphospholane) allows their use as synthons in DBU-catalyzed reaction with the 5'-hydroxylExpand
Recent advances in the elucidation of the mechanisms of action of ribozymes.
While high concentrations of monovalent metal ions or polyamines can facilitate cleavage by hammerhead ribozymes, divalent metal ions are the most effective acid/base catalysts under physiological conditions. Expand
Drosophila SOCS36E negatively regulates JAK/STAT pathway signaling via two separable mechanisms
The low-complexity Drosophila genome includes previously uncharacterized SOCS36E, an ancestral SOCS4/5 homologue. It is shown that SOCS36E suppresses JAK/STAT signaling through two separateExpand