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Concanamycin A, the Specific Inhibitor of V-ATPases, Binds to the Vo Subunit c*
Binding of J-concanolide A to subunit c was prevented in a concentration-dependent manner by concanamycin A, indicating that labeling was specific, and binding was also prevented by the plecomacrolides bafilomycin A1 and B1, respectively. Expand
The novel isoxazoline ectoparasiticide fluralaner: selective inhibition of arthropod γ-aminobutyric acid- and L-glutamate-gated chloride channels and insecticidal/acaricidal activity.
In agreement with the superior RDL on-target activity, fluralaner outperformed dieldrin and fipronil in insecticidal screens on cat fleas (Ctenocephalides felis), yellow fever mosquito larvae (Aedes aegypti) and sheep blowfly larvae (Lucilia cuprina), as well as in acar suicidal screens on cattle tick (R. microplus) adult females and Ornithodoros moubata nymphs. Expand
Mutants of protein kinase A that mimic the ATP-binding site of protein kinase B (AKT).
The phenomenon of Q181 shows how crystallographic analysis should accompany mutant studies to monitor possible spurious structural effects, and the triple mutant serves well as an easily crystallizable model for PKB inhibitor interactions. Expand
Expression of the recE gene during induction of the SOS response in Bacillus subtilis recombination‐deficient strains
A transcriptional fusion of the recE gene to a reporter gene has been constructed and de‐repression of recE seems to be independent of the ATP‐dependent DNase activity of the exonuclease V enzyme. Expand
The KdpF Subunit Is Part of the K+-translocating Kdp Complex of Escherichia coli and Is Responsible for Stabilization of the Complex in Vitro *
Upon expression of this operon in minicells, a so far unrecognized small hydrophobic polypeptide, KdpF, could be identified on high resolution SDS-polyacrylamide gels and proved to be indispensable for a functional enzyme complex in vitro. Expand
Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants.
The PKA to PKB exchanges F187L and Q84E enable the design of the selective inhibitors described herein which mimic ATP but extend further into a site not occupied by ATP, in which selectivity over PKA can be achieved by the introduction of bulkier substituents. Expand
Structural Analysis of Protein Kinase A Mutants with Rho-kinase Inhibitor Specificity*
Kinetic results corroborate the hypothesis that side-chain identities form the major determinants of selectivity in Rho-kinase and suggest that PKA mutants are valuable for use as surrogate kinases for structure-based inhibitor design. Expand
Head morphogenesis genes of the Bacillus subtilis bacteriophage SPP1.
The organization of the DNA packaging and head genes of SPP1 resembles the organization of genes in the analogous regions of phage lambda and P22. Expand
Semisynthetic derivatives of concanamycin A and C, as inhibitors of V- and P-type ATPases: structure-activity investigations and developments of photoaffinity probes.
V-type ATPases are inhibited by the plecomacrolides bafilomycin and concanamycin, which exert their inhibitory potential at nanomolar concentrations. In addition, some P-type ATPases are inhibited atExpand
The typically disordered N-terminus of PKA can fold as a helix and project the myristoylation site into solution.
An unusual structure of an unmyristoylated PKA, unphosphorylated at serine 10, with a completely ordered N-terminus is described, apparently the absence of phosphorylation of Ser10. Expand