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1.
Bioorg Med Chem ; 20(14): 4371-6, 2012 Jul 15.
Article in English | MEDLINE | ID: mdl-22705189

ABSTRACT

Arylstibonates structurally resemble phosphotyrosine side chains in proteins and here we addressed the ability of such compounds to act as inhibitors of a panel of mammalian tyrosine and dual-specificity phosphatases. Two arylstibonates both possessing a carboxylate side chain were identified as potent inhibitors of the protein tyrosine phosphatase PTP-ß. In addition, they inhibited the dual-specificity, cell cycle regulatory phosphatases Cdc25a and Cdc25b with sub-micromolar potency. However, the Cdc25c phosphatase was not affected demonstrating that arylstibonates may be viable leads from which to develop isoform specific Cdc25 inhibitors.


Subject(s)
Antimony/chemistry , Enzyme Inhibitors/chemistry , Organometallic Compounds/chemistry , Propionates/chemistry , cdc25 Phosphatases/antagonists & inhibitors , Kinetics , Structure-Activity Relationship , cdc25 Phosphatases/metabolism
2.
Langmuir ; 23(8): 4589-98, 2007 Apr 10.
Article in English | MEDLINE | ID: mdl-17371057

ABSTRACT

Mesostructured films of alkyltrimethylammonium bromides or cetylpyridinium bromide and polyethylenimines that spontaneously self-assemble at the air/water interface have been examined using a range of surface sensitive techniques. These films are unusual in that they can be micrometers thick and are relatively robust. Here we show that the films can be cross-linked and thus removed from the liquid surface where they form, as solid, mesostructured polymer-surfactant membranes. Cross-linking causes little change in the structure of the films but freezes in the metastable mesostructures, enhancing the potential of these films for future applications. Cross-linked films, dried after removal from the solution surface, retain the ordered nanoscale structure within the film. We also report grazing incidence X-ray diffraction (GID), which shows that most films display scattering consistent with 2D-hexagonal phase crystallites of rodlike surfactant micelles encased in polymer. Polymer branching makes little difference to the film structures; however, polymer molecular weight has a significant effect. Films with lower polymer MW are generally thinner and more ordered, while higher polymer MW films were thicker and less ordered. Increased pH causes formation of thicker films and improves the ordering in low MW films, while high MW films lose order. To rationalize these results, we propose a model for the film formation process that relates the kinetic and thermodynamic limits of phase separation and mesophase ordering to the structures observed.


Subject(s)
Polymers/chemistry , Surface-Active Agents/chemistry , Cations , Chemistry, Physical/methods , Cross-Linking Reagents/chemistry , Cross-Linking Reagents/pharmacology , Hydrogen-Ion Concentration , Kinetics , Micelles , Models, Chemical , Molecular Structure , Neutrons , Polyethyleneimine/chemistry , Sodium Hydroxide/chemistry , Surface Properties , Thermodynamics
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