Collagen comprises ¼ of the protein in humans and ¾ of the dry weight of human skin. Here, we implement recent discoveries about the structure and stability of the collagen triple helix to design new chemical modalities that anchor to natural collagen. The key components are collagen mimetic peptides (CMPs) that are incapable of self-assembly into homotrimeric triple helices, but are able to an...

The methoxy- and fluoro-derivatives of meta-nitrophenylacetic acid (mNPA) chromophores undergo photodecarboxylation with comparable quantum yields (Φ) to unsubstituted mNPA, but uncage at red-shifted excitation wavelengths. This observation prompted us investigate DPAdeCageOMe (2-[bis(pyridin-2-ylmethyl)amino]-2-(4-methoxy-3-nitrophenyl)acetic acid) DPAdeCageF (2-[bis(pyridin-2-ylmethyl)amino]-...

Treatment of laboratory mice and rats with the adrenal steroid, dehydroepiandrosterone (DHEA), produces antiobesity and broad spectrum tumor chemopreventive activity. Certain side effects are associated with DHEA administration which could limit its usefulness as a drug. DHEA can be metabolized into both testosterone and estrone and also increases liver weight and liver catalase activity. We ha...

OBJECTIVES The aim of this feasibility study was to evaluate [(18)F]-2-Fluoro-A85380 for in vivo imaging of arterial nicotinic acetylcholine receptors (nAChRs) in humans. Furthermore, potentially different vascular uptake patterns of this new tracer were evaluated in healthy volunteers and in patients with neurodegenerative disorders. BACKGROUND [(18)F]-2-Fluoro-A85380 was developed for in vi...

The substitution of 2'-fluoro for 2'-hydroxyl moieties in RNA substantially improves the stability of RNA. RNA stability is a major issue in RNA research and applications involving RNA. We report that the RNA polymerase from the marine cyanophage Syn5 has an intrinsic low discrimination against the incorporation of 2'-fluoro dNMPs during transcription elongation. The presence of both magnesium ...

The crystal structures of two ansa-titanocene tri-fluoro-methane-sulfonate complexes bearing the Me2Si(C5Me4)2 ligand are reported, namely [di-methylbis-(η5-tetra-methyl-cyclo-penta-dien-yl)silane](tri-fluoro-methane-sulfonato-κ2O,O')titanium(III) toluene monosolvate, [Ti(CF3O3S)(C20H30Si)]·C7H8, 1, and chlorido-[di-methyl-bis-(η5-tetra-methyl-cyclo-penta-dien-yl)silane](tri-fluoro-methane-sulf...

The title compound, C11H11FO2, is a building block in the synthesis of the active pharmaceutical ingredient dl-nebivolol. The synthesis starting from the enanti-omerically pure (R)-6-fluoro-4-oxo-3,4-di-hydro-2H-chromene-2-carb-oxy-lic acid resulted in a mixture of two stereoisomers, namely (R)-6-fluoro-2-[(S)-oxiran-2-yl]chroman and (R)-6-fluoro-2-[(R)-oxiran-2-yl]chroman. The mixture was sepa...

The microwave spectrum of the mono-fluoro-benzoic acids, 2-fluoro-, 3-fluoro-, and 4-fluoro-benzoic acid have been measured in the frequency range of 4-14 GHz using a pulsed beam Fourier transform microwave spectrometer. Measured rotational transition lines were assigned and fit using a rigid rotor Hamiltonian. Assignments were made for 3 conformers of 2-fluorobenzoic acid, 2 conformers of 3-fl...

Prior to their use in patients with hepatic metastasis of colon cancer, we studied the cell-killing effects of 5-fluorouracil, 5-fluoro-2'-deoxyuridine, 3',5'-dichloromethotrexate (DCM), and 5-fluoro-2'-deoxyuridine, 3',5'-dichloromethotrexate (DCM), and combinations of these fluoropyrimidines with DCM on a human colon carcinoma cell line (HCT-8). Sequential exposure of these cells to DCM follo...