The properties of anhydrous hydrogen fluoride (HF) as a reagent for the acidolysis of various protective groups have been studied. Amino acids with various protective groups were each treated with HF at 0 or 20°C in the presence of anisole, and the reaction products were tested. Thus, HF was found to be much better than the other known reagents, such as hydrogen bromide and trifluoroacetic acid. In the present study, the following groups were shown, for the first time, to be removed safely: the nitro group in nitroarginine, the diphenylmethyl group in diphenylmethylamide, the t-butyl group in S-t-butylcysteine, the isopropyloxycarbonyl group, and the isopropyl ester group. A new and convenient apparatus was designed for the safe handling of HF for peptide synthesis.

Patients with estrogen receptor (ER)-positive breast cancers have a better prognosis than those with ER-negative breast cancers, but often have low sensitivity to chemotherapy and a limited survival benefit. We have previously shown a combination effect of taxanes and fulvestrant and suggested that this treatment may be useful for ER-positive breast cancer. In this study, we evaluated the effects of combinations of hormone drugs and chemotherapeutic agents. In vitro, the effects of combinations of five chemotherapeutic agents (doxorubicin, paclitaxel, docetaxel, vinorelbine, and 5-fluorouracil) and three hormone drugs (fulvestrant, tamoxifen, and 4-hydroxytamoxifen) were examined in ER-positive breast cancer cell lines using CalcuSyn software. Changes in chemoresistant factors such as Bcl2, multidrug resistance-associated protein 1, and microtubule-associated protein tau were also examined after exposure of the cells to hormone drugs. In vivo, tumor sizes in mice were evaluated after treatment with docetaxel or doxorubicin alone, fulvestrant alone, and combinations of these agents. Combination treatment with fulvestrant and all five chemotherapeutic agents in vitro showed synergistic effects. In contrast, tamoxifen showed an antagonistic effect with all the chemotherapeutic agents. 4-Hydroxytamoxifen showed an antagonistic effect with doxorubicin and 5-fluorouracil, but a synergistic effect with taxanes and vinorelbine. Regarding chemoresistant factors, Bcl2 and microtubule-associated protein tau were downregulated by fulvestrant. In vivo, a combination of fulvestrant and docetaxel had a synergistic effect on tumor growth, but fulvestrant and doxorubicin did not show this effect. In conclusion, fulvestrant showed good compatibility with all the evaluated chemotherapeutic agents, and especially with docetaxel, in vitro and in vivo. (Cancer Sci 2011; 102: 2038-2042 T he malignant grade of estrogen receptor (ER)-positive breast cancer is generally low, thus patients with this cancer have a better prognosis than those with ER-negative breast cancer. However, ER-positive breast cancers have low sensitivity to chemotherapy and the survival benefit of chemotherapy is limited.(1-3) Estrogen receptors play a crucial role in the development and progression of breast cancers and modulate many genes including of chemoresistant factors. The low sensitivity to chemotherapy may be caused by ER itself or by ER modulation of the levels of factors that cause resistance to chemotherapy. (4)(5)(6)(7)(8)(9)(10)(11) Tamoxifen has significant efficacy for ER-positive breast cancer. However, the mechanism is not completely understood. Tamoxifen is metabolized and the metabolites (4-hydroxytamoxifen and 4-hydroxy-N-desmethyltamoxifen) have different affinities for ER and exert a variety of agonist and antagonist properties.(1,12-14) Fulvestrant, a selective ER inhibitor, is an active hormone drug for advanced breast cancer, and a randomized phase II comparative study of a fulvestrant high-dose regimen for advanced hormone receptor-pos...

We propose an experimental scheme to generate, in a heralded fashion, arbitrary quantum superpositions of two-mode optical states with a fixed total photon number n based on weakly squeezed two-mode squeezed state resources (obtained via weak parametric down conversion), linear optics, and photon detection. Arbitrary d-level (qudit) states can be created this way where d = n + 1. Furthermore, we experimentally demonstrate our scheme for n = 2. The resulting qutrit states are characterized via optical homodyne tomography. We also discuss possible extensions to more than two modes concluding that, in general, our approach ceases to work in this case. For illustration and with regards to possible applications, we explicitly calculate a few examples such as NOON states and logical qubit states for quantum error correction. In particular, our approach enables one to construct bosonic qubit error-correction codes against amplitude damping (photon loss) with a typical suppression of √ n − 1 losses and spanned by two logical codewords that each correspond to an n-photon superposition for two bosonic modes.

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