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Amino Acids - A direct inhibiting effect of NO on the function of CAT-1 and -2A has been postulated to occur via nitrosylation of cysteine residues in the transporters. Neither the NO donor SNAP... 相似文献
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Jadidi Majid Desyatova Anastasia MacTaggart Jason Kamenskiy Alexey 《Biomechanics and modeling in mechanobiology》2019,18(6):1591-1605
Biomechanics and Modeling in Mechanobiology - Planar biaxial testing is commonly used to characterize the mechanical properties of arteries, but stresses associated with specimen flattening during... 相似文献
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Giulia Schiroli Anastasia Conti Samuele Ferrari Lucrezia della Volpe Aurelien Jacob Luisa Albano Stefano Beretta Andrea Calabria Valentina Vavassori Patrizia Gasparini Eralda Salataj Delphine Ndiaye-Lobry Chiara Brombin Julie Chaumeil Eugenio Montini Ivan Merelli Pietro Genovese Luigi Naldini Raffaella Di Micco 《Cell Stem Cell》2019,24(4):551-565.e8
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Alexey E. Machulkin Dmitry A. Skvortsov Yan A. Ivanenkov Anton P. Ber Mikhail V. Kavalchuk Anastasia V. Aladinskaya Anastasia A. Uspenskaya Radik R. Shafikov Ekaterina A. Plotnikova Raisa I. Yakubovskaya Ekaterina A. Nimenko Nikolay U. Zyk Elena K. Beloglazkina Nikolay V. Zyk Victor E Koteliansky Alexander G. Majouga 《Bioorganic & medicinal chemistry letters》2019,29(16):2229-2235
Prostate cancer (PC) is the second most commonly occurring cancer in men. Conventional chemotherapy has wide variety of disadvantages such as high systemic toxicity and low selectivity. Targeted drug delivery is a promising approach to decrease side effects of therapy. Prostate specific membrane antigen (PSMA) is overexpressed in prostate cancer cells while low level of expression is observed in normal cells. In this study we describe the development of Glu-urea-Lys based PSMA-targeting conjugates with paclitaxel. A series of new PSMA targeting conjugates with paclitaxel was designed and synthesized. The cytotoxicity of conjugates was evaluated against prostate (LNCaP, 22Rv1 and PC-3) and non-prostate (Hek293T, VA13, A549 and MCF-7) cell lines. The most promising conjugate 21 was examined in vivo using 22Rv1 xenograft mice model. It demonstrated good efficiency comparable with paclitaxel, while reduced toxicity. 3D molecular docking study was also performed to understand underlying mechanism of binding and further optimization of the linker substructure and conjugates structure for improving the target affinity. These conjugates may be useful for further design of novel PSMA targeting delivery systems for PC. 相似文献