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Cyclam-Modified PEI for Combined VEGF siRNA Silencing and CXCR4 Inhibition To Treat Metastatic Breast Cancer

19.01.2018 | Yiwen Zhou; Fei Yu; Feiran Zhang; Gang Chen; Kaikai Wang; Minjie Sun; Jing Li; David Oupický, Biomacromolecules, 2018

Chemokine receptor CXCR4 plays an important role in cancer cell invasion and metastasis. Recent findings suggest that anti-VEGF therapies upregulate CXCR4 expression, which contributes to resistance to antiangiogenic therapies. Here, we report the development of novel derivatives of ...


Crystal Structures and Human Leukemia Cell Apoptosis Inducible Activities of Parthenolide Analogues Isolated from Piptocoma rufescens

19.01.2018 | Yulin Ren; Judith C. Gallucci; Xinxin Li; Lichao Chen; Jianhua Yu; A. Douglas Kinghorn, Journal of Natural Products, 2018

The molecular structures of three parthenolide analogues, (−)-goyazensolide (1), (−)-15-deoxygoyazensolide (2), and (−)-ereglomerulide (3), isolated from the leaves of Piptocoma rufescens in a previous study were determined by X-ray analysis, and the absolute configuration of (−)-goyazensolide ...


Mutual Impact of Phase Separation/Crystallization and Water Sorption in Amorphous Solid Dispersions

19.01.2018 | Christian Luebbert; Maximilian Wessner; Gabriele Sadowski, Molecular Pharmaceutics, 2018

The molecular integration of poorly water soluble active pharmaceutical ingredients (APIs) in a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and solubility of these APIs. Like all newly developed pharmaceutical formulations, these formulations (often ...


Design, Synthesis, and Biological Evaluation of 68Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

19.01.2018 | Fei Liu; Teli Liu; Xiaoxia Xu; Xiaoyi Guo; Nan Li; Chiyi Xiong; Chun Li; Hua Zhu; Zhi Yang, Molecular Pharmaceutics, 2018

Most of the radiolabeled somatostatin analogues (SSAs) are specific for subtype somatostatin receptor 2 (SSTR2). Lack of ligands targeting other subtypes of SSTRs, especially SSTR1, SSTR3, and SSTR5, limited their applications in tumors of low SSTR2 expression, including lung tumor. In this ...


Establishment of LCMS Based Platform for Discovery of Quorum Sensing Inhibitors: Signal Detection in Pseudomonas aeruginosa PAO1

18.01.2018 | Manoj Kushwaha; Shreyans K. Jain; Nisha Sharma; Vidushi Abrol; Sundeep Jaglan; Ram A. Vishwakarma, ACS Chemical Biology, 2018

Targeting the main three networking systems, viz. Las, RhI, and PQS, via natural quenchers is a new ray of hope for combating the persistent behavior of Pseudomonas aeruginosa. In the bacterial chemical vocabulary pyocyanin, N-AHLs and rhamnolipids are the main keywords, which are responsible for ...


Influence of Constraints within a Cyclic Polymer on Solution Properties

18.01.2018 | Md. D. Hossain; James C. Reid; Derong Lu; Zhongfan Jia; Debra J. Searles; Michael J. Monteiro, Biomacromolecules, 2018

Cyclic polymers with internal constraints provide new insight into polymer properties in solution and bulk and can serve as a model system to explain the stability and mobility of cyclic biomacromolecules. The model system used in this work consisted of cyclic polystyrene structures, all with a ...


Proteome of Bovine Mitochondria and Rod Outer Segment Disks: Commonalities and Differences

18.01.2018 | Maurizio Bruschi; Andrea Petretto; Federico Caicci; Martina Bartolucci; Daniela Calzia; Laura Santucci; Lucia Manni; ..., Journal of Proteome Research, 2018

The retinal rod outer segment (OS) is a stack of disks surrounded by the plasma membrane, housing proteins related to phototransduction, as well as mitochondrial proteins involved in oxidative phosphorylation (OxPhos). This prompted us to compare the proteome of bovine OS disks and mitochondria ...


Incorporation of mRNA in Lamellar Lipid Matrices for Parenteral Administration

18.01.2018 | Antje Ziller; Sara S. Nogueira; Eva Hühn; Sergio S. Funari; Gerald Brezesinski; Hermann Hartmann; Ugur Sahin; Heinri ..., Molecular Pharmaceutics, 2018

Insertion of high molecular weight messenger RNA (mRNA) into lyotropic lipid phases as model systems for controlled release formulations for the mRNA was investigated. Low fractions of 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) were used as an anchor to load the mRNA into a lamellar lipid ...


Cold and Hot Gelling of Alginate-graft-PNIPAM: a Schizophrenic Behavior Induced by Potassium Salts

18.01.2018 | Hui Guo; Mickaël de Magalhaes Goncalves; Guylaine Ducouret; Dominique Hourdet, Biomacromolecules, 2018

Recently, alginates (ALG) characterized by high mannuronic content (M blocks) have been shown to undergo a reversible sol/gel transition during cooling in the presence of potassium salts. Cold gelling takes place at low temperatures, just below 0 °C for a KCl concentration of 0.3 mol/kg, but the ...


Engineered Cellular Uptake and Controlled Drug Delivery Using Two Dimensional Nanoparticle and Polymer for Cancer Treatment

18.01.2018 | Sudipta Senapati; Rashmi Shukla; Yamini Bhusan Tripathi; Arun Kumar Mahanta; Dipak Rana; Pralay Maiti, Molecular Pharmaceutics, 2018

Two major problems in chemotherapy, poor bioavailability of hydrophobic anticancer drug and its adverse side effects causing nausea, are taken into account by developing a sustained drug release vehicle along with enhanced bioavailability using two-dimensional layered double hydroxides (LDHs) ...


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