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https://www.readbyqxmd.com/read/29656465/structural-characterization-of-the-interaction-of-the-fibroblast-growth-factor-receptor-with-a-small-molecule-allosteric-inhibitor
#1
Franziska Kappert, Sridhar Sreeramulu, Hendrik R A Jonker, Christian Richter, Vladimir V Rogov, Ewgenij Proschak, Bruno Hargittay, Krishna Saxena, Harald Schwalbe
The interaction of fibroblast growth factors (FGFs) with their fibroblast growth factor receptors (FGFRs) are important in the signaling network of cell growth and development. SSR128129E (SSR)[1,2], a ligand of small molecular weight with potential anti-cancer properties, acts allosterically on the extracellular domains of FGFRs. Up to now, the structural basis of SSR binding to the D3 domain of FGFR remained elusive. Here, we report the structural characterization of the interaction of SSR with one specific receptor, FGFR3 by NMR spectroscopy...
April 14, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29656362/evaluation-of-animal-models-by-comparison-with-human-late-onset-alzheimer-s-disease
#2
Bu-Yeo Kim, Hye-Sun Lim, Yoonju Kim, Yu Jin Kim, Imhoi Koo, Soo-Jin Jeong
Despite many efforts to alleviate the pathological conditions of Alzheimer's disease (AD), effective therapeutic drugs have not been developed, mainly because of the lack of molecular information about AD and animal models. We observed the reciprocal regulation of AD-associated genes (AD genes) and their related functions. Upregulated AD genes were positioned in central regions in the protein-protein interaction network and were involved in inflammation and DNA repair pathways. Downregulated AD genes positioned in the periphery of the network were associated with metabolic pathways...
April 14, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29656216/insights-into-cell-penetrating-peptide-conjugated-gold-nanoparticles-for-internalization-into-bacterial-cells
#3
Munish Kumar, Werner Tegge, Nishima Wangoo, Rahul Jain, Rohit K Sharma
Gold nanoparticles (AuNPs) functionalized with different biomolecules find extensive application in therapy, clinical diagnosis and biomedical imaging. Herein, two derivatives of TAT peptide with sequences YGRKKRRQRRR and YGRKKRRQRRR-(β-ala)3 -Cys-amide were conjugated with tannic acid capped gold nanoparticles which acted as a carrier for cell penetrating peptides (CPPs) into the bacterial cells. The interaction of YGRKKRRQRRR peptide with AuNPs was non-covalent in nature whereas YGRKKRRQRRR-(β-ala)3 -Cys-amide interacted covalently with the AuNPs due to presence of thiol group in cysteine which bind strongly to gold nanoparticles surface...
March 31, 2018: Biophysical Chemistry
https://www.readbyqxmd.com/read/29656201/anti-leishmanial-click-modifiable-thiosemicarbazones-design-synthesis-biological-evaluation-and-in-silico-studies
#4
Mohamed G Temraz, Perihan A Elzahhar, Alaa El-Din A Bekhit, Adnan A Bekhit, Hala F Labib, Ahmed S F Belal
Leishmaniasis is a devastating tropical disease with limited therapeutic options. Depending on recently reported active anti-leishmanial compounds, we designed and synthesized a series of click modifiable 1,2,3-triazole and thiosemicarbazone hybrids. Most of the synthesized compounds showed comparable to superior activity to a well-established anti-leishmanial drug miltefosine. Compounds 2 and 10a showed nanomolar IC50 s against promastigotes of L. major (227.4 nM and 140.3 nM respectively, vs 7.8 μM for miltefosine)...
April 3, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29656089/microbiology-catches-the-cryo-em-bug
#5
REVIEW
Lesley A Earl, Veronica Falconieri, Sriram Subramaniam
Over the past few years, the advances in technology and methods that have revolutionized cryo-EM are allowing for key insights in a variety of areas in biology, and microbiology is no exception. A wide range of important macromolecular assemblies in prokaryotic and eukaryotic cells, as well as intact viruses, have now become accessible to investigation by new methods in 3D electron microscopy. We focus here on selected examples that illustrate this breadth, and review the application of methods in single particle cryo-EM and cryo-electron tomography to progress in the structural biology of CRISPR systems, visualization of small molecule drugs in membrane proteins, in situ visualization of bacterial nanomachines, and the analysis of antigen-antibody interactions to drive vaccine design...
April 12, 2018: Current Opinion in Microbiology
https://www.readbyqxmd.com/read/29655904/3d-printed-controlled-release-tritherapeutic-tablet-matrix-for-advanced-anti-hiv-1-drug-delivery
#6
Margaret Siyawamwaya, Lisa C du Toit, Pradeep Kumar, Yahya E Choonara, Pierre P P D Kondiah, Viness Pillay
PURPOSE: A 3D-Bioplotter® was employed to 3D print (3DP) a humic acid-polyquaternium 10 (HA-PQ10) controlled release fixed dose combination (FDC) tablet comprising of the anti-HIV-1 drugs, efavirenz (EFV), tenofovir disoproxil fumarate (TDF) and emtricitabine (FTC). METHODS: Chemical interactions, surface morphology and mechanical strength of the FDC were ascertained. In vitro drug release studies were conducted in biorelevant media followed by in vivo study in the large white pigs, in comparison with a market formulation, Atripla® ...
April 12, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29655729/in-vitro-effects-of-rebaudioside-a-stevioside-and-steviol-on-porcine-cytochrome-p450-expression-and-activity
#7
Rebekka Thøgersen, Bjørn Petrat-Melin, Galia Zamaratskaia, Kai Grevsen, Jette Feveile Young, Martin Krøyer Rasmussen
The physiological effects of the Stevia-derived compounds, rebaudioside A, stevioside and steviol have been the focus of several studies due to their use as sweeteners in food. Despite that, little is known about their potential food-drug interactions. In the present study, IPEC-J2 cells and primary hepatocytes were used to investigate the effect of rebaudioside A, stevioside and steviol on cytochrome p450 (CYP) mRNA expression. Moreover, hepatic microsomes were used to investigate direct interactions between the compounds and specific CYP activity...
August 30, 2018: Food Chemistry
https://www.readbyqxmd.com/read/29655695/alisma-orientale-extract-exerts-the-reversing-cholestasis-effect-by-activation-of-farnesoid-x-receptor
#8
Xiao-Kui Huo, Jing Liu, Zhen-Long Yu, Yi-Fei Wang, Chao Wang, Xiang-Ge Tian, Jing Ning, Lei Feng, Cheng-Peng Sun, Bao-Jing Zhang, Xiao-Chi Ma
BACKGROUND: Cholestasis is a clinical syndrome of liver damage that is caused by accumulation of bile acids in the liver and systemic circulation. Farnesoid X receptor (FXR) can regulate synthesis, metabolism, and excretion of bile acids. The rhizomes of Alisma orientale is a well-known traditional Chinese medicine to treat edema, obesity, gonorrhea, leukorrhea, diarrhea, hyperlipidemia, and diabetes in China. HYPOTHESIS/PURPOSE: We hypothesized Alisma orientale extract (AOE) to exert hepatoprotective effect against α-naphthylisothiocyanate (ANIT) induced cholestasis in rat...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29655693/molecular-modeling-and-in-vitro-approaches-towards-cholinesterase-inhibitory-effect-of-some-natural-xanthohumol-naringenin-and-acyl-phloroglucinol-derivatives
#9
Ilkay Erdogan Orhan, Dariusz Jedrejek, F Sezer Senol, Ramin Ekhteiari Salmas, Serdar Durdagi, Iwona Kowalska, Lukasz Pecio, Wieslaw Oleszek
BACKGROUND: Many natural products, particularly phenolic compounds, have been reported to have a strong inhibition against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the key enzymes in the pathology of Alzheimer's disease (AD). HYPOTHESIS: Therefore, we hypothesized that some xanthahumol, naringenin, and acyl phloroglucinol derivatives (1-14) isolated from Humulus lupulus L. (hops) may have an inhibitory potential against AChE and BChE. METHODS: Inhibitory potential of compounds 1-14 were tested against AChE and BChE using ELISA microtiter assay...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29653288/ph-protective-y-1-receptor-ligand-functionalized-antiphagocytosis-bplp-wpu-micelles-for-enhanced-tumor-imaging-and-therapy-with-prolonged-survival-time
#10
Zhenqi Jiang, Yuchen Tian, Dingying Shan, Yinjie Wang, Ethan Gerhard, Jianbi Xia, Rong Huang, Yan He, Aiguo Li, Jianchao Tang, Huimin Ruan, Yong Li, Juan Li, Jian Yang, Aiguo Wu
Nanoparticle-based tumor therapies are extensively studied; however, few are capable of improving patient survival time due to premature drug leakage, off target effects, and poor tissue penetration. Previously, we successfully synthesized a novel family of Y1 receptor (Y1 R) ligand modified, photoluminescent BPLP nanobubbles and nanoparticles for targeted breast cancer ultrasound imaging; however, increased accumulation could also be observed in the liver, kidney, and spleen, suggesting significant interaction of the particles with macrophages in vivo...
April 4, 2018: Biomaterials
https://www.readbyqxmd.com/read/29653286/stromal-cell-laden-3d-hydrogel-microwell-arrays-as-tumor-microenvironment-model-for-studying-stiffness-dependent-stromal-cell-cancer-interactions
#11
Xiaoshan Yue, Trung Dung Nguyen, Victoria Zellmer, Siyuan Zhang, Pinar Zorlutuna
Tumor properties such as growth and metastasis are dramatically dependent on the tumor microenvironment (TME). However, the diversity of the TME including the stiffness and the composition of the extracellular matrix (ECM), as well as the involvement of stromal cells, makes it extremely difficult to establish proper in vitro models for studying tumor growth and metastasis. In this research, we fabricated a stromal cell-laden microwell array system with tunable stiffness ranging from 200 Pa up to 3 kPa, which covers the stiffness range of normal and cancerous mammary tissues, to study the effect of ECM stiffness on stromal-cancer interaction...
April 3, 2018: Biomaterials
https://www.readbyqxmd.com/read/29653244/opioid-utilization-following-cervical-spine-surgery-trends-and-factors-associated-with-long-term-use
#12
Andrew J Pugely, Nicholas A Bedard, Piyush Kalakoti, Nathan R Hendrickson, Jamal N Shillingford, Joseph L Laratta, Comron Saifi, Ronald A Lehman, K Daniel Riew
BACKGROUND CONTEXT: Limited or no data exist evaluating risk-factors associated with prolonged opioid use following cervical arthrodesis. PURPOSE: To assess trends in post-operative narcotic use amongst preoperative opioid users (OU) versus non-opioid users (NOU), and identify factors associated with postoperative narcotic use at 1-year following cervical arthrodesis. STUDY DESIGN/SETTING: Retrospective, observational study. PATIENT SAMPLE: 17,391 patients (OU: 52...
April 10, 2018: Spine Journal: Official Journal of the North American Spine Society
https://www.readbyqxmd.com/read/29653214/poly-propylene-imine-glycodendrimers-non-covalently-bind-atp-in-a-ph-and-salt-dependent-manner-model-studies-for-adenosine-analogue-drug-delivery
#13
Michał Gorzkiewicz, Adam Buczkowski, Dietmar Appelhans, Brigitte Voit, Łukasz Pułaski, Bartłomiej Pałecz, Barbara Klajnert-Maculewicz
Adenosine analogue drugs (such as fludarabine or cladribine) require transporter-mediated uptake into cells and subsequent phosphorylation for anticancer activity. Therefore, application of nanocarrier systems for direct delivery of active triphosphate nucleotides has been proposed. Here, we applied isothermal titration calorimetry (ITC) and zeta potential titration to determine the stoichiometry and thermodynamic parameters of interactions between 4th generation poly(propylene imine) (PPI G4) dendrimers (unmodified or sugar-modified for increased biocompatibility) and ATP as a model adenosine nucleotide...
April 10, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29653181/zh-1-enhances-the-anticancer-activity-of-gemcitabine-via-deoxyribonucleotide-synthesis-and-apoptotic-pathway-against-a549-cells
#14
Jianru Guo, Yan Li, Christopher Wai Kei Lam, Caiyun Wang, Meicun Yao, Wei Zhang
The purpose of this study was to investigate the inhibitory effect of ZH-1 ((6S,9aS,6aR,9bR)-6-(phenylcarbonyl)-6,6a,9a,9b-tetrahydro-8H-azolidino[3,4-a]b enzo [e]indolizine-7,9-dione) and its potential interactions with gemcitabine in A549 cells. MTT assay showed that the combined use of gemcitabine and ZH-1 presented a significant inhibition effect on A549 cell growth with the cell viability from 82.3 ± 5.6% to 51.0 ± 6.6%. The CI value was 0.60 suggesting a synergistic effect between these two drugs...
April 10, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29653076/e4bp4-regulates-carboxylesterase-2-enzymes-through-repression-of-the-nuclear-receptor-rev-erb%C3%AE-in-mice
#15
Mengjing Zhao, Tianpeng Zhang, Fangjun Yu, Lianxia Guo, Baojian Wu
Carboxylesterases (CES) are a family of phase I enzymes that plays an important role in xenobiotic clearance and lipid metabolism. Here, we investigate a potential role of E4 promoter-binding protein 4 (E4bp4) in regulation of Ces and CPT-11 (irinotecan, a first-line drug for treating colorectal cancer) pharmacokinetics in mice. Mouse hepatoma Hepa-1c1c7 cells were transfected with Rev-erbα expression plasmid or siRNA targeting E4bp4. The relative mRNA and protein levels of Ces enzymes in the cells or the livers of wild-type and E4bp4-deficient (E4bp4-/- ) mice were determined by qPCR and Western blotting, respectively...
April 10, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29652833/a-lipophilic-ir-780-dye-encapsulated-zwitterionic-polymer-lipid-micellar-nanoparticle-for-enhanced-photothermal-therapy-and-nir-based-fluorescence-imaging-in-a-cervical-tumor-mouse-model
#16
Santhosh Kalash Rajendrakumar, Ning-Chu Chang, Adityanarayan Mohapatra, Saji Uthaman, Byeong-Il Lee, Wei-Bor Tsai, In-Kyu Park
To prolong blood circulation and avoid the triggering of immune responses, nanoparticles in the bloodstream require conjugation with polyethylene glycol (PEG). However, PEGylation hinders the interaction between the nanoparticles and the tumor cells and therefore limits the applications of PEGylated nanoparticles for therapeutic drug delivery. To overcome this limitation, zwitterionic materials can be used to enhance the systemic blood circulation and tumor-specific delivery of hydrophobic agents such as IR-780 iodide dye for photothermal therapy...
April 13, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29652491/inhibition-of-voltage-gated-k-channel-kv1-5-by-anti-arrhythmic-drugs
#17
Rong Chen, Shin-Ho Chung
Molecular dynamics simulations are employed to determine the inhibitory mechanisms of three drugs, 5-(4- phenoxybutoxy)psoralen (PAP-1), vernakalant and flecainide, on the voltage-gated K+ channel Kv1.5, a target for the treatment of cardiac arrhythmia. At neutral pH, PAP-1 is neutral, whereas the other two molecules carry one positive charge. We show that PAP-1 forms stable dimers in water, primarily through the hydrophobic interactions between aromatic rings. All three molecules bind to the cavity between the Ile508 and Val512 residues from the four subunits of the channel...
April 13, 2018: Biochemistry
https://www.readbyqxmd.com/read/29652194/molecular-docking-revealed-the-binding-of-nucleotide-side-inhibitors-to-zika-viral-polymerase-solved-structures
#18
A A Elfiky, A M Ismail
A new Zika virus (ZIKV) outbreak started in 2015. According to the World Health Organization, 84 countries confirmed ZIKV infection. RNA-dependent RNA polymerase (RdRp) was an appealing target for drug designers during the last two decades. Through molecular docking, we screened 16 nucleotide/side inhibitors against ZIKV RdRp. While the mode of interaction with ZIKV is different from that in the hepatitis C virus (HCV), nucleotide/side inhibitors in this study (mostly anti-HCV) showed promising binding affinities (-6...
May 2018: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/29652130/in-vivo-targeted-responsive-and-synergistic-cancer-nanotheranostics-by-mri-guided-synergistic-hifu-ablation-and-chemotherapy
#19
Hailin Tang, Yuan Guo, Li Peng, Hui Fang, Zhigang Wang, Yuanyi Zheng, Haitao Ran, Yu Chen
As one of the most representative non-invasive therapeutic modalities, high-intensity focused ultrasound (HIFU) has shown the great promise for cancer therapy, but its low therapeutic efficacy and biosafety significantly hinder the further extensive clinical translation and application. In this work, we report on the construction of a multifunctional theranostic nanoplatform to synergistically enhance the HIFU-therapeutic efficacy based on nanomedicine. A targeted and temperature-responsive theranostic nanoplatform (PFH/DOX@PLGA/Fe3O4-FA) has been designed and fabricated for efficient ultrasound/magnetic resonance dual-modality imaging-guided HIFU/chemo synergistic therapy...
April 13, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29651943/benzoin-schiff-bases-design-synthesis-and-biological-evaluation-as-potential-antitumor-agents
#20
Dima A Sabbah, Fatima Al-Tarawneh, Wamidh H Talib, Kamal Sweidan, Sanaa K Bardaweel, Eveen Al-Shalabi, Haizhen A Zhong, Ghassan Abu Sheikha, Reema Abu Khalaf, Mohammad S Mubarak
BACKGROUND: Phosphoinositide 3-kinase α (PI3Kα) is an attractive target for anticancer drug design. OBJECTIVES: Target compounds were designed to probe the significance of alcohol and imine moieties tailored on a benzoin scaffold to better understand the structure activity relation (SAR) and improve their biological activity as anticancer compounds. METHODS: Chemical synthesis of the targeted compounds, biological evaluation tests against human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines, as well as Glide docking studies were employed in this investigation...
April 12, 2018: Medicinal Chemistry
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