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https://www.readbyqxmd.com/read/29786960/the-atomic-resolution-structure-of-a-class-c-%C3%AE-lactamase-and-of-its-complex-with-avibactam
#1
Stefano Mangani, Cecilia Pozzi, Flavio Di Pisa, Filomena De Luca, Manuela Benvenuti, Jean-Denis Docquier
β-lactamases (BLs) are important antibiotic resistance determinants that significantly compromise the efficacy of valuable β-lactam antibacterial drugs. For that reason, combinations with β-lactamase inhibitor were developed. Avibactam is the first non-β-lactam BL inhibitor introduced in clinical practice. Ceftazidime-avibactam represents one of the few last-resort antibiotics available for the treatment of infections caused by near pandrug-resistant bacteria. TRU-1 is a chromosomally-encoded AmpC-type BL of Aeromonas enteropelogenes, related to the FOX-type BLs and constitutes a good model for class C BLs...
May 22, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29786944/design-synthesis-and-evaluation-of-a-novel-series-of-inhibitors-reversing-p-glycoprotein-mediated-multidrug-resistance
#2
Hesham Ghaleb, Huilan Li, Mutta Kairuki, Qianqian Qiu, Xinzhou Bi, Chunxia Liu, Chen Liao, Jieming Li, Kamal Hezam, Wenlong Huang, Hai Qian
Multidrug resistance (MDR) is still the main barrier to attaining effective results with chemotherapy. Discovery of new chemo-reversal agents is needed to overcome MDR. Our study focused on a better way to obtain novel drugs with triazole rings that have an MDR-reversal ability through click chemistry. Among 20 developed compounds, compound 19 had a minimal cytotoxic effect compared to tariquidar and verapamil (VRP) and showed a higher reversal activity than VRP through increased accumulation in K562/A02 cells...
May 22, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29786852/evolution-of-lobar-abnormalities-of-cerebral-glucose-metabolism-in-41-children-with-drug-resistant-epilepsy
#3
Tuhina Govil-Dalela, Ajay Kumar, Michael E Behen, Harry T Chugani, Csaba Juhász
OBJECTIVE: We analyzed long-term changes of lobar glucose metabolic abnormalities in relation to clinical seizure variables and development in a large group of children with medically refractory epilepsy. METHODS: Forty-one children (25 males) with drug-resistant epilepsy had a baseline positron emission tomography (PET) scan at a median age of 4.7 years; the scans were repeated after a median of 4.3 years. Children with progressive neurological disorders or space-occupying lesion-related epilepsy and those who had undergone epilepsy surgery were excluded...
May 22, 2018: Epilepsia
https://www.readbyqxmd.com/read/29786784/generation-of-prostate-cancer-patient-derived-xenografts-to-investigate-mechanisms-of-novel-treatments-and-treatment-resistance
#4
Hung-Ming Lam, Holly M Nguyen, Eva Corey
Treatment advances lead to survival benefits of patients with advanced prostate cancer. These treatments are highly efficacious in a subset of patients; however, similarly to other cancers, after initial responses the tumors develop resistance (acquired resistance) and the patients succumb to the disease. Furthermore, there is a subset of patients who do not respond to the treatment at all (de novo resistance). Preclinical testing using patient-derived xenografts (PDXs) has led to successful drug development, and PDXs will continue to provide valuable resources to generate clinically relevant data with translational potential...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29786782/preclinical-impact-of-high-dose-intermittent-antiangiogenic-tyrosine-kinase-inhibitor-pazopanib-in-intrinsically-resistant-tumor-models
#5
Elaine Reguera-Nuñez, Shan Man, Ping Xu, Robert S Kerbel
Antiangiogenic tyrosine kinase inhibitors (TKIs) target vascular endothelial growth factor receptors and other receptor tyrosine kinases. As a result of toxicity, the clinical failures or the modest benefits associated with antiangiogenic TKI therapy may be related in some cases to suboptimal drug dosing and scheduling, thereby facilitating resistance. Most antiangiogenic TKIs, including pazopanib, are administered on a continuous daily basis. Here, instead, we evaluated the impact of increasing the dose and administering the drug intermittently...
May 21, 2018: Angiogenesis
https://www.readbyqxmd.com/read/29785875/egfr-tkis-in-non-small-cell-lung-cancer-focus-on-clinical-pharmacology-and-mechanisms-of-resistance
#6
Stefano Fogli, Beatrice Polini, Marzia Del Re, Iacopo Petrini, Antonio Passaro, Stefania Crucitta, Eleonora Rofi, Romano Danesi
The clinical introduction of EGFR-TKIs within the oncologic armamentarium has changed the therapeutic landscape of non-small-cell lung cancer (NSCLC) creating widespread expectations both in patients and clinicians. However, several gaps in current understanding leave open important questions regarding the use of these drugs in clinical practice. For instance, there is uncertainty in regard to which EGFR-TKI should be given first in naive patients with EGFR-driven malignancies since different generations of drugs are available with different pharmacological profiles...
May 22, 2018: Pharmacogenomics
https://www.readbyqxmd.com/read/29785848/the-total-synthesis-of-tetarimycin-a-%C3%A2-naphthacemycin-a-9-and-%C3%A2-fasamycin-a-structure-activity-relationship-studies-against-drug-resistant-bacteria
#7
Jing-Kai Huang, Tsai-Ling Yang Lauderdale, Chun-Cheng Lin, Kak-Shan Shia
Making use of a reductive olefin coupling reaction and Michael-Dieckmann condensation as two key operations, we have completed a concise total synthesis of tetarimycin A, (±)-naphthacemycin A9 and (±)-fasamycin A in a highly convergent and practical protocol. Synthetic procedures thus developed have also been applied to providing related analogues for structure-activity relationship studies, thereof coming to a conclusion that the free hydroxyl group at C-10 is essential for exerting inhibitory activities against a panel of Gram-positive bacteria, including drug-resistant strains VRE and MRSA...
May 22, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29785653/valproic-acid-treatment-response-in-vitro-is-determined-by-tp53-status-in-medulloblastoma
#8
Bruna Mascaro-Cordeiro, Indhira Dias Oliveira, Francine Tesser-Gamba, Lorena Favaro Pavon, Nasjla Saba-Silva, Sergio Cavalheiro, Patrícia Dastoli, Silvia Regina Caminada Toledo
PURPOSE: Histone deacetylate inhibitors (HDACi), as valproic acid (VA), have been reported to enhance efficacy and to prevent drug resistance in some tumors, including medulloblastoma (MB). In the present study, we investigated VA role, combined to cisplatin (CDDP) in cell viability and gene expression of MB cell lines. METHODS: Dose-response curve determined IC50 values for each treatment: (1) VA single, (2) CDDP single, and (3) VA and CDDP combined. Cytotoxicity and flow cytometry evaluated cell viability after exposure to treatments...
May 22, 2018: Child's Nervous System: ChNS: Official Journal of the International Society for Pediatric Neurosurgery
https://www.readbyqxmd.com/read/29785534/an-enzyme-free-homogenous-electrochemical-assay-for-sensitive-detection-of-the-plasmid-mediated-colistin-resistance-gene-mcr-1
#9
Bo Li, Zhixin Chai, Xiaohui Yan, Chunchen Liu, Bo Situ, Ye Zhang, Weilun Pan, Shihua Luo, Jianhua Liu, Lei Zheng
Antibiotic resistance associated with the mcr-1 gene of Gram-negative bacteria, which confers resistance to drugs of last resort and has the potential to spread via plasmids, is one of the most pressing issues facing global health today. Point-of-care testing for the mcr-1 gene is needed to aid in the identification of colistin resistance in the field and to control its horizontal transmission. Here, we report the successful development of an enzyme-free homogenous electrochemical strategy for sensitive detection of the antibiotic resistance gene mcr-1 using the hybridization chain reaction and mcr-1-specific toehold probe...
May 22, 2018: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/29785484/challenges-in-malaria-management-and-a-glimpse-at-some-nanotechnological-approaches
#10
Adrian Najer, Cornelia G Palivan, Hans-Peter Beck, Wolfgang Meier
Malaria is a devastating infectious disease transmitted by mosquitoes, affecting millions of people and killing about half a million children each year. Despite tremendous progress in the control and elimination of malaria within the past years, there are still considerable challenges to be solved. To name a few, drug-resistant parasites, insecticide-resistant mosquitoes and the difficulty to formulate a potent malaria vaccine need to be addressed with new strategies to achieve the final goal of malaria eradication...
2018: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29785480/potential-treatment-options-in-a-post-antibiotic-era
#11
R R Bragg, C M Meyburgh, J-Y Lee, M Coetzee
Following the Golden Age of antibiotic discovery in the previous century, the rate of antibiotic discovery has plummeted during the past 50 years while the incidence of antimicrobial resistance is ever-increasing. Presently, humankind is forced to address a major public health threat in the form of multiple drug resistance and urgent action is required to halt the advent of a post-antibiotic era. This chapter aims to draw the attention to the escalating global crisis of antimicrobial resistance fueled by the irresponsible use of antibiotics in healthcare and animal production sectors...
2018: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29785478/changing-trend-of-infectious-diseases-in-nepal
#12
Shiba Kumar Rai
Many infectious/communicable diseases (IDs) are endemic in Nepal. Until a decade and half ago, IDs were the major cause of both morbidity and mortality accounting 70% for both. However, as a result of various preventive measures implemented by both the state and non-state actors, the overall IDs have shown a changing (declining) trend. The most impressive decline has been seen in the intestinal helminth infection. Though the overall burden of IDs is decreasing, several newer infectious diseases (emerging infections) namely, dengue fever, scrub typhus, influenza (H5N1 and H1N1), and others are posing a great public health problem...
2018: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29785434/integration-of-phospholipid-hyaluronic-acid-methotrexate-nanocarrier-assembly-and-amphiphilic-drug-drug-conjugate-for-synergistic-targeted-delivery-and-combinational-tumor-therapy
#13
Yang Li, Huabing Zhang, Yilin Chen, Jinyuan Ma, Jinyan Lin, Yinying Zhang, Zhongxiong Fan, Guanghao Su, Liya Xie, Xuan Zhu, Zhenqing Hou
Combinational cancer therapy has been considered as a promising strategy to achieve synergetic therapeutic effects and suppression of multidrug resistance. Herein, we adopted a combination of methotrexate (MTX), an antimetabolite acting on cytoplasm, and 10-hydroxycamptothecin (HCPT), an alkaloid acting on nuclei, to treat cancer. Given the different solubilities, membrane permeabilities, and anticancer mechanisms of both drugs, we developed a dual-targeting delivery system based on 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-hyaluronic acid (a principal ligand of CD44 receptors)-MTX (a selective ligand of folate receptors) nanoparticles, which was exploited to carry HCPT-MTX conjugate for synergistically boosting dual-drug co-delivery...
May 22, 2018: Biomaterials Science
https://www.readbyqxmd.com/read/29785232/effects-of-fasudil-on-patients-with-pulmonary-hypertension-associated-with-left-ventricular-heart-failure-with-preserved-ejection-fraction-a-prospective-intervention-study
#14
Xiang Zhang, Xueming Zhang, Saihua Wang, Jun Luo, Zhihong Zhao, Changzhu Zheng, Jieyan Shen
Background: Pulmonary hypertension due to left ventricular heart failure with preserved ejection fraction (PH-HFpEF) is an increasingly medical problem. The aim of the study was to evaluate the clinical efficacy of fasudil on PH-HFpEF elderly patients and to figure out the subtype of PH-HFpEF which may be the therapeutic object of fasudil. Method: 58 PH-HFpEF elderly patients were enrolled. Patients were diagnosed with passive pulmonary hypertension (PPH) or reactive pulmonary hypertension (RPH) by right heart catheterization and all receiving Rho kinase inhibitor fasudil for 2 weeks...
2018: Canadian Respiratory Journal: Journal of the Canadian Thoracic Society
https://www.readbyqxmd.com/read/29785131/epidemiology-susceptibility-and-risk-factors-for-acquisition-of-mdr-xdr-gram-negative-bacteria-among-kidney-transplant-recipients-with-urinary-tract-infections
#15
Xiuhong Yuan, Taohua Liu, Di Wu, Qiquan Wan
Background: Multiple drug resistant/extensively drug resistant (MDR/XDR) Gram-negative urinary tract infections (UTIs) represent a growing threat to kidney transplant recipients. This retrospective study aimed to assess the incidence and microbiological profile of MDR/XDR Gram-negative UTIs, to identify drug susceptibility of MDR/XDR bacteria, and to determine the potential risk factors for MDR/XDR UTIs in kidney recipients. Materials and methods: During the study period, 1569 patients underwent consecutive kidney transplantation in two transplantation centers...
2018: Infection and Drug Resistance
https://www.readbyqxmd.com/read/29785129/performance-of-the-abbott-realtime-mtb-rif-inh-resistance-assay-when-used-to-test-mycobacterium-tuberculosis-specimens-from-bangladesh
#16
Joshua Kostera, Gregor Leckie, Klara Abravaya, Hong Wang
Introduction: The Abbott RealTime MTB RIF/INH Resistance Assay (RT MTB RIF/INH) is an assay for the detection of rifampicin (RIF)- and/or isoniazid (INH)-resistant Mycobacterium tuberculosis (MTB). The assay can be used to test sputum, bronchial alveolar lavage, and N-Acetyl-L-Cysteine (NALC)/NaOH pellets prepared from these samples. The assay can be used in direct testing mode, or in reflex mode following a MTB positive result produced by its companion assay, Abbott RT MTB. Methods: In this study, the direct testing mode was used to test paired sputum and NALC/NaOH pellets prepared from sputum collected from Bangladesh TB patients...
2018: Infection and Drug Resistance
https://www.readbyqxmd.com/read/29785088/insight-into-resistance-mechanism-of-anaplastic-lymphoma-kinase-to-alectinib-and-jh-viii-157-02-caused-by-g1202r-solvent-front-mutation
#17
Han Wang, Yao Wang, Wentao Guo, Bin Du, Xiaobing Huang, Riping Wu, Baoyu Yang, Xiaoyan Lin, Yilan Wu
Background: Mutated anaplastic lymphoma kinase (ALK) drives the development of advanced non-small cell lung cancer (NSCLC). Most reported small-molecule inhibitors targeting the ALK domain do not display good inhibition of the G1202R solvent front mutation. The solvent front mutation was assumed to hinder drug binding. However, a different fact could be uncovered by the simulations reported in this study through a structural analog of alectinib (JH-VIII-157-02), which demonstrated potent effects against the G1202R mutation...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29785042/inducible-high-efficiency-crispr-cas9-targeted-gene-editing-and-precision-base-editing-in-african-trypanosomes
#18
Eva Rico, Laura Jeacock, Julie Kovářová, David Horn
The Cas9 endonuclease can be programmed by guide RNA to introduce sequence-specific breaks in genomic DNA. Thus, Cas9-based approaches present a range of novel options for genome manipulation and precision editing. African trypanosomes are parasites that cause lethal human and animal diseases. They also serve as models for studies on eukaryotic biology, including 'divergent' biology. Genome modification, exploiting the native homologous recombination machinery, has been important for studies on trypanosomes but often requires multiple rounds of transfection using selectable markers that integrate at low efficiency...
May 21, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29784845/interaction-of-bacterial-phenazines-with-colistimethate-in-bronchial-epithelial-cells
#19
Valeri V Mossine, Deborah L Chance, James K Waters, Thomas P Mawhinney
Multidrug-resistant bacterial infections are being increasingly treated in clinics with polymyxins, a class of antibiotics associated with adverse effects in the kidney, nervous system, or airways of a significant proportion of human and animal patients. Although many of the resistant pathogens display enhanced virulence, a hazard of cytotoxic interactions between polymyxin antibiotics and bacterial virulence factors (VFs) has not been assessed, to date. We report here on testing paired combinations of four Pseudomonas aeruginosa VF phenazine toxins, pyocyanin (PYO), 1-hydroxyphenazine (1-HP), phenazine-1-carboxylic acid (PCA), phenazine-1-carboxamide (PCN), and two commonly prescribed polymyxin drugs, colistimethate (CMS)/colistin and polymyxin B, in three human airway cell lines, BEAS-2B, HBE-1, and CFT-1...
May 21, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29784838/in-vivo-and-in-vitro-effects-of-a-clpp-activating-antibiotic-against-vancomycin-resistant-enterococci
#20
Autumn Brown Gandt, Elizabeth C Griffith, Ida M Lister, Lisa L Billings, Angel Han, Rajendra Tangallapally, Ying Zhao, Aman P Singh, Richard E Lee, Michael D LaFleur
Antibiotics with novel bactericidal mechanisms of action are urgently needed. The antibiotic acyldepsipeptide 4 (ADEP4) activates the ClpP protease and causes cells to self-digest. The effects of ADEP4 and ClpP activation have not been sufficiently characterized for the enterococci, which are important pathogens known for high levels of acquired and intrinsic antibiotic resistance. In the present study, ADEP4 was found to be potently active against both Enterococcus faecalis and Enterococcus faecium with an MIC90 of 0...
May 21, 2018: Antimicrobial Agents and Chemotherapy
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