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https://www.readbyqxmd.com/read/29141199/disruption-of-mitochondrial-function-as-mechanism-for-anti-cancer-activity-of-a-novel-mitochondriotropic-menadione-derivative
#1
José Teixeira, Ricardo Amorim, Katia Santos, Pedro Soares, Sandipan Datta, Gino A Cortopassi, Teresa L Serafim, Vilma A Sardão, Jorge Garrido, Fernanda Borges, Paulo J Oliveira
Menadione, also known as vitamin K3, is a 2-methyl-1,4 naphthoquinone with a potent cytotoxic activity mainly resulting from its quinone redox-cycling with production of reactive oxygen species (ROS). Although increased ROS generation is considered a relevant mechanism in cancer cell death, it may not be sufficiently effective to kill cancer cells due to phenotypic adaptations. Therefore, combining ROS-generating agents with other molecules targeting important cancer cell phenotypes can be an effective therapeutic strategy...
November 12, 2017: Toxicology
https://www.readbyqxmd.com/read/29140684/janus-gold-nanoplatform-for-synergetic-chemoradiotherapy-and-computed-tomography-imaging-of-hepatocellular-carcinoma
#2
Zheng Wang, Dan Shao, Zhimin Chang, Mengmeng Lu, Yingshuai Wang, Juan Yue, Dian Yang, Mingqiang Li, Qiaobing Xu, Wenfei Dong
There is a pressing need to develop nanoplatforms that integrate multimodal therapeutics to improve treatment responses and prolong the survival of patients with unresectable hepatocellular carcinoma (HCC). Mesoporous silica-coated gold nanomaterials have emerged as a novel multifunctional platform combining tunable surface plasmon resonance and mesoporous properties that exhibit multimodality properties in cancer theranostics. However, their reduced radiation-absorption efficiency and limited surface area hinder their further radiochemotherapeutic applications...
November 15, 2017: ACS Nano
https://www.readbyqxmd.com/read/29140595/modulation-of-quorum-sensing-in-a-gram-positive-pathogen-by-linear-imprinted-copolymers-with-anti-infective-properties
#3
Anfal Motib, Antonio Guerreiro, Firas Al-Bayati, Elena Piletska, Irfan Manzoor, Sulman Shafeeq, Anagha Kadam, Oscar Kuipers, Luisa Hiller, Todd Cowen, Sergey Piletsky, Peter Andrew, Hasan Yesilkaya
Here we describe the development, characterization and biological testing of a new type of linear molecularly imprinted polymer (LMIP) designed to act as anti-infective by blocking the quorum sensing (QS) mechanism and so preventing virulence of the pathogen Streptococcus pneumoniae. The LMIP is prepared (polymerized) in presence of a template molecule, but unlike in traditional molecular imprinting approaches no cross-linker is used. This results in soluble low molecular weight polymer that can act as drug agent in vitro and in vivo...
November 15, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/29140472/uric-acid-predicts-adverse-outcomes-in-chronic-kidney-disease-a-novel-insight-from-trajectory-analyses
#4
Ching-Wei Tsai, Hsien-Tsai Chiu, Han-Chun Huang, I-Wen Ting, Hung-Chieh Yeh, Chin-Chi Kuo
Background: Very little is known about longitudinal trajectories of serum uric acid (SUA) over the course of chronic kidney disease (CKD). We aimed to determine whether longitudinal SUA trajectories are associated with the risk of end-stage renal disease (ESRD) and all-cause mortality among CKD patients. Methods: We conducted a prospective cohort study from a 13-year multidisciplinary pre-ESRD care registry. The final study population consisted of 5090 CKD patients aged 20-90 years between 2003 and 2015...
November 10, 2017: Nephrology, Dialysis, Transplantation
https://www.readbyqxmd.com/read/29139202/lego-inspired-drug-design-unveiling-of-the-novel-class-of-benzo-d-thiazole-containing-a-3-4-dihydroxyphenyl-moiety-as-plasma-membrane-h-atpase-inhibitors
#5
Truong Thanh Tung, Dao Trong Tuan, Marta Grifell Junyent, Michael Palmgren, Thomas Günther-Pomorski, Anja Thoe Fuglsang, Søren Brøgger Christensen, John Nielsen
The fungal plasma membrane H+-ATPase (Pma1p) is a potential target for the discovery of new antifungal agents. Surprisingly, no structure-activity relationship studies for small molecules targeting Pma1p have been reported. Herein, we disclose a LEGO-inspired fragment assembly strategy for design, synthesis and discovery of benzo[d]thiazoles containing a 3,4-dihydroxyphenyl moiety as potential Pma1p inhibitors. A series of 2-(benzo[d]thiazol-2-ylthio)-1-(3,4-dihydroxyphenyl)ethanones was found to inhibit Pma1p with the most potent IC50 of 8 µM in an in vitro plasma membrane H+-ATPase assay...
November 15, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29139135/phase-1-study-of-quizartinib-in-combination-with-induction-and-consolidation-chemotherapy-in-patients-with-newly-diagnosed-acute-myeloid-leukemia
#6
Jessica K Altman, James M Foran, Keith W Pratz, Denise Trone, Jorge E Cortes, Martin S Tallman
Novel therapies have potential to improve outcomes in patients with acute myeloid leukemia (AML) harboring FLT3-ITD mutations that have high risk of relapse and poor survival following standard of care (SOC) cytarabine/anthracycline-based induction/consolidation chemotherapy. Quizartinib is a selective and highly potent FLT3 inhibitor that has shown strong single-agent activity in relapsed or refractory (R/R) AML. This phase 1, open-label, sequential group dose-escalation trial (NCT 01390337) is the first evaluating safety and tolerability of quizartinib in combination with SOC chemotherapy in newly diagnosed AML (ndAML)...
November 15, 2017: American Journal of Hematology
https://www.readbyqxmd.com/read/29138944/design-synthesis-conformational-and-molecular-docking-study-of-some-novel-acyl-hydrazone-based-molecular-hybrids-as-antimalarial-and-antimicrobial-agents
#7
Parvin Kumar, Kulbir Kadyan, Meenakshi Duhan, Jayant Sindhu, Vineeta Singh, Baljeet Singh Saharan
BACKGROUND: Acyl hydrazones are an important class of heterocyclic compounds promising pharmacological characteristics. Malaria is a life-threatening mosquito-borne blood disease caused by a plasmodium parasite. In some places, malaria can be treated and controlled with early diagnosis. However, some countries lack the resources to do this effectively. RESULTS: The present work involves the design and synthesis of some novel acyl hydrazone based molecular hybrids of 1,4-dihydropyridine and pyrazole (5a-g)...
November 14, 2017: Chemistry Central Journal
https://www.readbyqxmd.com/read/29138869/cepharanthine-exhibits-a-potent-anticancer-activity-in-p53-mutated-colorectal-cancer-cells-through-upregulation-of-p21waf1-cip1
#8
Arkornnut Rattanawong, Vilawan Payon, Wacharee Limpanasittikul, Chatikorn Boonkrai, Apiwat Mutirangura, Piyanuch Wonganan
Cepharanthine (CEP), a biscoclurine alkaloid isolated from Stephania cepharantha Hayata, has demonstrated anticancer activity in several different types of cancer cells. Colorectal cancer (CRC) is one of the most common cancers in both men and women. Mutated p53 in CRC was reported to be associated with resistance to commonly used chemotherapeutic agents including, 5‑fluorouracil, oxaliplatin and irinotecan. Many studies reported that mutation of p53 induced chemoresistance through several mechanisms, including induction of drug efflux, disruption of cell cycle regulation, evasion of apoptosis and upregulation of DNA repair...
November 9, 2017: Oncology Reports
https://www.readbyqxmd.com/read/29138831/anti%C3%A2-inflammatory-effect-of-migri%C3%A2-heal%C3%A2-in-an-in%C3%A2-vitro-inflammatory-model-of-primary-mixed-glial-cells
#9
Mahmoud Hassani, Farzaneh Sabouni, Mohammad Ansari, Solaleh Emamgholipour, Mohammad-Sadegh Fallah, Shah-Sanam Abbasi, Saeed Ansari Majd
Migri‑Heal®, is a novel herbal remedy that was introduced for the treatment of migraine headaches. Previous studies revealed that this drug may reduce nitric oxide (NO) in an in vitro inflammatory model. The aim of the present study was to investigate the anti‑inflammatory effect of Migri‑Heal® on primary mix glial cells stimulated with LPS. In the current study, neonatal rat primary mix glial cells were isolated from the mixed glial cultures via shaking, and cultured in Dulbecco's' modified Eagle's medium supplemented with 10% fetal bovine serum...
November 13, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29138806/effect-of-bis-hydroxymethyl-alkanoate-curcuminoid-derivative-mth-3-on-cell-cycle-arrest-apoptotic-and-autophagic-pathway-in-triple-negative-breast-adenocarcinoma-mda-mb-231-cells-an-in-vitro-study
#10
Ling-Chu Chang, Min-Tsang Hsieh, Jai-Sing Yang, Chi-Cheng Lu, Fuu-Jen Tsai, Je-Wei Tsao, Yu-Jen Chiu, Sheng-Chu Kuo, Kuo-Hsiung Lee
Curcumin has been shown to exert potential antitumor activity in vitro and in vivo involved in multiple signaling pathways. However, the application of curcumin is still limited because of its poor hydrophilicity and low bio-availability. In the present study, we investigated the therapeutic effects of a novel and water soluble bis(hydroxymethyl) alkanoate curcuminoid derivative, MTH-3, on human breast adenocarcinoma MDA-MB-231 cells. This study investigated the effect of MTH-3 on cell viability, cell cycle and induction of autophagy and apoptosis in MDA-MB-231 cells...
November 14, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/29138609/non-valvular-atrial-fibrillation-impact-of-apixaban-on-patient-outcomes
#11
REVIEW
Adam Ioannou, Irene Tsappa, Sofia Metaxa, Constantinos G Missouris
Atrial fibrillation is the most common arrhythmia worldwide, and carries a significantly increased risk of thromboembolic stroke. Initially, vitamin K antagonists were used as stroke prophylaxis; but more recently, a group of drugs known as novel oral anticoagulants have been developed. Apixaban belongs to this group of drugs, and is a factor Xa inhibitor that has emerged as a popular pharmacological agent worldwide. In this review, we will provide an overview of the pivotal trials in the development of apixaban, while also critically evaluating the new emerging real-world data, and discussing the effectiveness, safety, economic viability and future prospects of apixaban and how it impacts on patient outcomes in those with non-valvular atrial fibrillation...
2017: Patient related Outcome Measures
https://www.readbyqxmd.com/read/29138537/development-of-novel-ultrashort-antimicrobial-peptide-nanoparticles-with-potent-antimicrobial-and-antibiofilm-activities-against-multidrug-resistant-bacteria
#12
Ammar Almaaytah, Gubran Khalil Mohammed, Ahmad Abualhaijaa, Qosay Al-Balas
Conventional antibiotics are facing strong microbial resistance that has recently reached critical levels. This situation is leading to significantly reduced therapeutic potential of a huge proportion of antimicrobial agents currently used in clinical settings. Antimicrobial peptides (AMPs) could provide the medical community with an alternative strategy to traditional antibiotics for combating microbial resistance. However, the development of AMPs into clinically useful antibiotics is hampered by their relatively low stability, toxicity, and high manufacturing costs...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29138437/photosensitized-ina-labelled-protein-1-phil1-is-novel-component-of-the-inner-membrane-complex-and-is-required-for-plasmodium-parasite-development
#13
Ekta Saini, Mohammad Zeeshan, Declan Brady, Rajan Pandey, Gesine Kaiser, Ludek Koreny, Pradeep Kumar, Vandana Thakur, Shreyansh Tatiya, Nicholas J Katris, Rebecca Stanway Limenitakis, Inderjeet Kaur, Judith L Green, Andrew R Bottrill, David S Guttery, Ross F Waller, Volker Heussler, Anthony A Holder, Asif Mohmmed, Pawan Malhotra, Rita Tewari
Plasmodium parasites, the causative agents of malaria, possess a distinctive membranous structure of flattened alveolar vesicles supported by a proteinaceous network, and referred to as the inner membrane complex (IMC). The IMC has a role in actomyosin-mediated motility and host cell invasion. Here, we examine the location, protein interactome and function of PhIL1, an IMC-associated protein on the motile and invasive stages of both human and rodent parasites. We show that PhIL1 is located in the IMC in all three invasive (merozoite, ookinete-, and sporozoite) stages of development, as well as in the male gametocyte and locates both at the apical and basal ends of ookinete and sporozoite stages...
November 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29138104/novel-mixed-vesicles-containing-lactobacilli-biosurfactant-for-vaginal-delivery-of-an-anti-candida-agent
#14
Angela Abruzzo, Barbara Giordani, Carola Parolin, Beatrice Vitali, Michele Protti, Laura Mercolini, Martina Cappelletti, Stefano Fedi, Federica Bigucci, Teresa Cerchiara, Barbara Luppi
The purpose of this work was to prepare and characterize an innovative formulation for vaginal delivery of econazole nitrate, commonly used for the treatment of Candida infections. A novel biosurfactant isolated from a vaginal Lactobacillus strain was used to prepare phosphatidylcholine based mixed vesicles. Biosurfactant was produced by Lactobacillus gasseri BC9, isolated from the vagina of a healthy premenopausal woman, and was chemically characterized by FT-IR and ESI-MS. Mixed vesicles, obtained through film rehydration and extrusion method, were characterized in terms of size, zeta potential, encapsulation efficiency, mucoadhesion properties and econazole release...
November 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29138086/eugenol-derivatives-prospectively-inhibit-l-asparaginase-a-heady-target-protein-of%C3%A2-salmonella-typhimurium
#15
Archana Vimal, Anubhuti Jha, Awanish Kumar
Salmonella typhimurium is the causative agent of severe human infections and mortality throughout the world. Pacing advent of new resistance mechanisms in this microorganism exists, rendering treatment of infectious disease difficult. Ciprofloxacin is no longer considered the first choice of antimicrobial agent due to the emergence of resistance. Therefore, the need for scenario is to find out novel drug target and its potential inhibitor to fight against this pathogen. The present study was undertaken to find out a novel drug target and its inhibitor for improving the current therapeutic methods for treating Salmonella infections...
November 11, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29138080/muscarinic-receptor-subtype-distribution-in-the-central-nervous-system-and-relevance-to-aging-and-alzheimer-s-disease
#16
REVIEW
E P Lebois, C Thorn, J R Edgerton, M Popiolek, S Xi
Muscarinic acetylcholine receptors (mAChRs) are G proteincoupled receptors (GPCRs) that mediate the metabotropic actions of acetylcholine (ACh). There are five subtypes of mAChR, M1 - M5, which are expressed throughout the central nervous system (CNS) on numerous cell types and represent promising treatment targets for a number of different diseases, disorders, and conditions of the CNS. Although the present review will focus on Alzheimer's disease (AD) and amnestic mild cognitive impairment (aMCI), a number of conditions such as Parkinson's disease (PD), schizophrenia, and others represent significant unmet medical needs for which selective muscarinic agents could offer therapeutic benefits...
November 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29137801/ultrasound-assisted-synthesis-of-nanocomposites-based-on-aromatic-polyamide-and-modified-zno-nanoparticle-for-removal-of-toxic-cr-vi-from-water
#17
Mohammad Dinari, Atefeh Haghighi
In this study, novel nanocomposites (NCs) of aromatic polyamide (PA) and surface modified ZnO nanoparticle with s-triazine heterocyclic ring was introduced for efficient removal of toxic hexavalent chromium (VI) from aqueous solution. The surface of ZnO nanoparticle was modified by s-triazine core silane coupling agent (ZnO-TSC) and PA/ZnO-TSC NCs with different amount of ZnO-TSC nanoparticles (0, 5, 10 and 15wt%) were prepared by ultrasonic irradiation. The synthesized PA/ZnO-TSC NCs were characterized by FT-IR, XRD, FE-SEM, TEM and TGA methods...
March 2018: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/29137796/construction-of-proton-exchange-membranes-under-ultrasonic-irradiation-based-on-novel-fluorine-functionalizing-sulfonated-polybenzimidazole-cellulose-silica-bionanocomposite
#18
Sheida Esmaielzadeh, Hashem Ahmadizadegan
Novel sulfonated polybenzimidazole (s-PBI)/cellulose/silica bionanocomposite membranes were prepared from fluorine-containing s-PBI copolymer with a cellulose/silica precursor and a bonding agent. The introduction of the bonding agent results in the reinforcing interfacial interaction between s-PBI chains and the cellulose/silica nanoparticles. Commercially available silica nanoparticles were modified with biodegradable nanocellolose through ultrasonic irradiation technique. Transmission electron microscopy (TEM) analyses showed that the cellulose/silica composites were well dispersed in the s-PBI matrix on a nanometer scale...
March 2018: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/29137784/surface-modified-sio2-nanoparticles-by-thiamine-and-ultrasonication-synthesis-of-pcl-sio2-vb1-ncs-morphology-thermal-mechanical-and-bioactivity-investigations
#19
Shadpour Mallakpour, Zahra Khani
The influence of silica (SiO2) nanoparticles (NPs) on the properties of polycaprolactone (PCL) was investigated. Due to the intense tendency of SiO2 NPs to aggregation and their high surface energy, the surface of SiO2 NPs was treatment via Vitamin B1 (VB1) as a biosafe coupling agent. Novel PCL/SiO2-VB1 nanocomposites (NC) films by variety of percentage of SiO2-VB1 NPs were prepared under ultrasonic irradiation as an eco-friendly and fast procedure following by casting method. Fourier transform infrared spectroscopy and energy dispersive X-ray analysis exposed the presence of SiO2 NPs into the polymer matrix...
March 2018: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/29137713/trpv1-a-potential-therapeutic-target-in-type-2-diabetes-and-comorbidities
#20
REVIEW
Dorte X Gram, Jens J Holst, Arpad Szallasi
With an estimated 422 million affected patients worldwide in 2016, type 2 diabetes (T2D) has reached pandemic proportions and represents a major unmet medical need. T2D is a polygenic disease with a chronic, low-grade inflammatory component. Second-generation transient receptor potential vanilloid-1 (TRPV1) antagonists are potent anti-inflammatory agents with proven clinical safety. In rodent models of T2D, TRPV1 blockade was shown to halt disease progression and improve glucose metabolism. Thus, we propose that TRPV1 antagonists merit further study as novel therapeutic approaches to potentially treat T2D and its comorbidities...
November 2017: Trends in Molecular Medicine
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