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https://www.readbyqxmd.com/read/28441580/the-computer-aided-discovery-of-novel-family-of-the-5-ht6-serotonin-receptor-ligands-among-derivatives-of-4-benzyl-1-3-5-triazine
#1
Dorota Łażewska, Rafał Kurczab, Małgorzata Więcek, Katarzyna Kamińska, Grzegorz Satała, Magdalena Jastrzębska-Więsek, Anna Partyka, Andrzej J Bojarski, Anna Wesołowska, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
The work describes a discovery of new chemical family of potent ligands for the 5-HT6 serotonin receptors. During the search for new histamine H4 receptor antagonists among 1,3,5-triazine derivatives, compound 2 (4-benzyl-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) was found. Compound 2, weakly active for the H4 receptor but fitted in 3/4 of pharmacophore features of the 5-HT6R ligand, occurred to be a moderate 5-HT6R agent, useful as a lead structure for further modifications. A series of new derivatives (3-19) of the lead 2 was synthesized, evaluated in the radioligand binding assay (RBA) and explored in comprehensive molecular modelling, including both pharmacophore- and structure-based approaches with docking to the homology model of 5-HT6R...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28441372/assessing-response-of-high-grade-gliomas-to-immune-checkpoint-inhibitors
#2
Solmaz Sahebjam, Dexter G Stallworth, Sepideh Mokhtari, Nam D Tran, John A Arrington
BACKGROUND: Immunotherapeutic agents, especially checkpoint inhibitors, have emerged as the mainstay of therapy for several solid and hematological malignancies. These therapies are under investigation for the treatment of high-grade gliomas and brain metastases. METHODS: This article reviews the unique challenges encountered when evaluating changes on magnetic resonance imaging (MRI) of glioblastomas seen in response to immunotherapy and checkpoint inhibitors and how to effectively incorporate MRI findings into the response assessment of high-grade gliomas to these emerging therapies...
April 2017: Cancer Control: Journal of the Moffitt Cancer Center
https://www.readbyqxmd.com/read/28441350/synthesis-and-bioactivity-evaluation-of-novel-2-salicyloylbenzofurans-as-antibacterial-agents
#3
Phuong-Thuy T Phan, Thu-Trang T Nguyen, Hong-Nhung T Nguyen, Bao-Khanh N Le, Thao T Vu, Dong C Tran, Tuan-Anh N Pham
In order to discover new antibacterial agents, series of 2-salicyloylbenzofuran derivatives were designed, synthesized and evaluated for their antibacterial activities against three Gram-(+) strains (methicillin-sensitive Staphylococcus aureus (MSSA) ATCC 29213, methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300, and Streptococcus faecalis (S. faecalis) ATCC 29212) and one Gram-(-) strain (Escherichia coli (E. coli) ATCC 25922). The 2-salicyloylbenzofuran heterocycles were generated by Rap-Stoermer condensation of salicylaldehydes with phenacyl bromides and then converted to diverse O-ether derivatives by Williamson synthesis...
April 25, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28441138/employing-rna-viruses-to-fight-cancer-novel-insights-into-oncolytic-virotherapy
#4
Dörthe Masemann, Yvonne Boergeling, Stephan Ludwig
Within the last decades, viruses that specifically target tumor cells have emerged as novel therapeutic agents against cancer. These viruses do not only act via their cell-lytic properties, but also harbor immunostimulatory features to re-direct the tumor-microenvironment and stimulate tumor-directed immune responses. Furthermore, oncolytic viruses are considered to be superior to classical cancer therapies due to higher selectivity towards tumor cell destruction and, consequently, less collateral damage of non-transformed healthy tissue...
April 25, 2017: Biological Chemistry
https://www.readbyqxmd.com/read/28441015/-bottom-up-construction-of-multi-polyprodrug-arm-hyperbranched-amphiphiles-for-cancer-therapy
#5
Pei Sun, Dong Chen, Hongping Deng, Nan Wang, Ping Huang, Xin Jin, Xinyuan Zhu
Despite of great advantages of polymer-drug conjugates (PDC) in cancer therapy, the controlling of drug loading site and degree via a facile approach remains a great challenge. Herein, combination the controllability of the "bottom-up" strategy and the stability of multi-arm hyperbranched amphiphiles, we have developed a novel multi-polyprodrug-arm hyperbranched amphiphiles (H40-star-(PHCPTMA-b-PMPC), hPCM) via reversible addition-fragmentation chain transfer (RAFT) polymerization for cancer therapy. The hPCM was constructed via two-step polymerization of an acid-labile prodrug monomer and a zwitterionic monomer, respectively...
April 25, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28440835/the-generation-of-compartmentalized-nanoparticles-containing-sirna-and-cisplatin-using-a-multi-needle-electrohydrodynamic-strategy
#6
Maria F Pina, Wai Lau, Kathrin Scherer, Maryam Parhizkar, Mohan Edirisinghe, Duncan Craig
This study outlines a novel manufacturing technique for the generation of compartmentalized trilayered nanoparticles loaded with an anti-cancer agent and siRNA as a platform for the combination treatment of cancers. More specifically, we describe the use of a multi-needle electrohydrodynamic approach to produce nanoparticles with high size specificity and scalable output, while allowing suitable environments for each therapeutic agent. The inner polylactic-glycolic-acid (PLGA) layer was loaded with cisplatin while the middle chitosan layer was loaded with siRNA...
April 25, 2017: Nanoscale
https://www.readbyqxmd.com/read/28440493/the-extracellular-signal-regulated-kinase-1-2-pathway-in-neurological-diseases-a-potential-therapeutic-target-review
#7
Jing Sun, Guangxian Nan
Signaling pathways are critical modulators of a variety of physiological and pathological processes, and the abnormal activation of some signaling pathways can contribute to disease progression in various conditions. As a result, signaling pathways have emerged as an important tool through which the occurrence and development of diseases can be studied, which may then lead to the development of novel drugs. Accumulating evidence supports a key role for extracellular signal-regulated kinase 1/2 (ERK1/2) signaling in the embryonic development of the central nervous system (CNS) and in the regulation of adult brain function...
April 21, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28440491/txnip-overexpression-suppresses-proliferation-and-induces-apoptosis-in-smmc7221-cells-through-ros-generation-and-mapk-pathway-activation
#8
Jian Li, Zhongyi Yue, Wancheng Xiong, Peisheng Sun, Kun You, Jianguo Wang
Thioredoxin binding protein (thioredoxin-interacting protein, TXNIP), known as vitamin D3 increase protein 1, has been identified as a tumor suppressor in various cancers such as pancreatic, breast, lung and thyroid cancer. However, the role of TXNIP in hepatocellular carcinoma cell proliferation and apoptosis remains unknown. In this study, we first used qRT-PCR, western blotting and immunohistochemistry to compare the expression of TXNIP between hepatocellular carcinoma tissues and tumor-adjacent normal liver tissues...
April 18, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28440463/livin-enhances-chemoresistance-in-head-and-neck-squamous-cell-carcinoma
#9
Tae Mi Yoon, Sun-Ae Kim, Dong Hoon Lee, Joon Kyoo Lee, Young-Lan Park, Kyung-Hwa Lee, Ik-Joo Chung, Young-Eun Joo, Sang Chul Lim
The responsiveness of head and neck squamous cell carcinoma (HNSCC) to chemotherapy widely affects prognosis. Overcoming chemoresistance is necessary to improve prognoses in patients with advanced HNSCC. Evasion of apoptosis by cancer cells is a major cause of chemoresistance. Livin, a member of the human inhibitors of apoptosis protein family, is highly expressed in various human cancer tissues and is associated with tumor progression and poor prognosis in human cancers. The aim of the present study was to evaluate the role of Livin in the susceptibility to popularly used chemotherapeutic drugs such as cisplatin, 5-fluorouracil (FU) and docetaxel in human HNSCC cell lines (SNU1041, PCI1 and PCI50 cells)...
April 19, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28440435/mitochondria-targeting-and-near-infrared-fluorescence-imaging-of-a-novel-heptamethine-cyanine-anticancer-agent
#10
Juewei Ning, Baozhan Huang, Zeliang Wei, Wen'en Li, Huajie Zheng, Limei Ma, Zhihua Xing, Hai Niu, Wen Huang
The future of personalized cancer treatments relies on the development of functional agents that have tumor-targeted anticancer activities and can be detected in tumors using imaging. However, application of these functional agents in the clinic has been limited due to inefficient drug delivery, low specificity for tumor imaging, development of drug resistance, low signal-to-noise ratio and safety concerns regarding potential toxicity. Currently, the most common strategy to develop these functional agents is to conjugate therapeutic agents with the appropriate fluorescent probe...
April 10, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28440397/hypermethylation-of-mirna-589-promoter-leads-to-upregulation-of-hdac5-which-promotes-malignancy-in-non-small-cell-lung-cancer
#11
Changhong Liu, Desheng Lv, Mo Li, Xuefei Zhang, Ge Sun, Yu Bai, Dongmin Chang
Histone deacetylases (HDACs) are crucial for regulating chromatin activity, which plays a critical role in cell proliferation, differentiation, and apoptosis of various cancers. Therefore, HDAC inhibitors have been applied as effective therapeutic agents for cancer treatment. However, the expression profiles and regulatory mechanisms of histone deacetylases in lung cancer are not well understood. In the present study, aberrant high levels of HDAC5 were observed in non-small cell lung cancer (NSCLC) and further analysis indicated a negative relationship between HDAC5 and a tumor suppressor, miR‑589‑5p, in NSCLC specimens...
April 20, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28440203/antimicrobial-biofilm-inhibitory-and-anti-infective-activity-of-metallic-nanoparticles-against-multi-drug-resistant-mrsa-and-pseudomonas-aeruginosa-pa01
#12
Jamuna Bai Ashwathanarayan, Ravishankar Rai Vittal
BACKGROUND: The emergence of drug resistant pathogens is a major concern to the scientific community. Novel approaches such as the use of functionalized nanomaterials with antimicrobial activity is required to treat infectious diseases. OBJECTIVE: In the present study, the metallic nanoparticles (iron, gold, zinc oxide and copper oxide) were evaluated for the antimicrobial, biofilm inhibitory and anti-infective activity against human pathogens methicillin resistant Staphylococcus aureus and Pseudomonas aeruginosa PA01...
April 24, 2017: Pharmaceutical Nanotechnology
https://www.readbyqxmd.com/read/28440196/mir-126-as-a-therapeutic-agent-for-diabetes-mellitus
#13
Elham Pishavar, Javad Behravan
Diabetes mellitus (DM) is a metabolic disorder which is characterized by inappropriate hyperglycemia. It is becoming an epidemic disease in developing countries. Diabetic patients are frequently afflicted with a vascular dysfunction and wound healing defect. In spite of intense investigations, over the past 2-3 decades, optimal treatment options and related mechanisms are still unclear. MicroRNAs (miRNAs) are small noncoding RNAs considered as regulators of a vast number of biological processes including endothelial cell function controlling molecular signaling pathways in diabetic pathogenesis...
April 24, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28440057/overcoming-linsitinib-intrinsic-resistance-through-inhibition-of-nuclear-factor-%C3%AE%C2%BAb-signaling-in-esophageal-squamous-cell-carcinoma
#14
Junzhou Wu, Kaiyan Chen, Fanrong Zhang, Jiaoyue Jin, Nan Zhang, Dan Li, Lisha Ying, Wei Chen, Herbert Yu, Weimin Mao, Dan Su
The aim of this study is to evaluate the efficacy of insulin-like growth factor 1 receptor (IGF-1R) inhibitor Linsitinib, in esophageal squamous cell carcinoma (ESCC), and to characterize special biomarker to screen Linsitinib-sensitive patients as well as explore the molecular-resistant mechanism to Linsitinib in ESCC. Our study evaluated the sensitivity of insulin-like growth factor 1 receptor (IGF-1R) inhibitor, Linsitinib in ESCC cells with MTT assay. After Linsitinib treatment, the expressions of downstream signaling molecules and apoptosis pathways were measured by western blot...
April 24, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28439883/an-update-for-richter-syndrome-new-directions-and-developments
#15
REVIEW
Toby A Eyre, Anna Schuh
High-grade transformation of chronic lymphocytic leukaemia [Richter syndrome (RS)] is rare and represents a unique and uncommon clinical challenge. Clonally related diffuse large B cell type RS is a chemotherapy-resistant and devastating disease. Patients are typically elderly, immunosuppressed and present with a rapidly deteriorating performance status. Historical outcomes suggest a median overall survival of approximately 8 months. RS remains is an area of high unmet clinical need. The molecular profile and treatment needs of patients are likely to change over time with the advent of novel B cell receptor inhibitors, monoclonal antibodies and BH3 mimetics...
April 25, 2017: British Journal of Haematology
https://www.readbyqxmd.com/read/28439501/the-cell-biology-of-the-trichosporon-host-interaction
#16
REVIEW
Cláudio Duarte-Oliveira, Fernando Rodrigues, Samuel M Gonçalves, Gustavo H Goldman, Agostinho Carvalho, Cristina Cunha
Fungi of the genus Trichosporon are increasingly recognized as causative agents of superficial and invasive fungal disease in humans. Although most species are considered commensals of the human skin and gastrointestinal tract, these basidiomycetes are an increasing cause of fungal disease among immunocompromised hosts, such as hematological patients and solid organ transplant recipients. The initiation of commensal or pathogenic programs by Trichosporon spp. involves the adaptation to the host microenvironment and its immune system...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28439126/necrotrophic-growth-of-periodontopathogens-is-a-novel-virulence-factor-in-oral-biofilms
#17
Esteban Rodriguez Herrero, Nico Boon, Martine Pauwels, Kristel Bernaerts, Vera Slomka, Marc Quirynen, Wim Teughels
The oral use of antimicrobial agents embedded in toothpastes and mouth rinses results in an oral microbial massacre with high amounts of dead bacteria in close proximity to few surviving bacteria. It was hypothesized that this provides the surviving pathogenic bacteria a large amount of dead microbial biomass as a nutritional source for growth (necrotrophy). This study demonstrated the necrotrophic growth of periodontal pathogens in the presence of different dead oral species. In addition, the presence of dead bacteria resulted in an outgrowth of several periodontal pathogens in complex multi-species biofilms...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28439081/long-lasting-neutralization-of-c5-by-sky59-a-novel-recycling-antibody-is-a-potential-therapy-for-complement-mediated-diseases
#18
Taku Fukuzawa, Zenjiro Sampei, Kenta Haraya, Yoshinao Ruike, Meiri Shida-Kawazoe, Yuichiro Shimizu, Siok Wan Gan, Machiko Irie, Yoshinori Tsuboi, Hitoshi Tai, Tetsushi Sakiyama, Akihisa Sakamoto, Shinya Ishii, Atsuhiko Maeda, Yuki Iwayanagi, Norihito Shibahara, Mitsuko Shibuya, Genki Nakamura, Takeru Nambu, Akira Hayasaka, Futa Mimoto, Yuu Okura, Yuji Hori, Kiyoshi Habu, Manabu Wada, Takaaki Miura, Tatsuhiko Tachibana, Kiyofumi Honda, Hiroyuki Tsunoda, Takehisa Kitazawa, Yoshiki Kawabe, Tomoyuki Igawa, Kunihiro Hattori, Junichi Nezu
Dysregulation of the complement system is linked to the pathogenesis of a variety of hematological disorders. Eculizumab, an anti-complement C5 monoclonal antibody, is the current standard of care for paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS). However, because of high levels of C5 in plasma, eculizumab has to be administered biweekly by intravenous infusion. By applying recycling technology through pH-dependent binding to C5, we generated a novel humanized antibody against C5, SKY59, which has long-lasting neutralization of C5...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28438936/demonstrating-the-protective-efficacy-of-the-novel-fluoroquinolone-finafloxacin-against-an-inhalational-exposure-to-burkholderia-pseudomallei
#19
Kay B Barnes, Karleigh A Hamblin, Mark I Richards, Thomas R Laws, Andreas Vente, Helen S Atkins, Sarah V Harding
Burkholderia pseudomallei is the causative agent of melioidosis, a serious disease endemic in South East Asia and Northern Australia. Antibiotic treatment is lengthy and relapse often occurs. Finafloxacin is a novel fluoroquinolone with increased antibacterial activity in acidic conditions in contrast to other fluoroquinolones which demonstrate reduced activity at lower pH. Therefore finafloxacin may have improved efficacy against B. pseudomallei, which can survive within host cells where the local pH is acidic...
April 24, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28438931/identification-of-antifungal-h-atpase-inhibitors-with-effect-on-the-plasma-membrane-potential
#20
Lasse Kjellerup, Sandra Gordon, Karen O'Hanlon Cohrt, William Dalby Brown, Anja Thoe Fuglsang, Anne-Marie Lund Winther
The plasma membrane H(+)-ATPase (Pma1) is an essential fungal protein and a proposed target for new antifungal medications. A small-molecule library containing ∼191,000 commercially available compounds was screened for inhibition of S. cerevisiae plasma membranes containing Pma1. The overall hit rate was 0.2 %, corresponding to 407 compounds.These hit compounds were further evaluated for ATPase selectivity and broad spectrum antifungal activity. Following this work, one Pma1 inhibitor series based on compound 14 and analogs, was selected for further evaluation...
April 24, 2017: Antimicrobial Agents and Chemotherapy
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