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Future Medicinal Chemistry

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https://www.readbyqxmd.com/read/28332860/corrigendum
#1
(no author information available yet)
No abstract text is available yet for this article.
March 23, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28211294/hemopred-a-web-server-for-predicting-the-hemolytic-activity-of-peptides
#2
Thet Su Win, Aijaz Ahmad Malik, Virapong Prachayasittikul, Jarl E S Wikberg, Chanin Nantasenamat, Watshara Shoombuatong
AIM: Toxicity arising from hemolytic activity of peptides hinders its further progress as drug candidates. MATERIALS & METHODS: This study describes a sequence-based predictor based on a random forest classifier using amino acid composition, dipeptide composition and physicochemical descriptors (named HemoPred). RESULTS: This approach could outperform previously reported method and typical classification methods (e.g., support vector machine and decision tree) verified by fivefold cross-validation and external validation with accuracy and Matthews correlation coefficient in excess of 95% and 0...
February 17, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28207349/disarming-pathogens-benefits-and-challenges-of-antimicrobials-that-target-bacterial-virulence-instead-of-growth-and-viability
#3
Makrina Totsika
No abstract text is available yet for this article.
February 16, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28207290/fatty-acid-and-mineral-receptors-as-drug-targets-for-gastrointestinal-disorders
#4
Pawin Pongkorpsakol, Aekkacha Moonwiriyakit, Chatchai Muanprasat
Nutrient-sensing receptors, including fatty acid receptors (FFA1-FFA4), Ca(2+)-sensing receptors and Zn(2+)-sensing receptors, are involved in several biological processes. These receptors are abundantly expressed in the GI tract, where they have been shown to play crucial roles in regulating GI function. This review provides an overview of the GI functions of fatty acid and mineral receptors, including the regulation of gastric and enteroendocrine functions, GI motility, ion transport and cell growth. Recently, several lines of evidence have implicated these receptors as promising therapeutic targets for the treatment of GI disorders, for example, inflammatory bowel disease, colorectal cancer, metabolic syndrome and diarrheal diseases...
February 16, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28176543/targeting-autophagy-as-a-strategy-for-drug-discovery-and-therapeutic-modulation
#5
Lixia Gao, Catherine E Jauregui, Yong Teng
Autophagy is a self-protective mechanism of living cells or organisms under various stress conditions. Studies of human genetics and pathophysiology have implicated that alterations in autophagy affect the context of cellular homeostasis and disease-associated phenotypes. The molecular components of autophagy are currently being explored as new pharmacologic targets for drug development and therapeutic intervention of various diseases. Drugs that restore the normal autophagic pathways have the potential for effectively treating human disorders that depend on aberrations of autophagy...
February 8, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28176540/antitumoral-activity-of-1-2-diaminocyclohexane-derivatives-in-breast-colon-and-skin-human-cancer-cells
#6
Fátima Morales, Alberto Ramírez, Cynthia Morata-Tarifa, Saúl A Navarro, Juan A Marchal, Joaquín M Campos, Ana Conejo-García
AIM: Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities against the MCF-7, HCT-116 and A375 cancer cell lines. Cell cycle and apoptosis analyses were also carried out. Our results show that all the compounds are potent cytotoxic agents, especially against the A375 cell line...
February 8, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28176537/the-impact-of-brexit-on-british-science-also-sprach-zunderland
#7
Bernard T Golding
No abstract text is available yet for this article.
February 8, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28176536/kinase-targets-in-cns-drug-discovery
#8
Hendra Gunosewoyo, Lifang Yu, Lenka Munoz, Michael Kassiou
Originally thought to be nondruggable, kinases represent attractive drug targets for pharmaceutical companies and academia. To date, there are over 40 kinase inhibitors approved by the US FDA, with 32 of these being small molecules, in addition to the three mammalian target of rapamycin inhibitor macrolides (sirolimus, temsirolimus and everolimus). Despite the rapid development of kinase inhibitors for cancer, presently none of these agents are approved for CNS indications. This mini perspective highlights selected kinase targets for CNS disorders, of which brain-permeable small-molecule inhibitors are reported, with demonstrated preclinical proof-of-concept efficacy...
February 8, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28128024/studies-of-staphylococcus-aureus-fabi-inhibitors-fragment-based-approach-based-on-holographic-structure-activity-relationship-analyses
#9
Thales Kronenberger, Leonardo Rander Asse, Carsten Wrenger, Gustavo Henrique Goulart Trossini, Kathia Maria Honorio, Vinicius Gonçalves Maltarollo
AIM: FabI is a key enzyme in the fatty acid metabolism of Gram-positive bacteria such as Staphylococcus aureus and is an established drug target for known antibiotics such as triclosan. However, due to increasing antibacterial resistance, there is an urgent demand for new drug discovery. Recently, aminopyridine derivatives have been proposed as promising competitive inhibitors of FabI. METHODS: In the present study, holographic structure-activity relationship (HQSAR) analyses were employed for determining structural contributions of a series containing 105 FabI inhibitors...
January 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28128003/current-and-future-developments-in-the-treatment-of-virus-induced-hypercytokinemia
#10
Jonathan P Wong, Satya Viswanathan, Ming Wang, Lun-Quan Sun, Graeme C Clark, Riccardo V D'Elia
Emerging pathogenic viruses such as Ebola and Middle Eastern Respiratory Syndrome coronavirus (MERS-CoV) can cause acute infections through the evasion of the host's antiviral immune responses and by inducing the upregulation of inflammatory cytokines. This immune dysregulation, termed a cytokine storm or hypercytokinemia, is potentially fatal and is a significant underlying factor in increased mortality of infected patients. The prevalence of global outbreaks in recent years has offered opportunities to study the progression of various viral infections and have provided an improved understanding of hypercytokinemia associated with these diseases...
January 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28127995/targeting-%C3%AE-amyloid-plaques-and-oligomers-development-of-near-ir-fluorescence-imaging-probes
#11
Hongwu Liu, Jian Yang, Letian Wang, Yungen Xu, Siyuan Zhang, Jie Lv, Chongzhao Ran, Yuyan Li
Evidence indicated that shifting treatment to a presymptomatic stage may produce significant benefits to prevent/alleviate the progression of Alzheimer's disease (AD); in particular, early incorporation of noninvasive imaging and biomarker testing will be significantly beneficial for AD drug development. Based on amyloid cascade hypothesis and its revised version, both β-amyloid deposition and soluble oligomeric species could be good diagnostic biomarkers for AD. Near-IR fluorescence (NIRF) imaging, which so far is limited to animal studies, is a promising method for its incomparable advantages such as low cost, high-throughput and easy operation...
January 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28263088/active-learning-for-computational-chemogenomics
#12
Daniel Reker, Petra Schneider, Gisbert Schneider, J B Brown
AIM: Computational chemogenomics models the compound-protein interaction space, typically for drug discovery, where existing methods predominantly either incorporate increasing numbers of bioactivity samples or focus on specific subfamilies of proteins and ligands. As an alternative to modeling entire large datasets at once, active learning adaptively incorporates a minimum of informative examples for modeling, yielding compact but high quality models. Results/methodology: We assessed active learning for protein/target family-wide chemogenomic modeling by replicate experiment...
March 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28263086/the-potential-of-combi-molecules-with-dna-damaging-function-as-anticancer-agents
#13
Guohui Sun, Tengjiao Fan, Lijiao Zhao, Yue Zhou, Rugang Zhong
DNA-damaging agents, such as methylating agents, chloroethylating agents and platinum-based agents, have been extensively used as anticancer drugs. However, the side effects, high toxicity, lack of selectivity and resistance severely limit their clinical applications. In recent years, a strategy combining a DNA-damaging agent with a bioactive molecule (e.g., enzyme inhibitors) or carrier (e.g., steroid hormone and DNA intercalators) to produce a new 'combi-molecule' with improved efficacy or selectivity has been attempted to overcome these drawbacks...
March 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28263085/exploration-of-thiaheterocyclic-hhdac6-inhibitors-as-potential-antiplasmodial-agents
#14
Rob De Vreese, Carmen de Kock, Peter J Smith, Kelly Chibale, Matthias D'hooghe
AIM: The recurring resistance of the malaria parasite to many drugs compels the design of innovative chemical entities in antimalarial research. Pan-histone deacetylase inhibitors (pan-HDACis) have recently been presented in the literature as powerful novel antimalarials, although their application is hampered due to toxic side effects. This drawback might be neutralized by the deployment of isoform-selective HDACis. RESULTS: In this study, 42 thiaheterocyclic benzohydroxamic acids, 17 of them being potent and selective hHDAC6 inhibitors, were tested to investigate a possible correlation between hHDAC6 inhibition and antiplasmodial activity...
March 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28263084/the-value-of-pet-ligand-discovery-to-cns-drug-development
#15
Mark E Schmidt, José Ignacio Andrés
No abstract text is available yet for this article.
March 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28263082/drugging-the-undruggable-targeting-challenging-e3-ligases-for-personalized-medicine
#16
Carles Galdeano
No abstract text is available yet for this article.
March 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28263081/an-effective-and-potentially-safe-blood-disinfection-protocol-using-tetrapyrrolic-photosensitizers
#17
Lúcia Marciel, Luís Teles, Beatriz Moreira, Mário Pacheco, Leandro Mo Lourenço, Maria Gpms Neves, João Pc Tomé, Maria Af Faustino, Adelaide Almeida
AIM: Conventional disinfection techniques, considered safe for plasma, are usually associated with collateral damages on concentrated platelets and erythrocytes. Alternative methods are required and antimicrobial photodynamic therapy (aPDT) seems promising. In this study the effectiveness of two photosensitizers (PS), a porphyrin and a phthalocyanine, to disinfect blood products was evaluated. RESULTS: The cationic porphyrin was more effective in the photoinactivation of bacteria...
March 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28128979/studies-of-staphylococcus-aureus-fabi-inhibitors-fragment-based-approach-based-on-holographic-structure-activity-relationship-analyses
#18
Thales Kronenberger, Leonardo Rander Asse, Carsten Wrenger, Gustavo Henrique Goulart Trossini, Kathia Maria Honorio, Vinicius Gonçalves Maltarollo
AIM: FabI is a key enzyme in the fatty acid metabolism of Gram-positive bacteria such as Staphylococcus aureus and is an established drug target for known antibiotics such as triclosan. However, due to increasing antibacterial resistance, there is an urgent demand for new drug discovery. Recently, aminopyridine derivatives have been proposed as promising competitive inhibitors of FabI. METHODS: In the present study, holographic structure-activity relationship (HQSAR) analyses were employed for determining structural contributions of a series containing 105 FabI inhibitors...
January 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28111982/short-peptides-interfering-with-signaling-pathways-as-new-therapeutic-tools-for-cancer-treatment
#19
Aleksandra Ellert-Miklaszewska, Katarzyna Poleszak, Bozena Kaminska
Short peptides have many advantages, such as low molecular weight, selectivity for a specific target, organelles or cells with minimal toxicity. We describe properties of short peptides, which interfere with communication networks in tumor cells and within microenvironment of malignant gliomas, the most common brain tumors. We focus on ligand/receptor axes and intracellular signaling pathways critical for gliomagenesis that could be targeted with interfering peptides. We review structures and efficacy of organelle-specific and cell-penetrating peptides and describe diverse chemical modifications increasing proteolytic stability and protecting synthetic peptides against degradation...
January 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28111979/a-tale-of-two-glutaminases-homologous-enzymes-with-distinct-roles-in-tumorigenesis
#20
William P Katt, Michael J Lukey, Richard A Cerione
Many cancer cells exhibit an altered metabolic phenotype, in which glutamine consumption is upregulated relative to healthy cells. This metabolic reprogramming often depends upon mitochondrial glutaminase activity, which converts glutamine to glutamate, a key precursor for biosynthetic and bioenergetic processes. Two isozymes of glutaminase exist, a kidney-type (GLS) and a liver-type enzyme (GLS2 or LGA). While a majority of studies have focused on GLS, here we summarize key findings on both glutaminases, describing their structure and function, their roles in cancer and pharmacological approaches to inhibiting their activities...
January 2017: Future Medicinal Chemistry
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