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Current Medicinal Chemistry

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https://www.readbyqxmd.com/read/28093986/antimicrobial-polymers-mimicking-amino-acid-functionality-sequence-control-and-three-dimensional-structure-of-host-defense-peptides
#1
Matthias Hartlieb, Elizabeth G L Williams, Agnès Kuroki, Sébastien Perrier, Katherine E S Locock
Peptides and proteins control and direct all aspects of cellular function and communication. Having been honed by nature for millions of years, they also typically display an unsurpassed specificity for their biological targets. This underlies the continued focus on peptides as promising drug candidates. However, the development of peptides into viable drugs is hampered by their lack of chemical and pharmacokinetic stability and the cost of large scale production. One method to overcome such hindrances is to develop polymer systems that are able to retain the important structural features of these biologically active peptides, while being cheaper and easier to produce and manipulate chemically...
January 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28093985/ketogenic-diet-and-other-dietary-intervention-strategies-in-the-treatment-of-cancer
#2
Matteo Vergati, Eriseld Krasniqi, Girolamo Del Monte, Silvia Riondino, Doriana Vallone, Fiorella Guadagni, Patrizia Ferroni, Mario Roselli
Pre-clinical and clinical studies have investigated the role of a dysregulated metabolism in the sustainability of tumor initiation and progression. One of the most familiar metabolic alterations encountered in several types of cancers is the upregulation of glycolysis, which is also maintained in conditions of normal oxygen tension (aerobic glycolysis, Warburg effect) while oxidative phosphorylation is apparently reduced. As a result, cancer cells convert most incoming glucose to lactate. Although more rapid, adenosine triphosphate (ATP) production by glycolysis is less efficient in terms of ATP generated per unit of glucose consumed than oxidative phosphorylation...
January 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28093984/polymer-conjugated-gold-nanoparticles-in-biomedical-applications
#3
Stanley Anniebell, Subash C B Gopinath
Research interests on the properties of polymer conjugated gold nanoparticle (GNP) in biomedicine are rapidly raised because of the extensive proof of their unique properties. In the field of biomedicine, GNPs are widely used because of their inertness and low levels of cytotoxicity. Therefore, when exposed to cells, they are less prone to exert damaging effects. GNPs are capable of being functionalized as desired and are ideal as it does not encourage undesired side reactions that might counter react with the initial intention of the functionalization...
January 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28093983/an-approach-towards-structure-based-antimicrobial-peptide-design-for-use-in-development-of-transgenic-plants-a-strategy-for-plant-disease-management
#4
Humaira Ilyas, Aritreyee Datta, Anirban Bhunia
Antimicrobial peptides (AMPs), also known as host defense peptides (HDPs), are ubiquitous and vital components of innate defense response that present themselves as potential candidates for drug design, aimed to control plant and animal diseases. Though their application for plant disease management has long been studied with natural AMPs, cytotoxicity and stability related shortcomings for the development of transgenic plants limits their usage. Newer technologies like molecular modelling, NMR spectroscopy and combinatorial chemistry allow screening for potent candidates and provide new avenues for the generation of rationally designed synthetic AMPs with multiple biological functions...
January 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28093982/pde7-selective-and-dual-inhibitors-advances-in-chemical-and-biological-research
#5
Agnieszka Jankowska, Artur Świerczek, Grażyna Chłoń-Rzepa, Maciej Pawłowski, Elżbieta Wyska
Phosphodiesterase 7 (PDE7) is an intracellular enzyme that specifically hydrolyses the second messenger, cyclic-3',5'-adenosine monophosphate (cAMP), into inactive non-cyclic nucleotide, 5'-AMP. To date, many structurally diverse compounds with PDE7 inhibitory properties have been described, including selective PDE7 inhibitors, dual PDE4/PDE7, PDE7/PDE8, and PDE7/GSK-3 inhibitors, and non-selective PDE inhibitors with high affinity for PDE7. Inhibitors of PDE7 provided beneficial effects in animal models of inflammatory and neurological disorders, including Alzheimer's disease, Parkinson's disease, multiple sclerosis, and many others...
16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28093981/chemical-and-biological-aspects-of-the-natural-1-4-benzoquinone-embelin-and-its-semi-synthetic-derivatives
#6
Priti Singh Shuveksh, Subhash Padhye, Rainer Schobert, Bernhard Biersack
BACKGROUND: Like the impressive biological properties of embelin, its chemical aspects have raised the interest of scientists in the field as well. A detailed understanding of the chemistry of embelin is necessary to fully exploit it medicinally. METHODS: Search for embelin isolation and its chemical modifications was carried out using web-based literature searching tools such as Pubmed and Scifinder. Pertinent literature is covered up to 2016. Structures of bioactive embelin derivatives are provided...
January 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28088905/update-on-recent-developments-in-small-molecular-hiv-1-rnase-h-inhibitors-2013-2016-opportunities-and-challenges
#7
Xueshun Wang, Ping Gao, Luis Menéndez-Arias, Xinyong Liu, Peng Zhan
Combinations of antiretroviral drugs are successfully used to treat HIV-infected patients. However, drug resistance is a major problem that makes discovery of new antiretroviral drugs an ongoing priority. The ribonuclease H (RNase H) activity of the HIV-1 reverse transcriptase catalyzes the selective hydrolysis of the RNA strand of RNA:DNA heteroduplex replication intermediates, and represents an attractive unexploited target for drug development. This review reports on recent progress in the characterization of HIV-1 RNase H inhibitors from 2013 to 2016, describing their chemical structures, structure-activity relationship and binding modes...
January 13, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28088904/fc-fusion-proteins-in-therapy-an-updated-view
#8
Reza Jafari, Naime Majidi Zolbanin, Houshang Rafatpanah, Jafar Majidi, Tohid Kazemi
Fc-fusion proteins are composed of Fc region of IgG antibody (Hinge-CH2-CH3) and a desired linked protein. Fc region of Fc-fusion proteins can bind to neonatal Fc receptor (FcRn) thereby rescuing it from degradation. The first therapeutic Fc-fusion protein was introduced for treatment of AIDS. The molecular designing is the first stage in production of Fc-fusion proteins. The amino acid residues in the Fc region and linked protein are very important in the bioactivity and affinity of the fusion proteins. Although, therapeutic monoclonal antibodies are the top selling biologics but the application of therapeutic Fc-fusion proteins in clinic is in progress and among of these medications Etanercept is the most effective in therapy...
January 13, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28088903/antitubercular-marine-natural-products
#9
Lishu Wang, Jungfeng Wang, Juan Liu, Yonghong Liu
Due to the importance of nature as a source of new drug candidates, the purpose of this article is to emphasize the marine natural products, which exhibit antitubercular activity, published between January 2000 and May 2016, with 138 quotation to 250 compounds obtained from marine resources. These metabolites are organized by chemical constitution and named as simple alkyl lipids derivatives, aromatics derivatives, peptides, alkaloids, terpenoids, steroids, macrolides, and polycyclic polyketides.
January 13, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28088907/tofacitinib-an-oral-janus-kinase-inhibitor-perspectives-in-dermatology
#10
Kresimir Kostovic, Sandra Jerkovic Gulin, Zrinka Bukvic Mokos, Romana Ceovic
BACKGROUND: Tofacitinib (formerly known as CP-690,550, CP690550, tasocitinib), a novel selective immunosuppressant, is a small molecule classified as Janus kinase inhibitor. The aim of this review article is to present updated data summary on the tofacitinib in the field of dermatology. METHOD: We undertook a structured search of bibliographic databases for peer-reviewed scientific articles, including review articles, original research articles as well as case report articles based on inclusion/exclusion criteria...
January 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28088906/epratuzumab-and-blinatumomab-as-therapeutic-antibodies-for-treatment-of-pediatric-acute-lymphoblastic-leukemia-current-status-and-future-perspectives
#11
Raffaella Franca, Diego Favretto, Marilena Granzotto, Giuliana Decorti, Marco Rabusin, Gabriele Stocco
BACKGROUND: More than 85% of children affected by acute lymphoblastic leukemia (ALL) are successfully treated; however relapse remains a remarkable clinical concern, with 50-60% of relapsing patients facing a fatal outcome. Management of relapsed patients includes standardized intensive risk-adapted regimens based on conventional drugs, and hematopoietic stem cells transplantation for patients with unfavourable features. Biological drugs, in particular the monoclonal antibody epratuzumab and the bi-functional recombinant single chain peptide blinatumomab, have been recently recognized as novel potential agents to be integrated in salvage ALL therapy to further improve rescue outcome...
January 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28078998/lipoprotein-a-management-pharmacological-and-apheretic-treatment
#12
Ruth Hanssen, Ioanna Gouni-Berthold
Lipoprotein (a) [Lp(a)] is an low-density lipoprotein (LDL)-like particle with an additional apolipoprotein, apolipoprotein (a), [apo(a)] attached to apolipoprotein B. Recent epidemiologic and Mendelian randomization studies have provided evidence that Lp(a) is causally related to the pathogenesis of atherosclerosis and cardiovascular disease (CVD). The risk association between Lp(a) concentrations and CVD is still controversial but seems to be continuous and without an obvious threshold Lp(a) level. Circulating concentrations of Lp(a) are genetically determined; desirable levels are amplt; 50 mg/dl...
12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28078997/lipoprotein-a-and-cardiovascular-risk-the-show-must-go-on
#13
Niki Katsiki, Khalid Al-Rasadi, Dimitri P Mikhailidis
Lipoprotein (a) [Lp(a)] is an independent but moderate, predictor for coronary heart disease (CHD) prevalence and severity. Several established and emerging cardiovascular (CV) risk factors including age, gender, ethnicity, smoking, dyslipidemia, hypertension, obesity, type 2 diabetes mellitus, alcohol consumption, arterial stiffness and hyperuricemia have been linked to Lp(a) metabolism. Apart from CHD, Lp(a) has been also associated with non-cardiac vascular diseases and diseases associated with increased CV risk such as chronic kidney disease, metabolic syndrome, non-alcoholic fatty liver disease, erectile dysfunction, obstructive sleep apnea syndrome, inflammatory bowel diseases and human immunodeficiency virus infection...
January 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28078996/kinase-inhibitors-in-multitargeted-cancer-therapy
#14
Carla Gentile, Annamaria Martorana, Antonino Lauria, Riccardo Bonsignore
The old-fashioned anticancer approaches, aiming in arresting cancer cell proliferation interfering with non-specific targets (e.g. DNA), have been replaced, in the last decades, by more specific target oriented ones. Nonetheless, single-target approaches have not always led to optimal outcomes because, for its complexity, cancer needs to be tackled at various levels by modulation of several targets. Although at present, combinations of individual single-target drugs represent the most clinically practiced therapeutic approaches, the modulation of multiple proteins by a single drug, in accordance with the polypharmacological strategy, has become more and more appealing...
January 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28078995/sphingolipids-in-genetic-and-acquired-forms-of-chronic-kidney-diseases
#15
Norishi Ueda
Sphingolipids (SLs) regulate apoptosis, proliferation, and stress response. SLs, including ceramide, glycosphingolipids (glucosylceramide, lactosylceramide, and gangliosides) and sphingosine-1-phosphate (S1P), play a role in the pathogenesis and progression of genetic (lysosomal storage disease, congenital nephrotic syndrome and polycystic kidney disease) and non-genetic forms of chronic kidney diseases (CKDs). SLs metabolism defects promote complications (cardiovascular events, etc.) via oxidant stress in CKDs...
January 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28078994/modulation-of-tumour-related-signaling-pathways-by-natural-pentacyclic-triterpenoids-and-their-semisynthetic-derivatives
#16
Andrey V Markov, Evgeniya B Logashenko, Marina A Zenkova
Pentacyclic triterpenoids are a large class of natural isoprenoids that are widely biosynthesized in higher plants. These compounds are potent anticancer agents that exhibit antiproliferative, antiangiogenic, antiinflammatory and proapoptotic activities. Although their effects on multiple pathways have been reported, unifying mechanisms of action have not yet been established. To date, a huge number of semisynthetic derivatives have been synthesized in different laboratories on the basis of triterpenoid scaffolds, and many have been assayed for their biological activities...
January 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28079003/colorectal-cancer-chemotherapy-the-evolution-of-treatment-and-new-approaches
#17
Rachel M McQuade, Vanesa Stojanovska, Joel C Bornstein, Kulmira Nurgali
Colorectal cancer (CRC) is one the greatest contributors to cancer related mortality. Although 5 year survival rate for patients at the early stage of CRC (stages I and II) is above 60%, more than 50% of patients are diagnosed at or beyond stage III when distant metastasis has already occurred, in which case 5 year survival rate drops to 10%. Chemotherapeutic intervention coupled with surgery is the backbone of metastatic CRC treatment and the only means of enhanced survival. For decades following its discovery, an antimetabolite 5-fluorouracil (5-FU) was the only chemotherapeutic agent available to successfully improve 12 month survival in CRC patients...
January 11, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28079002/neurotoxicity-associated-with-platinum-based-anti-cancer-agents-what-are-the-implications-of-copper-transporters
#18
Vanesa Stojanovska, Rachel McQuade, Emma Rybalka, Kulmira Nurgali
Platinum-based anti-cancer agents, which include cisplatin, carboplatin and oxaliplatin, are an important class of drugs used in clinical setting to treat a variety of cancers. The cytotoxic efficacy of these drugs is mediated by the formation of interstrand and intrastrand crosslinks, or platinum adducts on nuclear DNA. There is also evidence demonstrating that mitochondrial DNA is susceptible to platinum-adduct damage in dorsal root ganglia neurons. Although all platinum-based agents form similar DNA adducts, they are quite different in terms of activation, systemic toxicity and tolerance...
January 11, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28079001/application-of-organic-monolithic-materials-to-enantioseparation-in-capillary-separation-techniques
#19
Enrique Javier Carrasco-Correa, Ernesto Francisco Simó-Alfonso, Guillermo Ramis-Ramos, Jose Manuel Herero-Martinez
This review article is primarily focused on the state-of-the-art of enantioseparations on organic monolithic materials. The article gives an overview of the chiral stationary phases and its application in capillary electrochromatography (CEC), and capillary- and nano-liquid chromatography (cLC and nLC). Since thousands of publications have been emerged from 2000's and citing all these papers would extend the scope of this review, in this review, recent developments (from 2006 to 2016) last 10 years will be mentioned...
11, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28079000/application-of-monoterpenoids-and-their-derivatives-for-treatment-of-neurodegenerative-disorders
#20
Konstantin P Volcho, Sergey S Laev, Ghulam Md Ashraf, Gjumrakch Aliev, Nariman F Salakhutdinov
Neurodegenerative disorders (NDDs) like Alzheimer disease, Parkinson's disease and Huntington's disease are a heterogeneous group of disorders with the progressive and severe loss of neurons. There are no full proof cures for these diseases, and only medicines are available that can alleviate some of the symptoms. Developing effective treatments for the NDDs is a difficult but necessary task. Hence, the investigation of monoterpenoids which modulate targets applicable to many NDDs is highly relevant. Many monoterpenoids have demonstrated promising neuroprotective activity mediated by various systems...
11, 2017: Current Medicinal Chemistry
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