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Current Topics in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28270087/heterocyclic-analogues-as-kinase-inhibitors-a-focus-review
#1
Vipin Kumar, Raj Kamal, Vikas Sharma
Role of kinase inhibitors in various diseases is well established and discovery of imatinib opens up new paradigms in kinase inhibition. Furthermore, presence of heterocyclic moiety in a kinase inhibitor seems to be essential now. However, the potential of a single heterocyclic moiety was discussed in variety of reviews but a focus review considering the potential of different heterocyclic moieties is unavailable. Based on this, we classify prospective kinase inhibitors on the basis of number of heterocyclic moieties present and summarize the prospective kinase inhibitors...
March 7, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270086/therapeutic-implications-of-superoxide-dismutase-and-its-importance-inkinase-drug-discovery
#2
Monalisa Mukherjee, Satyendra K Rajput, Deepa Suhag, Apoorv Gupta, Aarti Singh, Vipin Kumar, Adeeba Shakeel, Arun Kumar Sharma, Nameet Kaur
In recent years, several scientific investigations have reported the therapeutic implications of superoxide dismutase (SOD) against oxidative stress and -induced pathology in clinical and preclinical trials. Indeed, various kinase, molecular signaling and physiological process has altered by reactive oxygen species. In spite of the abundant available literature reports, patents, clinical trials and commercialized products, the therapeutic application of SOD as a potential drug still remains unclear. Owing to the technical challenges associated with the utilization of SOD as a drug, we revisited the structural arrangement and cellular signaling, significant association with kinase which exploring the new target sites and introduction of new formulation strategies such as gene modulation, nano-formulations and click chemistry is a prerequisite...
March 7, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28260508/nitrone-derivatives-as-therapeutics-from-chemical-modification-to-specific-targeting
#3
Grégory Durand, Burkhard Poeggeler, Marie Rosselin
Nitrones have been extensively used for the detection of transient free radicals using electron paramagnetic resonance. Since the mid-80's, nitrones have also been widely used as protective agents against oxidative stress in several biological models. Due to the high potency of nitrones, there has been extensive research on the development of derivatives with improved biological and spin trapping properties as well as enhanced intra-cellular compartmentalization. The chemical and pharmacological properties of nitrones depend mainly on the connectivity as well as on the nature and the position of the substituents on the nitrone group...
March 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28240184/from-protein-structure-to-small-molecules-recent-advances-and-applications-to-fragment-based-drug-discovery
#4
Leonardo G Ferreira, Adriano D Andricopulo
Fragment-based drug discovery (FBDD) is a broadly used strategy in structure-guided ligand design, whereby low-molecular weight hits move from lead-like to drug-like compounds. Over the past 15 years, an increasingly important role of the integration of these strategies into industrial and academic research platforms has been successfully established, allowing outstanding contributions to drug discovery. One important factor for the current prominence of FBDD is the better coverage of the chemical space provided by fragment-like libraries...
February 24, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28240183/influenza-a-virus-nucleoprotein-a-highly-conserved-multi-functional-viral-protein-as-a-hot-antiviral-drug-target
#5
Yanmei Hu, Hannah Sneyd, Raphael Dekant, Jun Wang
Prevention and treatment of influenza virus infection is an ongoing unmet medical need. Each year, thousands of deaths and millions of hospitalizations are attributed to influenza virus infection, which poses a tremendous health and economic burden to the society. Aside from the annual influenza season, influenza viruses also lead to occasional influenza pandemics as a result of emerging or re-emerging influenza strains. Influenza viruses are RNA viruses that exist in quasispecies, meaning that they have a very diverse genetic background...
February 24, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28240182/integration-of-novel-materials-and-advanced-omics-technologies-into-new-vaccine-design
#6
Wenzhen Liao, Tian-Tian Zhang, Liqian Gao, Su Seong Lee, Jie Xu, Han Zhang, Zhaogang Yang, Zhaoyu Liu, Wen Li
Designing new vaccines is one of the most challenging tasks for public health to prevent both infectious and chronic diseases. Even though many research scientists have spent great efforts in improving the specificity, sensitivity and safety of current available vaccines, there are still much space on how to effectively combine different biomaterials and technologies to design universal or personalized vaccines. Traditionally, vaccines were made based on empirical approaches designed to mimic immunity induced by natural infection...
February 24, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28240181/recent-advances-in-synthesis-and-identification-of-cyclic-peptides-for-bioapplications
#7
Yong Siang Ong, Liqian Gao, Karunakaran A Kalesh, Zhiqiang Yu, Jigang Wang, Chengcheng Liu, Yiwen Li, Hongyan Sun, Su Seong Lee
Cyclic peptides, owing to their good stability, high resistance to exo- and to some extent endo-peptidases, enhanced binding affinity and selectivity towards target biomolecules, are actively investigated as biochemical tools and therapeutic agents. In this review, we discuss various commonly utilized synthetic strategies for cyclic peptides and peptoids (peptidomimetics), their important screening methods to identify the bioactive cyclic peptides and peptoids such as combinatorial bead-based peptide library, phage display, mRNA display etc...
February 24, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28240180/structure-based-virtual-screening-approaches-in-kinase-directed-drug-discovery
#8
Dávid Bajusz, György G Ferenczy, György M Keserű
Protein kinases are one of the most targeted protein families in current drug discovery pipelines. They are implicated in many oncological, inflammatory, CNS-related and other clinical indications. Virtual screening is a computational technique with a diverse set of available tools that has been shown many times to provide novel starting points for kinase-directed drug discovery. This review starts with a concise overview of the function, structural features and inhibitory mechanisms of protein kinases. In addition to briefly reviewing practical aspects of structure-based virtual screenings, we discuss several case studies to illustrate the state of the art in the virtual screening for type I, type II, allosteric (type III-V) and covalent (type VI) kinase inhibitors...
February 24, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28240179/the-application-of-stimuli-responsive-nanocarriers-for-targeted-drug-delivery
#9
Mengxue Zhou, Kaikai Wen, Ying Bi, Huiru Lu, Jun Chen, Yi Hu, Zhifang Chai
Nanocarriers are widely used for delivering drugs to tumors and are progressing in a stable trend, because malignant tumors remain a major health burden throughout the world and effective therapeutic strategies are urgently needed. Furthermore, as an integrated platform, nanocarriers have the potential to dramatically improve cancer diagnosis, imaging, and therapy, while reducing the toxicity associated with the current approaches. Significantly, intelligent nanocarriers are the new generation of the nanocarriers, exhibiting superior tumor targeting and improved therapeutic efficacy...
February 24, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137208/c-elegans-as-model-for-drug-discovery
#10
Maria Carretero, Gregory M Solis, Michael Petrascheck
Small molecule screens using C. elegans as a model are becoming increasingly popular as the number of high-throughput methodologies has steadily increased over the years. Here we focus on the biology that underlies this increased popularity and outline the reasons that make C. elegans an attractive model for drug discovery. We discuss successful C. elegans based drug discovery projects in the literature and future challenges ahead.
January 31, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137239/targeted-theranostics-against-solid-cancer-using-metal-bond-milk-protein-and-aptamers
#11
Suman Chaudhary, Rupinder Kaur Kanwar, Jagat Rakesh Kanwar
Targeted therapeutics is a new generation therapy that can increase the efficacy of chemotherapeutic drugs, by facilitating site-specific delivery with minimum off-target effects. Amongst the targeted therapy, nucleic-acid based aptamers are increasingly gaining interest due to their small size, long shelf-life and ease in synthesis. Further, lactoferrin, a milk protein belonging to the transferrin family is now an established multi-functional iron-binding protein. Its applicability as an immunomodulator, antimicrobial and an anti-cancer agent has made this protein highly valuable...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137238/a-practical-guide-to-molecular-docking-and-homology-modelling-for-medicinal-chemists
#12
Anna E Lohning, Stephan M Levonis, Billy Williams-Noonan, Stephanie S Schweiker
Elucidating details of the relationship between molecular structure and a particular biological end point is essential for successful rationally-based drug discovery. Molecular docking is a widely accepted tool for lead identification however navigating the intricacies of the software can be daunting. Our objective was therefore to provide a step-by-step guide for those interested in incorporating contemporary basic molecular docking and homology modelling into their design strategy. Three molecular docking programs, AutoDock4, SwissDock and Surflex-Dock, were compared in the context of a case study where a set of steroidal and non-steroidal ligands were docked into the human androgen receptor (hAR) using both rigid and flexible target atoms...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137237/model-systems-for-pulmonary-infectious-diseases-paradigms-of-anthrax-and-tuberculosis
#13
Gunjan Arora, Richa Misra, Andaleeb Sajid
Robert Koch utilized animal model systems to put forward his postulates while discovering the etiological agents of anthrax and tuberculosis, Bacillus anthracis and Mycobacterium tuberculosis, respectively. After more than 130 years, we have achieved limited success towards understanding these two pestilences, which have propagated as scourge against humans. B. anthracis and M. tuberculosis are diverse organisms, which share a common evolutionary path in tropics. They adapt unique strategies to overcome unfavorable conditions and surpass the host defense mechanisms...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137236/the-use-of-the-zebrafish-model-to-aid-in-drug-discovery-and-target-validation
#14
Prusothman Yoganantharjah, Yann Gibert
The zebrafish is fast becoming a leading and prominent model organism used by researchers for developmental biology, and research in modeling human diseases in zebrafish is being undertaken at a fast pace. Many therapeutic areas, including oncology and cardiovascular diseases to name a few all have zebrafish models based on known disease mechanisms that are translatable to modes of action in humans. Many novel assays have been and are continuing to be developed to study human disease in zebrafish. Prominent methods to identify novel drug targets within the organism include, chemical mutagenesis, insertional mutagenesis and high throughput small molecule screens...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137235/calcium-dependent-protein-kinases-cdpks-key-to-malaria-eradication
#15
Kavita Kadian, Yash Gupta, Prakasha Kempaiah, Nikesh Gupta, Arun Sharma, Manmeet Rawat
The family of calcium-dependent protein kinases (CDPKs) carries a kinase domain fused to a calmodulin-like domain. The presence of protein kinases devoid of clear mammalian eukaryotic protein kinase orthologues makes them potential targets for therapeutic development. Recent studies on CDPKs have inspired an important primary regulator of calcium (intracellular Ca2+ signaling), which is extensively reported to play a critical role in various stages of the apicomplexan life cycle such as microneme secretion of adhesions, cell invasion, gamete maturation, gliding motility and egress of Plasmodium Spp...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137234/mycobacterial-dna-replication-as-a-target-for-antituberculosis-drug-discovery
#16
Renata Płocińska, Małgorzata Korycka-Machała, Przemysław Płociński, Jarosław Dziadek
Mycobacterium tuberculosis (M. tuberculosis), the causative agent of tuberculosis, is a leading infectious disease organism, causing millions of deaths each year. This serious pathogen has been greatly spread worldwide and recent years have observed an increase in the number of multi-drug resistant and totally drug resistant M. tuberculosis strains (WHO report, 2014). The danger of tuberculosis becoming an incurable disease has emphasized the need for the discovery of a new generation of antimicrobial agents...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137233/antimalarials-molecular-drug-targets-and-mechanism-of-action
#17
Angela O Achieng, Manmeet Rawat, Bernhards Ogutu, Bernard Guyah, John Michael Ong Echa, Douglas J Perkins, Prakasha Kempaiah
Despite a reduction in the global burden of malaria, the disease remains responsible for 214 million cases and 438,000 deaths annually with 88% of the mortality occurring in sub-Saharan Africa. Malaria control largely depends on effective chemotherapy. However, the historic and current emergence and spread of multi-drug resistant parasite strains provides significant challenges to malaria control and consequently, reduction of malaria-associated morbidity and mortality. Combating parasite drug resistance requires pharmacological compounds that target both known and novel metabolic pathways that are crucial for parasite survival...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137232/synthesis-properties-and-mechanism-of-action-of-new-generation-of-polycyclic-glycopeptide-antibiotics
#18
Eugenia N Olsufyeva, Anna N Tevyashova
The increased resistance of glycopeptide based antibiotics has become a serious problem for the chemotherapy of infections triggered by resistant Gram-positive bacteria. This has motivated the urgent sincere efforts to develop potent glycopeptide-based antibiotics in both academy and industry research laboratories. Understanding of the mechanism of action of natural and modified glycopeptides is considered as the basis for the rational design of compounds with valuable properties to achieve the fundamental results...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137231/insp3-signaling-in-apicomplexan-parasites
#19
Celia R S Garcia, Eduardo Alves, Pedro H S Pereira, Paula J Bartlett, Andrew P Thomas, Katsuhiko Mikoshiba, Helmut Plattner, L David Sibley
Phosphoinositides (PIs) and their derivatives are essential cellular components that form the building blocks for cell membranes and regulate numerous cell functions. Specifically, the ability to generate myo-inositol 1,4,5-trisphosphate (InsP3) via phospholipase C (PLC) dependent hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2) to InsP3 and diacylglycerol (DAG) initiates intracellular calcium signaling events representing a fundamental signaling mechanism dependent on PIs. InsP3 produced by PI turnover as a second messenger causes intracellular calcium release, especially from endoplasmic reticulum, by binding to the InsP3 receptor (InsP3R)...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137230/proteases-in-mosquito-borne-diseases-new-avenues-in-drug-development
#20
A Pant, R Pasupureddy, V Pande, S Seshadri, R Dixit, K C Pandey
Mosquito borne diseases continue to propagate and cause millions of deaths annually. They are caused either by protozoan parasites such as Plasmodium, Toxoplasma or by flaviviruses including Dengue and Zika. Among the proteome of such parasitic organisms, proteases play essential roles in events such as host invasion, hemoglobin hydrolysis, replication and immune evasion. Plasmepsin V (PMV), an endoplasmic reticulum resident aspartic protease of Plasmodium spp., is involved in the export of ~400 proteins containing the conserved Plasmodium Export Element motif (PEXEL)...
January 30, 2017: Current Topics in Medicinal Chemistry
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