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Thursday, November 10, 2016
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Thursday, November 3, 2016
Highlighted Article: Non-adenosine Nucleoside Inosine, Guanosine and Uridine as Promising Antiepileptic Drugs: a Summary of Current Literature
Non-adenosine Nucleoside Inosine, Guanosine and Uridine as Promising Antiepileptic Drugs: a Summary of Current Literature
Author(s):
Zsolt Kovacs, Katalin A. Kekesi, Gabor Juhasz, Janos Barna, Laszlo Heja, Renata Lakatos and Arpad Dobolyi Pages 1033 - 1042 ( 10 )
Abstract:
Adenosine (Ado) and some non-adenosine (non-Ado) nucleosides including inosine (Ino), guanosine (Guo) and uridine (Urd) are modulatory molecules in the central nervous system (CNS), regulating different physiological and pathophysiological processes in the brain such as sleep and epilepsy. Indeed, different drugs effective on adenosinergic system (e.g., Ado metabolism inhibitors, agonists and antagonists of Ado receptors) are being used in drug development for the treatment of epileptic disorders. Although (i) endogenous Ino, Guo and Urd showed anticonvulsant/antiepileptic effects (e.g., in quinolinic acid - induced seizures and in different epilepsy models such as hippocampal kindling models), and (ii) there is a need to generate new and more effective antiepileptic drugs for the treatment of drug-resistant epilepsies, our knowledge about antiepileptic influence of non-Ado nucleosides is far from complete. Thus, in this review article, we give a short summary of anticonvulsant/antiepileptic effects and mechanisms evoked by Ino, Guo, and Urd. Finally, we discuss some non-Ado nucleoside derivatives and their structures, which may be candidates as potential antiepileptic agents.
Keywords:
Epilepsy, guanosine, inosine, uridine.
Affiliation:
Department of Zoology, University of West Hungary, Savaria Campus, Szombathely, Karolyi Gaspar ter 4., 9700 Hungary.
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Thursday, October 27, 2016
Most Accessed Article: Review on EGFR Inhibitors: Critical Updates
Review on EGFR Inhibitors: Critical Updates
Author(s):
Davinder Singh, Bhupinder Kumar Attri, Rupinder Kaur Gill and Jitender Bariwal Pages 1134 - 1166 ( 33 )
Abstract:
Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR leads to autophosphorylation of receptor tyrosine kinase that initiates a cascade of downstream signaling pathways involved in regulating cellular proliferation, differentiation, and survival. EGFR is abnormally activated by various mechanisms like receptor overexpression, mutation, ligand-dependent receptor dimerization, ligand-independent activation and is associated with the development of variety of human cancers. EGFR inhibition is one of the key targets for cancer chemotherapy. Approval of tyrosine kinase inhibitors such as erlotinib, gefitinib, and lapatinib for the treatment of non-small cell lung cancer led to tremendous development of novel EGFR inhibitors in the last decade. Diverse class of chemical compounds from the synthetic origin has been extensively studied. This review highlights the various classes of synthetically derived molecules which have been reported in the last few years as potential EGFR and EGFR/ErbB-2 dual inhibitors. A brief synthetic methodology to access these compounds has been highlighted along with the SAR. We strongly believe that this review will provide a platform to the synthetic chemists and biologists to design and synthesize new and potent compounds that inhibit EGFR and ErbB-2.
Keywords:
Antibodies, Apoptosis, Carcinoma, EGFR, Heterocyclic, Proliferation.
Affiliation:
Satiate Resaerch & Anatech Pvt. Ltd., HSIIDC, Barwala, Panchkula-134118, Haryana, India.
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Thursday, October 20, 2016
Thursday, October 13, 2016
New Issue for Journal Mini-Reviews in Medicinal Chemistry, Volume 16 - Number 10
Contents
Mini-Reviews in Medicinal Chemistry, Volume 16 - Number 10
Editorial (Thematic Issue: Anticancer Ruthenium Complexes in Drug Discovery and Medicinal Chemistry)
, 16(10): 771Sreekanth Thota.
DOI: 10.2174/138955751610160503003405
Ruthenium Complexes: An Emerging Ground to the Development of Metallopharmaceuticals for Cancer Therapy
, 16(10): 772 - 786Mohammad Abid, Farheen Shamsi and Amir Azam.
DOI: 10.2174/1389557515666151001142012
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Development of Arene Ruthenium Antitumor Complexes
, 16(10): 787 - 795Wei Su, Zhaofeng Tang and Peiyuan Li.
DOI: 10.2174/138955751610160503003937
Arene ruthenium(II) Complexes: The Promising Chemotherapeutic Agent in Inhibiting the Proliferation, Migration and Invasion
, 16(10): 796 - 803Kangdi Zheng, Qiong Wu, Yang Ding and Wenjie Mei.
DOI: 10.2174/1389557515666151001142159
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Anticancer Activity and Modes of Action of (arene) ruthenium(II) Complexes Coordinated to C-, N-, and O-ligands
, 16(10): 804 - 814Bernhard Biersack.
DOI: 10.2174/138955751610160503004623
Novel Drugs Targeting the c-Ring of the F1FO-ATP Synthase
, 16(10): 815 - 824Alessandra Pagliarani, S. Nesci and V Ventrella.
DOI: 10.2174/1389557516666160211120955
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Synthesis and Biological Activities of Oxadiazole Derivatives: A Review
, 16(10): 825 - 845Ankur Vaidya, Shweta Jain, Priyanka Jain, Prachi Jain, Nidhi Tiwari, Roshni Jain, Rashi Jain, Abhishek K. Jain and Ram K Agrawal.
DOI: 10.2174/1389557516666160211120835
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The Development of Protein Chips for High Throughput Screening (HTS) of Chemically Labeling Small Molecular Drugs
, 16(10): 846 - 850Yingzhu Feng, Bochu Wang, Xinxin Chu, Yazhou Wang and Liancai Zhu.
DOI: 10.2174/1389557515666150511152922
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Friday, October 7, 2016
Recently Published Issue of the Journal Mini-Reviews in Medicinal Chemistry
The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines. The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
Following are the articles from the journal Mini-Reviews in Medicinal Chemistry, 15 Issue 11:
Editorial: (Thematic Issue: Vitamin D and Vitamin D Receptor in Asthma and Allergy)
Author(s): Anna Papadopoulou and Kostas N. Priftis
Article: Association of Serum Vitamin D with Asthma and Atopy in Childhood: Review of Epidemiological Observational Studies
Author(s): Ourania Kolokotroni, Nicos Middleton, Christiana Kouta, Vasilios Raftopoulos and Panayiotis K.
Article: Maternal Vitamin D Status and Development of Asthma and Allergy in Early Childhood
Author(s): Anna Papadopoulou, Evangelia Bountouvi, Vasiliki Papaevaggelou and Kostas N. Priftis
Article: Vitamin D Metabolism Genes in Asthma and Atopy
Author(s): Eva Morales, Manuel Sanchez-Solis and Luis Garcia-Marcos
Article: Vitamin D and Atopic Dermatitis
Author(s): Rosa M. Pacheco-Gonzalez, Patricia W. Garcia-Marcos and Luis Garcia-Marcos
Article: Therapeutic Effects of Vitamin D in Asthma and Allergy
Author(s): Cecilia Benetti, Pasquale Comberiati, Carlo Capristo, Attilio L. Boner and Diego G. Peroni
Article: Is Low Vitamin D Status A Risk Factor For Food Allergy? Current Evidence And Future Directions
Author(s): John Molloy, Anne-Louise Ponsonby, Katrina J. Allen, Mimi L.K. Tang, Fiona M. Collier, Alister C. Ward, Jennifer Koplin and Peter Vuillermin
Article: Vitamin-D in the Immune System: Genomic and Non-Genomic Actions
Author(s): Aikaterini I. Trochoutsou, Vaia Kloukina, Konstantinos Samitas and Georgina Xanthou
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Friday, September 30, 2016
Mini-Reviews in Medicinal Chemistry – New Issue
The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines. The scope of this journal will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.
Following are the articles from the journal Mini-Reviews in Medicinal Chemistry, Volume 15 Issue 12:
EDITORIAL (Thematic Issue): Vitamin D in Allergy and Chronic Airway Inflammation
Author(s): Anna Papadopoulou and Kostas N. Priftis
Does Vitamin D Deficiency Epidemic Parallel with Allergy and Asthma Epidemic?
Author(s): Konstantinos Douros, Ioanna Loukou, Barbara Boutopoulou and Sotirios Fouzas
Vitamin D and Cystic Fibrosis Lung Disease
Author(s): Ioanna Loukou, Barbara Boutopoulou, Sotirios Fouzas and Konstantinos Douros
Vitamin D, Breastfeeding and Food Allergy
Author(s): Sophia Tsabouri, Anna Challa, Vasilios Giapros and Nikolaos Chaliasos
Exploration of N-arylpiperazine Binding Sites of D2 Dopaminergic Receptor
Author(s): Vukic Soskic, Vladimir Sukalovic and Sladjana Kostic-Rajacic
The Medical Use of Wheatgrass: Review of the Gap Between Basic and Clinical Applications
Author(s): Gil Bar-Sela, Miri Cohen, Eran Ben-Arye and Ron Epelbaum
Main Anti-tumor Angiogenesis Agents Isolated From Chinese Herbal Medicines
Author(s): Xue Yang and Xiong-Zhi Wu
Past, Present and Future of Antiepileptic Drug Therapy – Finding a Place for Heterocyclics
Author(s): Ruhi Ali, Mohammad Ahmed Khan and Nadeem Siddiqui
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Friday, August 19, 2016
MicroRNAs Used in Combination with Anti-Cancer Treatments Can Enhance Therapy Efficacy
Author(s):
Maddalena Mognato and Lucia CelottiPages 1052-1062 (11)
Abstract:
MicroRNAs (miRNAs), a recently discovered class of small non-coding RNAs, constitute a promising approach to anti-cancer treatments when they are used in combination with other agents. MiRNAs are evolutionarily conserved non-coding RNAs that negatively regulate gene expression by binding to the complementary sequence in the 3’-untranslated region (UTR) of target genes. MiRNAs typically suppress gene expression by direct association with target transcripts, thus decreasing the expression levels of target proteins. The delivery to cells of synthetic miRNAs that mimic endogenous miRNA targeting genes involved in the DNA-Damage Response (DDR) can perturb the process, making cells more sensitive to chemotherapy or radiotherapy. This review examines how cells respond to combined therapy and it provides insights into the role of miRNAs in targeting the DDR repair pathway when they are used in combination with chemical compounds or ionizing radiation to enhance cellular sensitivity to treatments.
Keywords:
Apoptosis, Cell cycle checkpoints, DNA-Damage Response, DNA Repair, microRNAs, Tumor resistance.
Affiliation:
Department of Biology, School of Science, University of Padova, Padova, Italy.
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G4 Aptamers: Trends in Structural Design
Author(s):
Anna Varizhuk, Nikolay Ilyinsky, Igor Smirnov and Galina PozmogovaPages 1-9 (9)
Abstract:
Many potent DNA aptamers are known to contain a G-quadruplex (G4) core. Structures and applications of the majority of such aptamers have been reviewed previously. The present review focuses on the design and optimization of G4 aptamers. General features of bioactive G4s are analyzed, and the main strategies for construction of aptamers with desired properties and topologies, including modular assembly, control of an aptamer folding and some others, are outlined. Chemical modification as a method for post-SELEX G4 aptamer optimization is also discussed, and the effects of loop and core modifications are compared. Particular attention is paid to the emerging trends, such as the development of genomic G4-inspired aptamers and the combinatorial approaches which aim to find a balance between rational design and selection.
Keywords:
aptamers; chemical modification; combinatorial approaches; drug design; G-quadruplexes; structure-activity relationship
Affiliation:
Department of Molecular Biology and Genetics, Federal Research and Clinical Center of Physical-Chemical Medicine of FMBA, P.O. Box: 119435, Moscow, Russia
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Augmentation of Creatine in the Heart
Author(s):
Sevasti Zervou, Hannah J. Whittington, Angela J. Russell and Craig A. LygatePages 19-28 (10)
Abstract:
Creatine is a principle component of the creatine kinase (CK) phosphagen system common to all vertebrates. It is found in excitable cells, such as cardiomyocytes, where it plays an important role in the buffering and transport of chemical energy to ensure that supply meets the dynamic demands of the heart. Multiple components of the CK system, including intracellular creatine levels, are reduced in heart failure, while ischaemia and hypoxia represent acute crises of energy provision. Elevation of myocardial creatine levels has therefore been suggested as potentially beneficial, however, achieving this goal is not trivial. This mini-review outlines the evidence in support of creatine elevation and critically examines the pharmacological approaches that are currently available. In particular, dietary creatine-supplementation does not sufficiently elevate creatine levels in the heart due to subsequent down-regulation of the plasma membrane creatine transporter (CrT). Attempts to increase passive diffusion and bypass the CrT, e.g. via creatine esters, have yet to be tested in the heart. However, studies in mice with genetic overexpression of the CrT demonstrate proof-of-principle that elevated creatine protects the heart from ischaemia-reperfusion injury. This suggests activation of the CrT as a major unmet pharmacological target. However, translation of this finding to the clinic will require a greater understanding of CrT regulation in health and disease and the development of small molecule activators.
Keywords:
Creatine transporter, energetics, heart disease.
Affiliation:
Division of Cardiovascular Medicine, Radcliffe Department of Medicine, University of Oxford, Wellcome Trust Centre for Human Genetics, Roosevelt Drive, Headington OX3 7BN, UK.
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RAS/Effector Interactions from Structural and Biophysical Perspective
Author(s):
Ariel Erijman and Julia M. ShifmanPages 370-375 (6)
Abstract:
RAS is a molecular switch that regulates a large number of pathways through interactions with many effector proteins. Most RAS/effector complexes are short-lived, demonstrating fast association and fast dissociation rate and Kds ranging from 10-8–10-5 M, compatible with the signaling function of these interactions in the cell. RAS effectors share little sequence homology but all contain an RAS binding domain that exhibits ubiquitin fold. All effectors bind to the same epitope on RAS by forming an intermolecular beta sheet and creating a number of favorable hydrogen bonds and salt bridges across the binding interface. Several hot-spots on both RAS and effector molecules constitute a general recognition mode. RAS/effector interactions occur only when RAS is found in the active, GTP-bound state, and are disrupted upon GTP hydrolysis, most probably due to increased flexibility of the RAS molecule. Recent NMR studies demonstrate how in the presence of multiple binding partners, RAS prefers certain effectors to others. The hierarchy of these interactions could be altered for RAS oncogenic mutants, thus perturbing the network of the downstream signaling. Insights obtained through biophysical and structural studies of effectors interacting with RAS and its mutants establish the basic principles that could be used for designing drugs in RAS-associated diseases.
Keywords:
Binding affinity, complex structure, intermolecular interactions, protein-protein interactions.
Affiliation:
Department of Biological Chemistry, The Alexander Silberman Institute of Life Sciences, The Hebrew University of Jerusalem, Jerusalem 91904, Israel.
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