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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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