3,068 results match your criteria Current Topics in Medicinal Chemistry [Journal]


Recent Advancement against Neglected Diseases.

Curr Top Med Chem 2018 ;18(18):1520-1521

Department of Biochemistry/Bioinformatics Institute of Science GITAM University, Visakhapatnam, A.P, India.

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http://dx.doi.org/10.2174/156802661818181119142905DOI Listing
January 2018

From Darkness to Light: Pretargeted Radionuclide Imaging Driven by Tetrazine Bioorthogonal Chemistry.

Curr Top Med Chem 2018 ;18(18):1515-1519

Huaxi MR Research Center, Department of Radiology, West China Hospital and West China School of Medicine, Sichuan University, Chengdu (610041), China.

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http://dx.doi.org/10.2174/156802661818181119142326DOI Listing
January 2018

Identification of Drug Binding Sites and Action Mechanisms with Molecular Dynamics Simulations.

Curr Top Med Chem 2018 Dec 11. Epub 2018 Dec 11.

Beijing Advanced Innovation Center for Biomedical Engineering, Medicine-Engineering Interdisciplinary Research Institute, Beihang University, Beijing 100083. China.

Identifying drug binding sites and elucidating drug action mechanisms are important components in a drug discovery process. In this review, we briefly compared three different approaches (sequence-based methods, structure-based methods and probe-based molecular dynamics (MD) methods) to identifying drug binding sites, and concluded that probe-based MD methods are much more advantageous in dealing with flexible target macromolecules and digging out druggable macromolecule conformations for subsequent drug screening. The applications of MD simulation to studying drug-target interactions were demonstrated with different types of target molecules, including lipid membrane, protein and DNA. Read More

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http://dx.doi.org/10.2174/1568026619666181212102856DOI Listing
December 2018

Psychobiome feeding mind: poliphenolics in depression and anxiety.

Curr Top Med Chem 2018 Dec 10. Epub 2018 Dec 10.

Institute of Molecular Genetics, National Research Council, Section of Chieti, Chieti. Italy.

Recently gut bacterial populations seem to be involved in many functions and in the pathogenesis of several medical conditions. Traditionally the intestinal microbiome has been recognized to play an important role in metabolizing food compounds in simpler chemical structures for the absorption of different nutrients, and in maintenance control on gastrointestinal pathogens species. Bacterial populations are implicated in a complicated network of interactions within the immune system, epithelial cells, local endocrine system, that affects the peripheral and the central nervous system, via blood circulation. Read More

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http://dx.doi.org/10.2174/1568026619666181210151348DOI Listing
December 2018

Histone Deacetylase Inhibitors in Cancer Therapy.

Curr Top Med Chem 2018 Dec 10. Epub 2018 Dec 10.

National Centre for International Research in Cell and Gene Therapy, School of Basic Medical Sciences, Academy of Medical Sciences, Zhengzhou University, Zhengzhou. China.

Histone deacetylases (HDACs), as epigenetic modifiers, are essential for gene transcriptional activities. The alternation of HDACs expression, mutation and/or inappropriate recruitments have been discorvered in a broad range of tumors contributing to the tumorigenesis through a serial of biological pathways. HDACs, therefore, are characterized as promising cancer therapeutic targets, and their inhibitors are under rapid development. Read More

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http://dx.doi.org/10.2174/1568026619666181210152115DOI Listing
December 2018

Computer aided Drug Designing for the identification of high affinity small molecule targeting CD20 for the clinical treatment of Chronic Lymphocytic Leukemia (CLL).

Curr Top Med Chem 2018 Dec 10. Epub 2018 Dec 10.

Computer Aided Drug Designing and Molecular Modeling Lab, Department of Bioinformatics, Alagappa University, Karaikudi-630 003, Tamil Nadu. India.

Background: Chronic lymphocytic leukemia (CLL) is a B-lineage lymphoid malignancy of self-reactive cells that are focused to produce polyreactive natural auto antibodies. Its surface protein marker CD20 plays an important role in the humoral immune response, targeting which have emerged as an attractive therapeutic option for the treatment of CLL. The present study explains the interaction of the CD20 with its established inhibitors and to discover the compound having high binding affinity against the target protein receptor. Read More

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http://www.eurekaselect.com/168206/article
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http://dx.doi.org/10.2174/1568026619666181210150044DOI Listing
December 2018
2 Reads

Chemistry and Biology of Farnesol and its Derivatives: Quorum Sensing Molecules with Immense Therapeutic Potential.

Curr Top Med Chem 2018 Dec 10. Epub 2018 Dec 10.

Department of Biotechnology, Indian Institute of Technology Roorkee Roorkee - 247667, Uttarakhand. India.

Background: Farnesol is an acyclic sesquiterpene alcohol, endogenously synthesized via the ergosterol pathway. It is a quorum sensing molecule (QSM) that was first discovered in C. albicans, and is involved in the inhibition of hyphae formation. Read More

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http://dx.doi.org/10.2174/1568026619666181210124159DOI Listing
December 2018

Antifungal And Antimicrobial Properties Of A Purified Protease Inhibitor From Macrotyloma Uniflorum Seeds.

Curr Top Med Chem 2018 Dec 10. Epub 2018 Dec 10.

Department of Biotechnology, University of Calicut, 673635, Kerala. India.

Plant protease Inhibitors (PIs) play key roles in regulation of many biological activities and being less toxic, more potent and specific compared to chemical inhibitors. A new proteinaceous trypsin inhibitor (MUTI) was isolated and purified from Macrotyloma uniflorum seeds. MUTI with a molecular mass of 25 KDa was purified to homogeneity via three sequential purification steps i. Read More

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http://dx.doi.org/10.2174/1568026619666181210150923DOI Listing
December 2018
3 Reads

Structure base Virtual screening for the identification of high affinity compounds as potent VEGFR2 inhibitors for the treatment of Renal Cell Carcinoma.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

In silico Research Laboratory, Eminent Biosciences, Vijayanagar, Indore - 452010. India.

Renal Cell Carcinoma is a common type of renal cancer-causing deaths worldwide is characterized by sustained angiogenesis. VEGF and its receptors play a major role in physiologic and pathologic angiogenesis, which is marked in tumour progression and metastasis development. Induction of VEGF genes occur due to hypoxic condition induced by tumour growth after a critical size in cancerous cell. Read More

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http://dx.doi.org/10.2174/1568026619666181130142237DOI Listing
November 2018

In Silico and In Vitro Investigation of the Antifungal Activity of Isoeugenol against Penicillium citrinum.

Curr Top Med Chem 2018 11 30. Epub 2018 Nov 30.

Postgraduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, Cidade Universitária, s / n - Castelo Branco, 58051-900, João Pessoa, Paraíba, Brazil.

This increase in the prevalence of drug-resistant pathogens occurs at a time when the discovery and development of new antimicrobial agents occur slowly. In this context, the objective of this study was to investigate the antifungal activity of isoeugenol, a phenylpropanoid, by in vitro and in silico assays against Penicillium citrinum strains. For in silico analysis, the software PASS online, Molinspiration and Osíris were used. Read More

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http://dx.doi.org/10.2174/1568026619666181130141818DOI Listing
November 2018
1 Read

AO-BBO: A Novel Optimization Algorithm and Its Application in Plant Drug Extraction.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

College of Information Science and Technology, Beijing University of Chemical Technology, Beijing. China.

It is well-known that the biogeography-based optimization (BBO) algorithm lacks searching power in some circumstances. In order to address this issue, an adaptive opposition-based biogeography-based optimization algorithm (AO-BBO) is proposed. Based on the BBO algorithm and opposite learning strategy, this algorithm chooses different opposite learning probabilities for each individual according to the habitat suitability index (HSI), so as to avoid elite individuals from returning to local optimal solution. Read More

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http://dx.doi.org/10.2174/1568026619666181130140709DOI Listing
November 2018

In silico assessment of ADME properties: Advances in Caco-2 Cell Monolayer Permeability Modeling.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Department of Coatings and Polymer Materials, North Dakota State University, Fargo, North Dakota, 58102. United States.

One of the main goals of in silico Caco-2 cell permeability models is to identify those drug substances with high intestinal absorption in human (HIA). For more than a decade, several in silico Caco-2 models have been made, applying a wide range of modeling techniques; nevertheless, their capacity for intestinal absorption extrapolation is still doubtful. There are three main problems related to the modest capacity of obtained models, including the existence of inter- and/or intra-laboratory variability of recollected data, the influence of the metabolism mechanism, and the inconsistent in vitro-in vivo correlation (IVIVC) of Caco-2 cell permeability. Read More

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http://dx.doi.org/10.2174/1568026619666181130140350DOI Listing
November 2018

A review of neuroimaging studies on working memory paradigms in patients with bipolar disorder.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Department of Anatomy, Histology and Embryology, Faculty of Medicine, Medical University Plovdiv. Bulgaria.

New brain technologies including neuroimaging studies are powerful means for providing new insights into clinical and cognitive neuroscience. Bipolar disorder is a severe chronic phasic mental disease characterized by various cognitive dysfunctions. Working memory is one prominent domain of cognitive impairment in bipolar disorder. Read More

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http://dx.doi.org/10.2174/1568026619666181130135703DOI Listing
November 2018
1 Read

The Dysregulation Of Micrornas And The Role Of Stress In The Pathogenesis Of Mental Disorders.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Clinic of Psychiatry, University Multiprofile Hospital for Active Treatment "Alexandrovska" - Sofia. Bulgaria.

MicroRNAs are endogenous small non-coding RNAs that regulate gene expression by means of partial complementarity to microRNA binding sites at their target genes. These molecules have emerged as key regulators of almost every biological process including accurate control of neuronal gene expression. The authors discuss the current state of microRNA research, including studies of psychiatric disorders (schizophrenia, autism spectrum disorder and affective disorders). Read More

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http://dx.doi.org/10.2174/1568026619666181130135253DOI Listing
November 2018

Apicoplast Metabolism: Parasite's Achilles' Heel.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Department of Internal Medicine, University of New Mexico School of Medicine, Albuquerque, NM. United States.

Malaria continues to impinge heavily on mankind, with five continents still under its clasp. Wide spread and rapid emergence of drug resistance in the Plasmodium parasite to current therapies, accentuate the quest for novel drug targets and antimalarial compounds. Plasmodium parasites, maintain a non-photosynthetic relict organelle known as Apicoplast. Read More

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http://dx.doi.org/10.2174/1568026619666181130134742DOI Listing
November 2018
2 Reads

Counting on Fragment Based Drug Design Approach for Drug Discovery.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Molecular Modeling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab, 147002. India.

Fragment based drug design (FBDD) is a structure guided ligand design approach used in the process of drug discovery. It involves identification of low molecular weight fragments as hits followed by determination of their binding mode using X-ray crystallography and/or NMR spectroscopy. X-ray protein crystallography is one of the most sensitive biophysical methods used for screening and is least prone to false positives. Read More

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http://dx.doi.org/10.2174/1568026619666181130134250DOI Listing
November 2018

Exploring the biology and structural architecture of sortase roleon Biofilm formation in gram positive pathogens.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Department of Bioinformatics, Computer Aided Drug Design and Molecular Modeling Lab, Alagappa University, Science Block, Karaikudi-630003, Tamilnadu. India.

Gram-positive bacteria signify a surface organelle that decorates the cell surfaces using Sortase enzymes. The mechanism of SrtC lings to the formation of amide or peptide bonds between cell surface proteins that sorting signal to strategically positioned amino groups. Sorting signals linked to peptidoglycan function as the principal architects of cell wall and facilitate each microbe to effectively interact with its host environment. Read More

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http://dx.doi.org/10.2174/1568026619666181130133916DOI Listing
November 2018
1 Read

Antimalarials: Review Of Plasmepsins As Drug Targets And Hiv Protease Inhibitors Interactions.

Curr Top Med Chem 2018 11 30. Epub 2018 Nov 30.

Department of Biomedical Engineering, School of Engineering Sciences, College of Basic & Applied Sciences, University of Ghana, PMB LG 77, Legon, Accra. Ghana.

Malaria is a major global health concern with majority of cases reported in regions of South-East Asia, Eastern Mediterranean, Western Pacific, the Americas, and Sub-Saharan Africa. The World Health Organization (WHO) estimated 216 million worldwide reported cases of malaria in 2016. It is an infection of the red blood cells by parasites of the genus Plasmodium with most severe and common forms caused by Plasmodium falciparum (P. Read More

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http://dx.doi.org/10.2174/1568026619666181130133548DOI Listing
November 2018
4 Reads

New Experimental and Computational Tools for Drug Discovery: Medicinal Chemistry, Molecular Docking, and Machine Learning. Part - VI.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Department of Organic Chemistry II, University of the Basque Country UPV/EHU, Leioa 48940. Spain.

We are publishing the series of special issues "New experimental and computational tools for drug discovery" focused on the use of enabling technologies like Computational Chemistry, Bioinformatics, OMICS, Combinatorial Chemistry, Data Analysis, etc. in Medicinal Chemistry and Drug Discovery. The series have published a total of five special issues until this moment (1-5). Read More

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http://www.eurekaselect.com/167938/article
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http://dx.doi.org/10.2174/1568026619666181130122945DOI Listing
November 2018
1 Read

Computational identification of chemical compounds with potential activity against Leishmania amazonensis using nonlinear machine learning techniques.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Unidad de Investigación de Diseño de Fármacos y Conectividad Molecular, Departamento de Química Física, Facultad de Farmacia, Universitat de València. Spain.

Leishmaniasis is poverty-related disease endemic in 98 countries worldwide, with morbidity and mortality increasing daily. All currently used first-line and second-line drugs for the treatment of leishmaniasis exhibit several drawbacks including toxicity, high costs and route of administration. Consequently, the development of new treatments for leishmaniasis is a priority in the field of neglected tropical diseases. Read More

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http://dx.doi.org/10.2174/1568026619666181130121558DOI Listing
November 2018
2 Reads

Hotspot identification on protein surfaces using probe-based MD simulations: Successes and Challenges.

Curr Top Med Chem 2018 Nov 30. Epub 2018 Nov 30.

Department of Physics, Birzeit University, PO BOX 14, Birzeit. Palestinian Territory, Occupied.

Molecular dynamics (MD) based computational co-solvent mapping methods involve the generation of an ensemble of MD-sampled target protein conformations and using selected small molecule fragments to identify and characterize binding sites on the surface of a target protein. This approach incorporates atomic-level solvation effects and protein mobility. It has shown great promise in the identification of conventional competitive and allosteric binding sites. Read More

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http://dx.doi.org/10.2174/1568026619666181130120308DOI Listing
November 2018

Targeting α-(1,4)-glucosidase in Diabetes mellitus Type 2: The Role of New Synthetic Coumarins as Potent Inhibitors.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Laboratorio de Productos Naturales, Departamento de Química Farmacológica y Toxicológica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santos Dumont 964, Independencia, Santiago. Chile.

Diabetes mellitus type 2 (DMT2) is a metabolic disease characterized by a chronic increase in glycemia that promotes several long-term complications and high mortality. Some enzymes involved in glycaemic control, such as α-(1,4)-glucosidase, have now been established as novel pharmacological targets. Coumarins have shown benefits in attenuating signs and complications of DMT2, including inhibition of this enzyme. Read More

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http://dx.doi.org/10.2174/1568026619666181130113033DOI Listing
November 2018
1 Read

Advances in in-silico B-cell epitope prediction.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

School of Information Science and Technology, Northeast Normal University, Changchun 130117. China.

Identification of B-cell epitopes in target antigens is one of the most crucial steps for epitope-based vaccine development, immunodiagnostic tests, antibody production, and disease diagnosis and therapy. Experimental methods for B-cell epitope mapping is time consuming, costly and labor intensive; in the meantime, various in-silico methods are proposed to predict both linear and conformational B-cell epitopes. The accurate identification of B-cell epitopes present major challenges for immunoinformaticians. Read More

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http://dx.doi.org/10.2174/1568026619666181130111827DOI Listing
November 2018

Current understanding of the potential of proteomics and metabolomics approaches in cancer chemoresistance: A focus on Multiple Myeloma.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Proteomics Lab, National Centre for Cell Science, Ganeshkhind, Pune-411007, MH. India.

Chemoresistance is one of the major hurdles in cancer treatment leading to recurrence of cancer and affects overall survival of patients. Cancer chemoresistance can be associated with various phenomena including modulation of vital cellular pathways. Unrevealing these alterations could provide better understanding of chemoresistance and assist in identification of new targets to overcome it. Read More

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http://dx.doi.org/10.2174/1568026619666181130111202DOI Listing
November 2018
1 Read

Current practice and new developments in the use of in vivo Magnetic Resonance Spectroscopy for the assessment of key metabolites implicated in the pathophysiology of schizophrenia.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Department of Radiology, Haukeland University Hospital, Bergen. Norway.

Magnetic Resonance Spectroscopy (MRS) has become a valuable tool for investigating the biochemical bases of both normal processes in the healthy brain and elucidating the pathophysiology of neuropsychiatric disorders. As a rapidly advancing field, new developments in pulse sequence design have seen new possibilities arise in terms of what can be done with in vivo spectroscopy. While the applications of MRS are numerous, this review has been confined to the use of single voxel spectroscopy in the assessment of five key metabolites and their roles in schizophrenia: N-acetylaspartate (NAA), glutamate (Glu) and glutamine (Gln), γ-aminobutyric acid (GABA) and glutathione (GSH). Read More

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http://dx.doi.org/10.2174/1568026619666181130103559DOI Listing
November 2018

An In silico Investigation of Potential EGFR Inhibitors for the clinical treatment of Colorectal Cancer.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Computer Aided Drug Designing and Molecular Modeling Lab, Department of Bioinformatics, Alagappa University, Karaikudi-630 003, Tamil Nadu. India.

CLC commonly gives the risk symptoms to older age, obesity and lack of physical exercise, but less likely to generate in people having little genetic risk. Colorectal cancer originates in the vicinity of the colon as well as rectum. Epithelium or lamina proparia is the top layer lining of the colon or rectum of the gastrointestinal tract where the most frequent mutations take place in the Wnt signaling pathway, TGF-β signaling, EGFR, PI3K. Read More

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http://dx.doi.org/10.2174/1568026619666181129144107DOI Listing
November 2018
1 Read

Small Molecules Effective against Liver and Blood Stage Malarial Infection.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Department of Chemistry, Miranda House, University of Delhi, Delhi-110007. India.

Malaria is a lethal disease causing devastating global impact by killing more than 8,00,000 individuals yearly. A noticeable decline in malaria related deaths can be attributed to the most reliable treatment, ACTs against P. falciparum. Read More

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http://dx.doi.org/10.2174/1568026619666181129143623DOI Listing
November 2018
2 Reads

Internet Resources For Drug Discovery And Design.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

ITMO University, St. Petersburg 197101. Russian Federation.

The review describes online resources used for drug discovery and design. The Internet resources can be classified into two classes. The first class of resources accumulates an information about drugs, drug candidates, compounds, bioassays. Read More

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http://dx.doi.org/10.2174/1568026619666181129142127DOI Listing
November 2018
2 Reads

Structure, Functions and Selective Inhibitors of HDAC6.

Authors:
Tao Liang Hao Fang

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44, Wenhuaxi Road, Jinan, Shandong, 250012. China.

Histone deacetylases 6 (HDAC6) has emerged as a promising target for the treatment of various human diseases including cancer, neurodegenerative disease and immunology due to its unique structure, substrate and biological functions. HDAC6 is involved in cell motility, cell survival, cell cycle progression, developmental events, prognosis as well as protein degradation and the involvement of HDAC6 in multiple biological process have gained lots of attention. There is increasing interest in HDAC6 and its selective inhibitors. Read More

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http://dx.doi.org/10.2174/1568026619666181129141822DOI Listing
November 2018
1 Read

Antibiotics-Peptide Conjugates Against Multidrug-Resistant Bacterial Pathogens.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Center for Targeted Drug Delivery, Department of Biomedical and Pharmaceutical Sciences, Chapman University School of Pharmacy, Harry and Diane Rinker Health Science Campus, 9401 Jeronimo Road, Irvine, California 92618-1908. United States.

The menace of multi-drug resistance by bacterial pathogens that are responsible for infectious diseases in humans and animals cannot be over-emphasized. Many bacteria develop resistance to antibiotics by one or more combination of resistance mechanisms namely, efflux pump activation thereby reducing bacteria intracellular antibiotic concentration, synthesizing a protein that protects target site causing poor antibiotic affinity to the binding site, or mutations in DNA and topoisomerase gene coding that alters residues in the binding sites. The ability to use a combination of these resistance mechanisms among others create a phenomenon known as antimicrobial drug resistance. Read More

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http://dx.doi.org/10.2174/1568026619666181129141524DOI Listing
November 2018
1 Read
3.400 Impact Factor

Chemotherapeutic Potential of Monensin as an Anti-microbial Agent.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Department of Biochemistry, University of Delhi South Campus, Benito Juarez Road, New Delhi 110021. India.

Monensin is a lipid soluble naturally occurring bioactive ionophore produced by Streptomyces spp. Its antimicrobial activity is mediated by its ability to exchangeNa+ and K+ ions across the cell membrane thereby disrupting ionic gradients and altering cellular physiology. It is approved by Food and Drug Administration as a veterinary antibiotic to treat coccidiosis. Read More

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http://dx.doi.org/10.2174/1568026619666181129141151DOI Listing
November 2018
2 Reads

Ionophores as Potent Anti-Malarials: A Miracle in the Making.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Department of Biochemistry, University of Delhi South Campus, Benito Juarez Road, New Delhi-110021. India.

Plasmodium has a complex life cycle that spans between mosquito and human. For survival and pathogenesis it banks upon dynamic alterations in ionic transport across organelle and plasma membrane. Being a fundamental contributor of crucial biological processes in parasite, ionic balance facilitates parasite invasion, augmentation and transmission. Read More

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http://dx.doi.org/10.2174/1568026619666181129125950DOI Listing
November 2018

Designing of a Novel Indoline scaffold based Antibacterial Compound and Pharmacological Evaluation using Chemoinformatics approach.

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Drug Discovery & Development Laboratory, Department of Chemistry, University of Delhi, Delhi-110007. India.

Antibiotic resistance is not only a global public health threat but also a huge economic burden to our society that urgently needs to be addressed by improved antibiotics and continuing development of novel molecules to treat resistant bacterial infections. Nowadays combination therapies offer a competent approach to counteract antibiotic resistance in bacteria. Better knowledge of mechanisms of antibiotic resistance has lead to the finding of new alternatives to antibiotic therapy. Read More

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http://dx.doi.org/10.2174/1568026619666181129125524DOI Listing
November 2018

Biology of Heme: Drug Interactions and Adverse Drug Reactions with CYP450".

Curr Top Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Drug Discovery and Development Laboratory, Department of Chemistry, University of Delhi, Delhi-110007. India.

Heme is central to functions of many biologically important enzymes (hemoproteins). It is an assembly of four porphyrin rings joined through methylene bridges with a central Fe (II). Heme is present in all cells, and its synthesis and degradation balance its amount in the cell. Read More

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http://dx.doi.org/10.2174/1568026619666181129124638DOI Listing
November 2018
4 Reads

Synthesis and Biological Profiles of 1,2,3-Triazole Scaffold.

Curr Top Med Chem 2018 ;18(17):1426-1427

Universidade Federal Fluminense, Instituto de Quimica, Campus do Valonguinho, 24020-150 Niteroi, RJ, Brazil.

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http://dx.doi.org/10.2174/156802661817181107151553DOI Listing
January 2018

Targeting the DCN1-UBC12 Protein-Protein Interaction for Selective Modulation of Cullin Substrates.

Curr Top Med Chem 2018 ;18(17):1423-1425

School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.

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http://dx.doi.org/10.2174/156802661817181107151134DOI Listing
January 2018

Discovery of New Medication for the Treatment of Depression Comorbid with Inflammatory Diseases.

Curr Top Med Chem 2018 ;18(16):1393-1394

Department of Pharmaceutical Chemistry Faculty of Pharmacy Yeditepe University Istanbul, Turkey.

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http://dx.doi.org/10.2174/156802661816181107142751DOI Listing
December 2018
2 Reads

New Drugs and Therapeutic/Diagnostic Targets for Fungal and Parasitic Diseases - Part II.

Curr Top Med Chem 2018 ;18(16):1357

Departamento de Farmacia y Tecnologia Farmaceutica Facultad de Farmacia Universidad Complutense de Madrid Plaza Ramon y Cajal s/n, Madrid, 28040, Spain.

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http://dx.doi.org/10.2174/156802661816181107142130DOI Listing
December 2018

Bioactive Small Molecules in the Pathogenesis and Pharmacology of Cardiovascular Diseases: From Bench to Bedside.

Authors:
Lihui Jin Yu Yu

Curr Top Med Chem 2018 ;18(16):1351-1353

Department of Pediatric Cardiovascular, Xin Hua Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200092, China.

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http://dx.doi.org/10.2174/156802661816181107141558DOI Listing
December 2018
3 Reads

Current Breakthroughs in Structure-Based Design of Synthetic and Natural Sourced Inhibitors against Zika Viral Targets.

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Pharmacognosy and Phytotherapy Laboratory, Division of Pharmacognosy, Department of Pharmaceutical Technology, Jadavpur University, Kolkata -700032. India.

Background: Zika is a worldwide pandemic dreadful viral transmission through Aedes mosquito vector. It significantly causes fever, joint pain or rash, and conjunctivitis. Pregnant mothers suffering from Zika viral infection may have fetal abnormalities due to severe neurological problems, characterized by microcephaly along with Guillain-Barré syndrome, issuing ZIKV a major public health concern as declared by the World Health Organization. Read More

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http://dx.doi.org/10.2174/1568026619666181120125525DOI Listing
November 2018
2 Reads
3.402 Impact Factor

NMR based metabolomics: An exquisite and facile method for evaluating therapeutic efficacy and screening drug toxicity.

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Centre of Biomedical Research, SGPGIMS Campus, Raibareli Road, Lucknow-226014. India.

Metabolomics is an analytical approach to metabolism and involves quantitative and comparative analysis of low-molecular-weight metabolites in body fluids or cellular/tissues extracts. Owing to its ability to reveal disease-specific metabolic patterns or metabolic changes produced in response to a therapeutic intervention; it is gaining widespread applications virtually in all aspects of biomedical and pharmaceutical research pertaining to human healthcare management. It has also started playing a strategic role in pharmacological and toxicological research for evaluating therapeutic efficacy/safety of promising drug candidates either alone or in conjunction with other omics tools such as genomics, transcriptomics and proteomics. Read More

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http://dx.doi.org/10.2174/1568026619666181120141603DOI Listing
November 2018
3 Reads

Application of Computational Techniques to Unravel Structure-Function Relationship and Their Role in Therapeutic Development.

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Department of Biotechnology, Indian Institute of Technology Roorkee, Roorkee-247667, Uttarakhand. India.

Application of computational tools and techniques has emerged as an invincible instrument to unravel the structure-function relationship and offered better mechanistic insights in the designing and development of new drugs along with treatment regime. The use of in silico tools equipped modern chemist with armamentarium of extensive methods to meticulously comprehend the structural tenacity of receptor-ligand interactions and their dynamics. In silico methods offers a striking property of being less resource intensive and viable economically as compared to experimental evaluation. Read More

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http://dx.doi.org/10.2174/1568026619666181120142141DOI Listing
November 2018
4 Reads

Flavanoids and Anthranquinones as Xanthine oxidase and Monoamine oxidase inhibitors: A new approach towards Inflammation and oxidative stress.

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Faculty of Pharmaceutical Sciences, M. D. University, Rohtak. India.

The development of xanthine oxidase and monoamine oxidase inhibitors led to important breakthroughs in the therapy of oxidative damage, hyperuricemia, gout, neurological, neuropsychiatric disorders and management of reperfusion injury. Drugs obtained from natural sources play an important role in treatment of various pathological disorders and act as lead compound for the discovery of new synthetic drug substances. In this review various pharmacological effects produced by inhibition of xanthine oxidase and monoamine oxidase through natural and synthetic flavanoids as well as anthraquinones are discussed in detail. Read More

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http://dx.doi.org/10.2174/1568026619666181120143050DOI Listing
November 2018
5 Reads

Personalized Medicine and Medicinal Chemistry:Toward a legal framework in the European Union ].

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Department of Public Law, Chair in Law and Human Genome Research Group, University of the Basque Country UPV/EHU, 48940, Leioa, Biscay. Spain.

In the last years the fields of Medicinal Chemistry and especially the ones related to the so-called Personalized Medicine, has received a great attention. Significant investment and remarkable researches surround the matter; however, not all those promising advances are reaching patients as quickly as they should. The absence of an adequate regulatory framework could be not helping. Read More

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http://dx.doi.org/10.2174/1568026619666181120144213DOI Listing
November 2018
2 Reads

DNA Methyltransferase Inhibitors and Their Therapeutic Potential.

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Jiangsu Key Laboratory of Neuropsychiatric Diseases and Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Soochow University, 199 Ren-Ai Road, Suzhou, Jiangsu 215123. China.

Aberrant DNA methylation at the 5-position of cytosine, catalyzed by DNA methyltransferases (DNMTs), is associated with not only various cancers by silencing of tumor suppressor genes but also other diseases. The DNMTs, especially the DNMT1, DNMT3A and DNMT3B, are often overexpressed in various cancer tissues and cell lines. DNMTs are important epigenetic targets for drug development since the DNA methylation is reversible. Read More

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http://dx.doi.org/10.2174/1568026619666181120150122DOI Listing
November 2018
12 Reads

In silico protein interaction network analysis of virulence proteins associated with invasive aspergillosis for drug discovery.

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Centre for Biotechnology, Maharshi Dayanand University, Rohtak-124001, Haryana. India.

Protein-Protein interaction (PPI) network analysis of virulence proteins of Aspergillus fumigatus is prevailing strategy to understand the mechanism behind the virulence of A. fumigatus. The identification of major hub proteins and targeting the hub protein as a new antifungal drug target will help in treating the invasive aspergillosis. Read More

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http://dx.doi.org/10.2174/1568026619666181120150633DOI Listing
November 2018
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Intelligently applying Artificial Intelligence in Chemoinformatics.

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Department of Biotechnology, Indian Institute of Technology Roorkee, Roorkee 247667. India.

The intertwining of chemoinformatics with artificial intelligence (AI) has given a tremendous fillip to the field of drug discovery. With the rapid growth of chemical data from high throughput screening and combinatorial synthesis, AI has become an indispensable tool for drug designers to mine chemical information from large compound databases for developing drugs at a much faster rate as never before. The applications of AI have gone beyond bioactivity predictions and have shown promise in addressing diverse problems in drug discovery like de novo molecular design, synthesis prediction and biological image analysis. Read More

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http://dx.doi.org/10.2174/1568026619666181120150938DOI Listing
November 2018

MicroRNAs as therapeutic agents: The future of the battle against cancer.

Authors:
Sumit Biswas

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Department of Biological Sciences, BITS, Pilani - K K Birla Goa Campus, Zuarinagar, Goa 403726. India.

Since their discovery in the 1990's, the study of a class of non-coding, single-stranded RNAs, christened the microRNAs has opened up new vistas in the field of cancer biology. MicroRNAs bind to their target mRNAs to act as either oncogenes or tumour suppressors. With the near-complete elucidation of the biogenesis pathway, and the advent of rapid sequencing technologies, microRNAs have slowly cemented their place as essential biomarkers for delineating the progression, metastasis, relapse or drug resistance of cancer. Read More

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http://dx.doi.org/10.2174/1568026619666181120121830DOI Listing
November 2018
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Editorial: ADVANCEMENT IN MICROBIAL CHEMINFORMATICS.

Curr Top Med Chem 2018 Nov 20. Epub 2018 Nov 20.

Bioinformatics Research Laboratory, LeGene Biosciences Pvt Ltd, Indore - 452010, Madhya Pradesh. India.

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http://dx.doi.org/10.2174/1568026619666181120121528DOI Listing
November 2018
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Tetramethoxyluteolin for the treatment of neurodegenerative diseases.

Curr Top Med Chem 2018 Nov 19. Epub 2018 Nov 19.

Molecular Immunopharmacology and Drug Discovery Laboratory, Department of Immunology, Tufts University School of Medicine, Boston, MA. United States.

Background Most neurodegenerative and other brain disorders, especially Myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS) and autism spectrum disorder (ASD) continue to elude objective biomarkers and effective treatments. Increasing evidence indicates that such diseases involve focal inflammation of the brain. Objective To review the role of cytokine-neuropeptide interactions in the pathogenesis of inflammation of the brain and the beneficial role of natural flavonoids. Read More

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http://dx.doi.org/10.2174/1568026617666181119154247DOI Listing
November 2018
4 Reads