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Tuesday, November 8, 2016

Call For Paper


Bentham Science Publishers would like to invite you to submit your research paper for publishing in the Journal of 
Current Topics in Medicinal Chemistry


Wednesday, November 2, 2016

Highlighted Article: The Glitter of Carbon Nanostructures in Hybrid/Composite Hydrogels for Medicinal Use



The Glitter of Carbon Nanostructures in Hybrid/Composite Hydrogels for Medicinal Use


Author(s):

Daniel Iglesias, Susanna Bosi, Michele Melchionna, Tatiana Da Ros and Silvia Marchesan   Pages 1976 - 1989 ( 14 )

Abstract:


In recent years, we have witnessed to fast developments in the medicinal field of hydrogels containing various forms of integrated nanostructured carbon that adds interesting mechanical, thermal, and electronic properties. Besides key advances in tissue engineering (especially for conductive tissue, such as for the brain and the heart), there has been innovation also in the area of drug delivery on-demand, with engineered hydrogels capable of repeated response to light, thermal, or electric stimuli. This mini-review focusses on the most promising developments as applied to the gelation of protein/ peptide (including self-assembling amino acids and low-molecular-weight gelators), polysaccharide, and/or synthetic polymer components in medicine. The emerging field of graphene-only hydrogels is also briefly discussed, to give the reader a full flavor of the rising new paradigms in medicine that are made possible through the integration of nanostructured carbon (e.g., carbon nanotubes, nanohorns, nanodiamonds, fullerene, etc.). Nanocarbons are offering great opportunities to bring on a revolution in therapy that the modern medicinal chemist needs to master, to realise their full potential into powerful therapeutic solutions for the patient.

Keywords:

Carbon nanostructures, Carbon nanotubes, Composite, Graphene, Hybrid, Hydrogels.

Affiliation:

Department of Chemical and Pharmaceutical Sciences, University of Trieste, Via Giorgieri 1, 34127 Trieste, Italy.

Graphical Abstract:





For More Information Please Visit Our Website Current Topics in Medicinal Chemistry

Monday, October 24, 2016

Most Cited Article: Next Generation Biofilm Inhibitors for Pseudomonas aeruginosa: Synthesis and Rational Design Approaches



Next Generation Biofilm Inhibitors for Pseudomonas aeruginosa: Synthesis and Rational Design Approaches
Author(s):
Mahesh S. Majik and Prakash T. ParvatkarPages 81-109 (29)
Abstract:

The bacterial biofilms and the emergence of multiple drug resistance have become a major threat for current medical treatment of nosocomial infections. It has been estimated that about 65-80% of microbial infections in the developed countries are associated with biofilms. Given the prominence of biofilms in infectious diseases, increasing efforts toward the development of small molecules that will modulate bacterial biofilm development and maintenance is on the rise. Till date, marine natural products have shown a tremendous potential as pharma leads and also given new skeletons which would be used as biofilm/QS inhibitors. Medically relevant biofilm forming bacteria such as Pseudomonas aeruginosa which is most frequently isolated bacteria in nosocomial infection is believed to be a model organism for biofilm studies. Hence, in this review, we have highlighted the development of small molecules that inhibit and/or disperse bacterial biofilms of P. aeruginosa in particular. Additionally, the rational design approaches as well as synthetic methodologies along with biological studies has been accounted in this article.
Keywords:
Marine natural products, biofilms, quorum sensing inhibitors, antifouling, chemical signaling.
Affiliation:
Bio-organic Chemistry Laboratory, CSIR-National Institute of Oceanography, Dona-Paula Goa 403 004, India




For More Information Please Visit Our Website Current Topic in Medicinal Chemistry


Tuesday, October 18, 2016

Copper Homeostasis for the Developmental Progression of Intraerythrocytic Malarial Parasite

Article Details


Copper Homeostasis for the Developmental Progression of Intraerythrocytic Malarial Parasite

[ Vol. 16 , Issue. 27 ]

Author(s):

Hiroko Asahi, Fumie Kobayashi, Shin-Ichi Inoue, Mamoru Niikura, Kenji Yagita and Mohammed Essa Marghany TolbaPages 3048-3057 (10)

Abstract:


Malaria is one of the world’s most devastating diseases, particularly in the tropics. In humans, Plasmodium falciparum lives mainly within red blood cells, and malaria pathogenesis depends on the red blood cells being infected with the parasite. Nonesterified fatty acids (NEFAs), including cis-9-octadecenoic acid, and phospholipids have been critical for complete parasite growth in serum-free culture, although the efficacy of NEFAs in sustaining the growth of P. falciparum has varied markedly. Hexadecanoic acid and trans-9-octadecenoic acid have arrested development of the parasite, in association with down-regulation of genes encoding copper-binding proteins. Selective removal of Cu
+ ions has blockaded completely the ring–trophozoite–schizont progression of the parasite. The importance of copper homeostasis for the developmental progression of P. falciparum has been confirmed by inhibition of copper-binding proteins that regulate copper physiology and function by associating with copper ions. These data have provided strong evidence for a link between healthy copper homeostasis and successive developmental progression of P. falciparum. Perturbation of copper homeostasis may be, thus, instrumental in drug and vaccine development for the malaria medication. We review the importance of copper homeostasis in the asexual growth of P. falciparum in relation to NEFAs, copperbinding proteins, apoptosis, mitochondria, and gene expression.

Keywords:

Copper-binding protein, Copper homeostasis, Developmental arrest, Gene expression, Non-esterified fatty acids, Plasmodium falciparum, Copper ion.

Affiliation:

Division of Tropical Diseases and Parasitology, Department of Infectious Diseases, Kyorin University School of Medicine, Tokyo 181 8611, Japan.

Graphical Abstract:




For More Detail Please Visit Our Website Current Topics in Medicinal Chemistry




Monday, October 10, 2016

New Issue ::: Current Topics in Medicinal Chemistry, Volume 16 Issue 18



Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.
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Articles from the journal Current Topics in Medicinal Chemistry, Volume 16 Issue 18:

  • Editorial (Thematic Issue: Nanoinformatics to Organic Synthesis, ADMET Profiling, and Application of Nanomaterials in Medicinal Chemistry, Medicine, and Biotechnology)
  • Nano Particles: Emerging Warheads Against Bacterial Superbugs
  • The Glitter of Carbon Nanostructures in Hybrid/Composite Hydrogels for Medicinal Use
  • Advancements in Devices and Particle Engineering in Dry Powder Inhalation Technology
  • The Unexpected Advantages of Using D-Amino Acids for Peptide Self- Assembly into Nanostructured Hydrogels for Medicine
  • Biosynthesis of Fluorescent Bi2S3 Nanoparticles and their Application as Dual-Function SPECT-CT Probe for Animal Imaging
  • Development of Crystalline Cellulosic Fibres for Sustained Release of Drug
  • Biosynthesis of Anti-Proliferative Gold Nanoparticles Using Endophytic Fusarium oxysporum Strain Isolated from Neem (A. indica) Leaves
  • Synthesis of Gold Mediated Biocompatible Nanocomposite of Lactone Enriched Fraction from Sahadevi (Vernonia cinerea Lees): An Assessment of Antimalarial Potential
  • Development of Quercetin Based Nanodispersions
  • Development and Characterization of Cassia grandis and Bixa orellana Nanoformulations
For details on the articles, please visit this link :: http://bit.ly/1tllt9c
courtesy by: Bentham Insight

Tuesday, October 4, 2016

Podcast Integrin-Targeted Peptide/Peptidomimetic-Drug Conjugates: In-Depth Analysis of the Linker Technology

Integrin-Targeted Peptide/Peptidomimetic-Drug Conjugates: In-Depth Analysis of the Linker Technology


Podcast Nuclear Targeting of Gold Nanoparticles for Improved Therapeutics

 Nuclear Targeting of Gold Nanoparticles for Improved Therapeutics


Highlighted Article Flyer for the journal “Current Topics in Medicinal Chemistry”

Highlighted Article Flyer for the journal “Current Topics in Medicinal Chemistry”

courtesy by : Bentham Insight

Current Topics in Medicinal Chemistry



Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.
p

Articles from the journal Current Topics in Medicinal Chemistry, Volume 16 Issue 18:

  • Editorial (Thematic Issue: Nanoinformatics to Organic Synthesis, ADMET Profiling, and Application of Nanomaterials in Medicinal Chemistry, Medicine, and Biotechnology)
  • Nano Particles: Emerging Warheads Against Bacterial Superbugs
  • The Glitter of Carbon Nanostructures in Hybrid/Composite Hydrogels for Medicinal Use
  • Advancements in Devices and Particle Engineering in Dry Powder Inhalation Technology
  • The Unexpected Advantages of Using D-Amino Acids for Peptide Self- Assembly into Nanostructured Hydrogels for Medicine
  • Biosynthesis of Fluorescent Bi2S3 Nanoparticles and their Application as Dual-Function SPECT-CT Probe for Animal Imaging
  • Development of Crystalline Cellulosic Fibres for Sustained Release of Drug
  • Biosynthesis of Anti-Proliferative Gold Nanoparticles Using Endophytic Fusarium oxysporum Strain Isolated from Neem (A. indica) Leaves
  • Synthesis of Gold Mediated Biocompatible Nanocomposite of Lactone Enriched Fraction from Sahadevi (Vernonia cinerea Lees): An Assessment of Antimalarial Potential
  • Development of Quercetin Based Nanodispersions
  • Development and Characterization of Cassia grandis and Bixa orellana Nanoformulations
For details on the articles, please visit this link :: http://bit.ly/1tllt9c
courtesy by : Bentham Insight

Highlighted Article Flyer – Current Topics in Medicinal Chemistry Vol 16, Issue 20



courtesy by : Bentham Insight

Friday, August 12, 2016

Nuclear Targeting of Gold Nanoparticles for Improved Therapeutics



Saturday, June 25, 2016

Cellular Selenoprotein mRNA Tethering via Antisense Interactions with Ebola and HIV-1 mRNAs May Impact Host Selenium Biochemistry

Author(s):

Ethan Will Taylor, Jan A. Ruzicka, Lakmini Premadasa and Lijun ZhaoPages 1530-1535 (6)

Abstract:


Regulation of protein expression by non-coding RNAs typically involves effects on mRNA degradation and/or ribosomal translation. The possibility of virus-host mRNA-mRNA antisense tethering interactions (ATI) as a gain-of-function strategy, via the capture of functional RNA motifs, has not been hitherto considered. We present evidence that ATIs may be exploited by certain RNA viruses in order to tether the mRNAs of host selenoproteins, potentially exploiting the proximity of a captured host selenocysteine insertion sequence (SECIS) element to enable the expression of virally-encoded selenoprotein modules, via translation of in-frame UGA stop codons as selenocysteine. Computational analysis predicts thermodynamically stable ATIs between several widely expressed mammalian selenoprotein mRNAs (e.g., isoforms of thioredoxin reductase) and specific Ebola virus mRNAs, and HIV-1 mRNA, which we demonstrate via DNA gel shift assays. The probable functional significance of these ATIs is further supported by the observation that, in both viruses, they are located in close proximity to highly conserved in-frame UGA stop codons at the 3′ end of open reading frames that encode essential viral proteins (the HIV-1 nef protein and the Ebola nucleoprotein). Significantly, in HIV/AIDS patients, an inverse correlation between serum selenium and mortality has been repeatedly documented, and clinical benefits of selenium in the context of multi-micronutrient supplementation have been demonstrated in several well-controlled clinical trials. Hence, in the light of our findings, the possibility of a similar role for selenium in Ebola pathogenesis and treatment merits serious investigation.

Keywords:

Antisense, Ebola, mRNA, Selenium, Selenoprotein, HIV, Tethering, Thioredoxin reductase

Affiliation:

Dept. of Nanoscience, University of North Carolina at Greensboro, Joint School of Nanoscience and Nanoengineering, 2907 E. Gate City Blvd., Greensboro, NC 27401 USA

Graphical Abstract:



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Biomarkers in the Management of Difficult Asthma

Author(s):

Florence Schleich, Demarche Sophie and Louis RenaudPages 1561-1573 (13)

Abstract:


Difficult asthma is a heterogeneous disease of the airways including various types of bronchial inflammation and various degrees of airway remodeling. Therapeutic response of severe asthmatics can be predicted by the use of biomarkers of Type2-high or Type2-low inflammation. Based on sputum cell analysis, four inflammatory phenotypes have been described. As induced sputum is timeconsuming and expensive technique, surrogate biomarkers are useful in clinical practice.
Eosinophilic phenotype is likely to reflect ongoing adaptive immunity in response to allergen. Several biomarkers of eosinophilic asthma are easily available in clinical practice (blood eosinophils, serum IgE, exhaled nitric oxyde, serum periostin). Neutrophilic asthma is thought to reflect innate immune system activation in response to pollutants or infectious agents while paucigranulocytic asthma is thought to be not inflammatory and characterized by smooth muscle dysfunction. We currently lack of user-friendly biomarkers of neutrophilic asthma and airway remodeling.
In this review, we summarize the biomarkers available for the management of difficult asthma.

Keywords:

Airway remodeling, Biomarker, Difficult asthma, Inflammation, Phenotype, Severe.

Affiliation:

Respiratory Medicine, CHU Sart-Tilman B35, 4000 Li├Ęge, Belgium.

Graphical Abstract:



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Linking Biosynthetic Gene Clusters to their Metabolites via Pathway- Targeted Molecular Networking

Author(s):

Eric P. Trautman and Jason M. CrawfordPages 1705-1716 (12)

Abstract:


The connection of microbial biosynthetic gene clusters to the small molecule metabolites they encode is central to the discovery and characterization of new metabolic pathways with ecological and pharmacological potential. With increasing microbial genome sequence information being deposited into publicly available databases, it is clear that microbes have the coding capacity for many more biologically active small molecules than previously realized. Of increasing interest are the small molecules encoded by the human microbiome, as these metabolites likely mediate a variety of currently uncharacterized human-microbe interactions that influence health and disease. In this mini-review, we describe the ongoing biosynthetic, structural, and functional characterizations of the genotoxic colibactin pathway in gut bacteria as a thematic example of linking biosynthetic gene clusters to their metabolites. We also highlight other natural products that are produced through analogous biosynthetic logic and comment on some current disconnects between bioinformatics predictions and experimental structural characterizations. Lastly, we describe the use of pathway-targeted molecular networking as a tool to characterize secondary metabolic pathways within complex metabolomes and to aid in downstream metabolite structural elucidation efforts.

Keywords:

Biosynthesis, Colibactin, Pathway-Targeted Molecular Networking

Affiliation:

Department of Chemistry, Faculty of Yale University, P.O. Box: 27392, West Haven, CT, 06516, USA

Graphical Abstract:



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The Unexpected Advantages of Using D-Amino Acids for Peptide Self- Assembly into Nanostructured Hydrogels for Medicine

Author(s):

Michele Melchionna, Katie E. Styan and Silvia MarchesanPages 2009-2018 (10)

Abstract:


Self-assembled peptide hydrogels have brought innovation to the medicinal field, not only as responsive biomaterials but also as nanostructured therapeutic agents or as smart drug delivery systems. D-amino acids are typically introduced to increase the peptide enzymatic stability. However, there are several reports of unexpected effects on peptide conformation, self-assembly behavior, cytotoxicity and even therapeutic activity. This mini-review discusses all the surprising twists of heterochiral self-assembled peptide hydrogels, and delineates emerging key findings to exploit all the benefits of D-amino acids in this novel medicinal area.

Keywords:

Chirality, D-Amino acids, Enantiomers, Heterochiral, Hydrogels, Nanomaterials, Peptides, Self-assembly.

Affiliation:

Department of Chemical and Pharmaceutical Sciences, University of Trieste, 34127 Trieste, Italy.

Graphical Abstract:



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