LYMPHATIC FILARIASIS Therapeutic Arsenal and Drug Discovery for Lymphatic Filariasis from a Synthetic Point of View

2014 ◽  
pp. 149-171
Keyword(s):  
Drug Discovery ◽  
Lymphatic Filariasis ◽  
Point Of View

scholarly journals Aptamers in the Treatment of Bacterial Infections: Problems and Prospects

2016 ◽  
Vol 71 (5) ◽  
pp. 350-358
Author(s):  
N. A. Zeninskaya ◽  
A. V. Kolesnikov ◽  
A. K. Ryabko ◽  
I. G. Shemyakin ◽  
I. A. Dyatlov ◽  
...  
Keyword(s):  
Drug Discovery ◽  
High Throughput Screening ◽  
Bacterial Infections ◽  
Point Of View ◽  
Aptamer Selection ◽  
Wide Range ◽  
Therapeutic Molecules ◽  
Molecular Selection ◽  
The Stability

Aptamers are short single-stranded oligonucleotides which are selected via targeted chemical evolution in vitro to bind a molecular target of interest. The aptamer selection technology is designated as SELEX (Systematic evolution of ligands by exponential enrichment). SELEX enables isolation of oligonucleotide aptamers binding a wide range of targets of interest with little respect for their nature and molecular weight. A number of applications of aptamer selection were developed ranging from biosensor technologies to antitumor drug discovery. First aptamer-based pharmaceutical (Macugen) was approved by FDA for clinical use in 2004, and since then more than ten aptamer-based drugs undergo various phases of clinical trials. From the medicinal chemist’s point of view, aptamers represent a new class of molecules suitable for the development of new therapeutics. Due to the stability, relative synthesis simplicity, and development of advanced strategies of target specific molecular selection, aptamers attract increased attention of drug discovery community. Difficulties of the development of next-generation antibiotics basing on the conventional basis of combinatorial chemistry and high-throughput screening have also amplified the interest to aptamer-based therapeutic candidates. The present article reviews the investigations focused on the development of antibacterial aptamers and discusses the potential and current limitations of the use of this type of therapeutic molecules.

Relevance of Molecular Docking Studies in Drug Designing

2020 ◽  
Vol 15 (4) ◽  
pp. 270-278
Author(s):  
Ritu Jakhar ◽  
Mehak Dangi ◽  
Alka Khichi ◽  
Anil Kumar Chhillar
Keyword(s):  
Molecular Docking ◽  
Drug Discovery ◽  
3D Structure ◽  
Docking Studies ◽  
Point Of View ◽  
Compound Libraries ◽  
Drug Discovery Program ◽  
Protein Ensembles ◽  
Drug Receptor ◽  
Dynamic Docking

Molecular Docking is used to positioning the computer-generated 3D structure of small ligands into a receptor structure in a variety of orientations, conformations and positions. This method is useful in drug discovery and medicinal chemistry providing insights into molecular recognition. Docking has become an integral part of Computer-Aided Drug Design and Discovery (CADDD). Traditional docking methods suffer from limitations of semi-flexible or static treatment of targets and ligand. Over the last decade, advances in the field of computational, proteomics and genomics have also led to the development of different docking methods which incorporate protein-ligand flexibility and their different binding conformations. Receptor flexibility accounts for more accurate binding pose predictions and a more rational depiction of protein binding interactions with the ligand. Protein flexibility has been included by generating protein ensembles or by dynamic docking methods. Dynamic docking considers solvation, entropic effects and also fully explores the drug-receptor binding and recognition from both energetic and mechanistic point of view. Though in the fast-paced drug discovery program, dynamic docking is computationally expensive but is being progressively used for screening of large compound libraries to identify the potential drugs. In this review, a quick introduction is presented to the available docking methods and their application and limitations in drug discovery.

Phosphodiesterase 10 Inhibitors - Novel Perspectives for Psychiatric and Neurodegenerative Drug Discovery

2018 ◽  
Vol 25 (29) ◽  
pp. 3455-3481 ◽  
Author(s):  
Agnieszka Zagorska ◽  
Anna Partyka ◽  
Adam Bucki ◽  
Alicja Gawalskax ◽  
Anna Czopek ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Neurodegenerative Diseases ◽  
Medicinal Chemistry ◽  
Point Of View ◽  
Medium Spiny Neurons ◽  
Lead Discovery ◽  
Spiny Neurons ◽  
Wide Range ◽  
The Brain

Background: The phosphodiesterase 10 (PDE10) family, identified in 1999, is mainly expressed in the brain, particularly in the striatum, within the medium spiny neurons, nucleus accumbens, and olfactory tubercle. Inhibitors of PDE10 (PDE10-Is) are a conceptually rational subject for medicinal chemistry with potential use in the treatment of psychiatric and neurodegenerative diseases. Objective: This review is based on peer-reviewed published articles, and summarizes the cellular and molecular biology of PDE10 as a rational target for psychiatric and neurodegenerative drug discovery. Here, we present the classification of PDE10-Is from a medicinal chemistry point of view across a wide range of different, drug-like chemotypes starting from theophylline and caffeine analogs, papaverine and dimethoxy catechol type PDE10-Is, TP-10, MP-10, MP-10/papaverine/quinazoline series inhibitors, and ending with the newest inhibitors obtained from fragment-based lead discovery (FBLD). The authors have collated recent research on inhibition of PDE10A as a promising therapeutic strategy for psychiatric and neurodegenerative diseases, based on its efficacy in animal models of schizophrenia, Parkinson’s, Huntington’s, and Alzheimer’s diseases. This review also presents pharmacological data on PDE10-Is as possible therapeutics for the treatment of cognitive deficits, obesity and depression. Moreover, it summarizes the current strategies for PDE10-Is drug discovery based on the results of clinical trials. The authors also present the latest studies on crystal structures of PDE10 complexes with novel inhibitors.

scholarly journals TRADITIONAL AND INDIGENOUS PRACTICES OF SOME MEDICINAL PLANTS AS IMMUNITY BOOSTERS BY FOLKLORE OF MANDI DISTRICT, HIMACHAL PRADESH

2020 ◽  
pp. 56-64
Author(s):  
Sharma Ritu ◽  
Goraya G.S ◽  
Seth M.K
Keyword(s):  
Drug Discovery ◽  
Medicinal Plants ◽  
Himachal Pradesh ◽  
Point Of View ◽  
Suitable Habitat ◽  
Herbal Drug ◽  
Herbal Plants ◽  
The Rich ◽  
Indigenous Uses ◽  
Novel Drug

Himachal Pradesh being a hilly State is one of the top repositories of various herbal plants of medicinal aspects. District Mandi, popular as Varanasi of Hills, is one of the twelve districts, with great variations in elevation which provide a suitable habitat for the rich biodiversity of flora and fauna. The present paper aimed to document indigenous uses of some therapeutically significant plants which have been utilized by folklore to improve their immunity and to cure immunity-related diseases like cough, cold, and allergies. Indeed, even today when the Corona pandemic has influenced the whole world gravely, provincial fables of the State have kept themselves safe and have indicated their confidence on these plant assets which are being utilized by their predecessors for ages. Herein 21 species belonging to 17 families used as immunity boosters are compiled (8 herbs, 6 shrubs, 6 trees, 1 climber) used by folklore to enhance their immunity. Documentation of traditional knowledge is the need of the hour as it the base of the Naturopathy and Ayurveda. The documentation of the traditional medicinal knowledge will give another point of view to herbal drug researchers for extending and improving the utilization of botanical drugs and their therapeutic applications. Plant-based natural products offer an infinite source of compounds to help to design the pharmacologically important molecular products and novel drug discovery as well.

The Geosciences Applied to Lunar Exploration

1962 ◽  
Vol 14 ◽  
pp. 169-257 ◽  
Author(s):  
J. Green
Keyword(s):  
Lunar Surface ◽  
Probable Mechanism ◽  
Point Of View ◽  
Lunar Exploration ◽  
Geological Model ◽  
Apply Geophysics ◽  
Surface Features ◽  
The Impact

The term geo-sciences has been used here to include the disciplines geology, geophysics and geochemistry. However, in order to apply geophysics and geochemistry effectively one must begin with a geological model. Therefore, the science of geology should be used as the basis for lunar exploration. From an astronomical point of view, a lunar terrain heavily impacted with meteors appears the more reasonable; although from a geological standpoint, volcanism seems the more probable mechanism. A surface liberally marked with volcanic features has been advocated by such geologists as Bülow, Dana, Suess, von Wolff, Shaler, Spurr, and Kuno. In this paper, both the impact and volcanic hypotheses are considered in the application of the geo-sciences to manned lunar exploration. However, more emphasis is placed on the volcanic, or more correctly the defluidization, hypothesis to account for lunar surface features.

How a sheperd guides a sheep herd?

1984 ◽  
Vol 75 ◽  
pp. 331-337
Author(s):  
Richard Greenberg
Keyword(s):  
Point Of View ◽  
Single Ring ◽  
Damping Effects ◽  
Ring Particle

ABSTRACTThe mechanism by which a shepherd satellite exerts a confining torque on a ring is considered from the point of view of a single ring particle. It is still not clear how one might most meaningfully include damping effects and other collisional processes into this type of approach to the problem.

The growth of mica polytypes as studied by conventional and high-resolution TEM

1983 ◽  
Vol 41 ◽  
pp. 174-177
Author(s):  
A. Baronnet ◽  
M. Amouric
Keyword(s):  
Water Pressure ◽  
Point Of View ◽  
Temperature Fields ◽  
Natural Occurrence ◽  
Growth Mechanisms ◽  
Long Period ◽  
High Resolution Tem ◽  
Layer Stacking ◽  
Experimental Works ◽  
Potential Use

The origin of mica polytypes has long been a challenging problem for crystal- lographers, mineralogists and petrologists. From the petrological point of view, interest in this field arose from the potential use of layer stacking data to furnish further informations about equilibrium and/or kinetic conditions prevailing during the crystallization of the widespread mica-bearing rocks. From the compilation of previous experimental works dealing with the occurrence domains of the various mica "polymorphs" (1Mr, 1M, 2M1, 2M2 and 3T) within water-pressure vs temperature fields, it became clear that most of these modifications should be considered as metastable for a fixed mica species. Furthermore, the natural occurrence of long-period (or complex) polytypes could not be accounted for by phase considerations. This highlighted the need of a more detailed kinetic approach of the problem and, in particular, of the role growth mechanisms of basal faces could play in this crystallographic phenomenon.

Radiation Damage in Ceramics

1982 ◽  
Vol 40 ◽  
pp. 600-603
Author(s):  
T. E. Mitchell ◽  
M. R. Pascucci ◽  
R. A. Youngman
Keyword(s):  
Radiation Damage ◽  
Outer Space ◽  
Point Of View ◽  
Nuclear Waste Storage ◽  
Waste Storage ◽  
Storage Media ◽  
Transmission Electron ◽  
Fundamental Point ◽  
Small Defect ◽  
Present Understanding

1. Introduction. Studies of radiation damage in ceramics are of interest not only from a fundamental point of view but also because it is important to understand the behavior of ceramics in various practical radiation enyironments- fission and fusion reactors, nuclear waste storage media, ion-implantation devices, outer space, etc. A great deal of work has been done on the spectroscopy of point defects and small defect clusters in ceramics, but relatively little has been performed on defect agglomeration using transmission electron microscopy (TEM) in the same kind of detail that has been so successful in metals. This article will assess our present understanding of radiation damage in ceramics with illustrations using results obtained from the authors' work.

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