Assay development in leishmaniasis drug discovery: a comprehensive review

Author(s):  
Bilal Zulfiqar ◽  
Vicky. M. Avery
2020 ◽  
Vol 2020 ◽  
pp. 1-41
Author(s):  
Aida Rodriguez-Garcia ◽  
Jacqueline Oliva-Ramirez ◽  
Claudia Bautista-Flores ◽  
Samira Hosseini

The past few decades have shown significant advancement as complex in vitro humanized systems have substituted animal trials and 2D in vitro studies. 3D humanized platforms mimic the organs of interest with their stimulations (physical, electrical, chemical, and mechanical). Organ-on-chip devices, including in vitro modelling of 3D organoids, 3D microfabrication, and 3D bioprinted platforms, play an essential role in drug discovery, testing, and assessment. In this article, a thorough review is provided of the latest advancements in the area of organ-on-chip devices targeting liver, kidney, lung, gut, heart, skin, and brain mimicry devices for drug discovery, development, and/or assessment. The current strategies, fabrication methods, and the specific application of each device, as well as the advantages and disadvantages, are presented for each reported platform. This comprehensive review also provides some insights on the challenges and future perspectives for the further advancement of each organ-on-chip device.


Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1629 ◽  
Author(s):  
Johannes Ottl ◽  
Lukas Leder ◽  
Jonas V. Schaefer ◽  
Christoph E. Dumelin

The scope of targets investigated in pharmaceutical research is continuously moving into uncharted territory. Consequently, finding suitable chemical matter with current compound collections is proving increasingly difficult. Encoded library technologies enable the rapid exploration of large chemical space for the identification of ligands for such targets. These binders facilitate drug discovery projects both as tools for target validation, structural elucidation and assay development as well as starting points for medicinal chemistry. Novartis internalized two complementing encoded library platforms to accelerate the initiation of its drug discovery programs. For the identification of low-molecular weight ligands, we apply DNA-encoded libraries. In addition, encoded peptide libraries are employed to identify cyclic peptides. This review discusses how we apply these two platforms in our research and why we consider it beneficial to run both pipelines in-house.


RSC Advances ◽  
2015 ◽  
Vol 5 (41) ◽  
pp. 32376-32415 ◽  
Author(s):  
Jaiprakash N. Sangshetti ◽  
Firoz A. Kalam Khan ◽  
Abhishek A. Kulkarni ◽  
Rohidas Arote ◽  
Rajendra H. Patil

This review covers the current aspects of leishmaniasis including marketed drugs, new antileishmanial agents, and possible drug targets of antileishmanial agents.


ChemInform ◽  
2015 ◽  
Vol 46 (28) ◽  
pp. no-no
Author(s):  
Jaiprakash N. Sangshetti ◽  
Firoz A. Kalam Khan ◽  
Abhishek A. Kulkarni ◽  
Rohidas Arote ◽  
Rajendra H. Patil

Metabolites ◽  
2019 ◽  
Vol 9 (11) ◽  
pp. 258 ◽  
Author(s):  
Uttpal Anand ◽  
Nadia Jacobo-Herrera ◽  
Ammar Altemimi ◽  
Naoufal Lakhssassi

The war on multidrug resistance (MDR) has resulted in the greatest loss to the world’s economy. Antibiotics, the bedrock, and wonder drug of the 20th century have played a central role in treating infectious diseases. However, the inappropriate, irregular, and irrational uses of antibiotics have resulted in the emergence of antimicrobial resistance. This has resulted in an increased interest in medicinal plants since 30–50% of current pharmaceuticals and nutraceuticals are plant-derived. The question we address in this review is whether plants, which produce a rich diversity of secondary metabolites, may provide novel antibiotics to tackle MDR microbes and novel chemosensitizers to reclaim currently used antibiotics that have been rendered ineffective by the MDR microbes. Plants synthesize secondary metabolites and phytochemicals and have great potential to act as therapeutics. The main focus of this mini-review is to highlight the potential benefits of plant derived multiple compounds and the importance of phytochemicals for the development of biocompatible therapeutics. In addition, this review focuses on the diverse effects and efficacy of herbal compounds in controlling the development of MDR in microbes and hopes to inspire research into unexplored plants with a view to identify novel antibiotics for global health benefits.


RSC Advances ◽  
2020 ◽  
Vol 10 (47) ◽  
pp. 28287-28299
Author(s):  
Maryam S. Hosseini-Zare ◽  
Ramasamy Thilagavathi ◽  
Chelliah Selvam

Since the coronaviruses that cause COVID-19 and SARS-CoV-1 share 80% structural similarity, we present a comprehensive review of the diverse molecular inhibitors of SARS-CoV-1. This will help to accelerate drug discovery for deadly coronavirus diseases.


ADMET & DMPK ◽  
2019 ◽  
Vol 7 (4) ◽  
pp. 222-241
Author(s):  
Geoffrey Holdgate ◽  
Kevin Embrey ◽  
Alexander Milbradt ◽  
Gareth Davies

Biophysical methods such as mass spectrometry, surface plasmon resonance, nuclear magnetic resonance, and both differential scanning isothermal titration calorimetry are now well established as key components of the early drug discovery process. These approaches are used successfully for a range of activities, including assay development, primary screening, hit confirmation and detailed mechanistic characterisation of compound binding. Matching the speed, sensitivity and information content of the various techniques to the generation of critical data and information required at each phase of the drug discovery process has been key. This review describes the framework by which these methods have been applied in the drug discovery process and provides case studies to exemplify the impact.


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