The design of pharmacokinetic studies to support drug discovery: The selection of the optimum number of animals for a study

2003 ◽  
Vol 28 (3) ◽  
pp. 233-235 ◽  
Author(s):  
Brian Law ◽  
Dave Temesi
2021 ◽  
Vol 22 (14) ◽  
pp. 7560
Author(s):  
Julie A. Tucker ◽  
Mathew P. Martin

This special issue on Advances in Kinase Drug Discovery provides a selection of research articles and topical reviews covering all aspects of drug discovery targeting the phosphotransferase enzyme family [...]


2012 ◽  
Vol 17 (4) ◽  
pp. 542-549 ◽  
Author(s):  
Maria Cândida Monteiro ◽  
Mercedes de la Cruz ◽  
Juan Cantizani ◽  
Catalina Moreno ◽  
José R. Tormo ◽  
...  

Natural products are an inexhaustible source for drug discovery. However, the validation and selection of primary screening assays are vital to guarantee a selection of extracts or molecules with relevant pharmacological action and worthy of following up. The assay must be rapid, simple, easy to implement, and produce quick results and preferably at a low cost. In this work, we developed and validated a colorimetric microtiter assay using the resazurin viability dye. The parameters of the resazurin method for high-throughput screening (HTS) using natural extracts against Aspergillus fumigatus were optimized and set up. The extracts plus RPMI-1640 modified medium containing the spores and 0.002% resazurin were added per well. The fluorescence was read after 24 to 30 h of incubation. The resazurin proved to be as suitable as Alamar Blue for determining the minimal inhibitory concentration of different antifungals against A. fumigatus and effective to analyze fungicidal and fungistatic compounds. An HTS of 12 000 microbial extracts was carried out against two A. fumigatus strains, and 2.7% of the extracts displayed antifungal activity. Our group has been the first to use this methodology for screening a collection of natural extracts to identify compounds with antifungal activity against the medically important human pathogen A. fumigatus.


2007 ◽  
Vol 21 (4) ◽  
pp. 167-188 ◽  
Author(s):  
Yovani Marrero-Ponce ◽  
Mahmud Tareq Hassan Khan ◽  
Gerardo M. Casañola-Martín ◽  
Arjumand Ather ◽  
Mukhlis N. Sultankhodzhaev ◽  
...  

2016 ◽  
Vol 5 (1) ◽  
pp. 29-41 ◽  
Author(s):  
Suzanne I.S. Mosely ◽  
John E. Prime ◽  
Richard C.A. Sainson ◽  
Jens-Oliver Koopmann ◽  
Dennis Y.Q. Wang ◽  
...  

2011 ◽  
Vol 03 (11) ◽  
Author(s):  
Nishant Toomula ◽  
Sathish Kumar D ◽  
Arun Kumar ◽  
Phaneendra M

2020 ◽  
Vol 16 (1) ◽  
pp. 13-23
Author(s):  
Nazmina Vhora ◽  
Ujjal Naskar ◽  
Aishwarya Hiray ◽  
Abhijeet S. Kate ◽  
Alok Jain

BACKGROUND: A higher rate of attenuation of molecules in drug discovery has enabled pharmaceutical companies to enhance the efficiency of their hit identification and lead optimization. Selection and development of appropriate in-vitro and in-vivo strategies may improve this process as primary and secondary screening utilize both strategies. In-vivo approaches are too relentless and expensive for assessing hits. Therefore, it has become indispensable to develop and implement suitable in-vitro screening methods to execute the required activities and meet the respective targets. However, the selection of an appropriate in-vitro assay for specific evaluation of cellular activity is no trivial task. It requires thorough investigation of the various parameters involved. AIM: In this review, we aim to discuss in-vitro assays for type 2 diabetes (T2D), which have been utilized extensively by researchers over the last five years, including target-based, non-target based, low-throughput, and high-throughput screening assays. METHODS: The literature search was conducted using databases including Scifinder, PubMed, ScienceDirect, and Google Scholar to find the significant published articles. DISCUSSION and CONCLUSION: The accuracy and relevance of in-vitro assays have a significant impact on the drug discovery process for T2D, especially in assessing the antidiabetic activity of compounds and identifying the site of effect in high-throughput screening. The report reviews the advantages, limitations, quality parameters, and applications of the probed invitro assays, and compares them with one another to enable the selection of the optimal method for any purpose. The information on these assays will accelerate numerous procedures in the drug development process with consistent quality and accuracy.


Author(s):  
Naomi Clapp ◽  
Augustin Amour ◽  
Wendy C. Rowan ◽  
Pelin L. Candarlioglu

Organ-on-chip (OoC) systems are in vitro microfluidic models that mimic the microstructures, functions and physiochemical environments of whole living organs more accurately than two-dimensional models. While still in their infancy, OoCs are expected to bring ground-breaking benefits to a myriad of applications, enabling more human-relevant candidate drug efficacy and toxicity studies, and providing greater insights into mechanisms of human disease. Here, we explore a selection of applications of OoC systems. The future directions and scope of implementing OoCs across the drug discovery process are also discussed.


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