FRET-Based Probe for High-Throughput DNA Intercalator Drug Discovery and In Vivo Imaging

ACS Sensors ◽  
2021 ◽  
Author(s):  
Chandrashekhar U. Murade ◽  
Samata Chaudhuri ◽  
Ibtissem Nabti ◽  
Hala Fahs ◽  
Fatima S. M. Refai ◽  
...  
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
In Vivo Imaging ◽  
Dna Intercalator

scholarly journals A FRET-based Probe for High Throughput DNA Intercalator Drug Discovery and In Vivo Imaging

2020 ◽  
Vol 118 (3) ◽  
pp. 315a
Author(s):  
Chandrashekhar U. Murade ◽  
Samata Chadhuri ◽  
Ibtissem Nabita ◽  
Hala Fahs ◽  
Fathima Refai ◽  
...  
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
In Vivo Imaging ◽  
Dna Intercalator

scholarly journals Meeting Report: High-Throughput Technologies for In Vivo Imaging Agents

2005 ◽  
Vol 4 (2) ◽  
pp. 153535002005051 ◽  
Author(s):  
Robert J. Gillies ◽  
John M. Hoffman ◽  
Kit S. Lam ◽  
Anne E. Menkens ◽  
David R. Piwnica-Worms ◽  
...  
Keyword(s):  
High Throughput ◽  
In Vivo Imaging ◽  
High Throughput Screening ◽  
Imaging Agents ◽  
Meeting Report ◽  
Screening Methods ◽  
Pharmacological Properties ◽  
Drug Candidates ◽  
Good Imaging

Combinatorial chemistry and high-throughput screening have become standard tools for discovering new drug candidates with suitable pharmacological properties. Now, those same technologies are starting to be applied to the problem of discovering novel in vivo imaging agents. Important differences in the biological and pharmacological properties needed for imaging agents, compared to those for a therapeutic agent, require new screening methods that emphasize those characteristics, such as optimized residence time and tissue specificity, that make for a good imaging agent candidate.

scholarly journals Live Cell in Vitro and in Vivo Imaging Applications: Accelerating Drug Discovery

Pharmaceutics ◽  
2011 ◽  
Vol 3 (2) ◽  
pp. 141-170 ◽  
Author(s):  
Beverley Isherwood ◽  
Paul Timpson ◽  
Ewan J McGhee ◽  
Kurt I Anderson ◽  
Marta Canel ◽  
...  
Keyword(s):  
Drug Discovery ◽  
In Vivo Imaging ◽  
Live Cell

scholarly journals Recent Advances in In-Vitro Assays for Type 2 Diabetes Mellitus: An Overview

2020 ◽  
Vol 16 (1) ◽  
pp. 13-23
Author(s):  
Nazmina Vhora ◽  
Ujjal Naskar ◽  
Aishwarya Hiray ◽  
Abhijeet S. Kate ◽  
Alok Jain
Keyword(s):  
Type 2 Diabetes ◽  
Drug Discovery ◽  
High Throughput ◽  
High Throughput Screening ◽  
Antidiabetic Activity ◽  
Screening Methods ◽  
Selection Of

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.

scholarly journals High Throughput Screening of Pharmacokinetics and Metabolism in Drug Discovery (II) —Investigation on In vitro and In vivo Correlation in Drug Metabolism Screening—

2005 ◽  
Vol 125 (1) ◽  
pp. 131-139 ◽  
Author(s):  
Hiroshi KOMURA ◽  
Kenichi MATSUDA ◽  
Yukie SHIGEMOTO ◽  
Iichiro KAWAHARA ◽  
Rieko ANO ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Drug Metabolism ◽  
High Throughput ◽  
High Throughput Screening

scholarly journals An In Vivo Platform for Rapid High-Throughput Antitubercular Drug Discovery

Cell Reports ◽  
2012 ◽  
Vol 2 (1) ◽  
pp. 175-184 ◽  
Author(s):  
Kevin Takaki ◽  
Christine L. Cosma ◽  
Mark A. Troll ◽  
Lalita Ramakrishnan
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
Antitubercular Drug

scholarly journals A cross-species drug discovery pipeline to identify and validate new treatments for osteosarcoma

2020 ◽  
Author(s):  
Jason A. Somarelli ◽  
Gabrielle Rupprecht ◽  
Erdem Altunel ◽  
Etienne M. Flamant ◽  
Sneha Rao ◽  
...  
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
Nuclear Export ◽  
Complex Disease ◽  
Rare Cancers ◽  
Synergistic Cytotoxicity ◽  
New Treatments ◽  
Discovery Pipeline

AbstractPurposeOsteosarcoma is a rare but aggressive bone cancer that occurs primarily in children. Like other rare cancers, treatment advances for osteosarcoma have stagnated, with little improvement in survival for the past several decades. Developing new treatments has been hampered by extensive genomic heterogeneity and limited access to patient samples to study the biology of this complex disease.Experimental designTo overcome these barriers, we combined the power of comparative oncology with patient-derived models of cancer and high-throughput chemical screens in a cross-species drug discovery pipeline.ResultsCoupling in vitro high-throughput drug screens on low-passage and established cell lines with in vivo validation in patient-derived xenografts we identify the proteasome and CRM1 nuclear export pathways as therapeutic sensitivities in osteosarcoma, with dual inhibition of these pathways inducing synergistic cytotoxicity.ConclusionsThese collective efforts provide an experimental framework and set of new tools for osteosarcoma and other rare cancers to identify and study new therapeutic vulnerabilities.

scholarly journals An orthotopic glioblastoma animal model suitable for high-throughput screenings

2018 ◽  
Vol 20 (11) ◽  
pp. 1475-1484 ◽  
Author(s):  
Linda Pudelko ◽  
Steven Edwards ◽  
Mirela Balan ◽  
Daniel Nyqvist ◽  
Jonathan Al-Saadi ◽  
...  
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
Large Scale ◽  
Light Sheet ◽  
Time Lapse ◽  
Zebrafish Model ◽  
Light Sheet Microscopy ◽  
Disease Biology ◽  
Vertebrate Model

Abstract Background Glioblastoma (GBM) is an aggressive form of brain cancer with poor prognosis. Although murine animal models have given valuable insights into the GBM disease biology, they cannot be used in high-throughput screens to identify and profile novel therapies. The only vertebrate model suitable for large-scale screens, the zebrafish, has proven to faithfully recapitulate biology and pathology of human malignancies, and clinically relevant orthotopic zebrafish models have been developed. However, currently available GBM orthotopic zebrafish models do not support high-throughput drug discovery screens. Methods We transplanted both GBM cell lines as well as patient-derived material into zebrafish blastulas. We followed the behavior of the transplants with time-lapse microscopy and real-time in vivo light-sheet microscopy. Results We found that GBM material transplanted into zebrafish blastomeres robustly migrated into the developing nervous system, establishing an orthotopic intracranial tumor already 24 hours after transplantation. Detailed analysis revealed that our model faithfully recapitulates the human disease. Conclusion We have developed a robust, fast, and automatable transplantation assay to establish orthotopic GBM tumors in zebrafish. In contrast to currently available orthotopic zebrafish models, our approach does not require technically challenging intracranial transplantation of single embryos. Our improved zebrafish model enables transplantation of thousands of embryos per hour, thus providing an orthotopic vertebrate GBM model for direct application in drug discovery screens.

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