Overview of High‐Throughput Screening

Entzeroth, Michael; Flotow, Horst; Condron, Peter

doi:10.1002/0471141755.ph0904s44

Cited by 62 publications

(35 citation statements)

References 127 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Zebra fish embryos have been successfully used for this kind of assay [7]. Other commonly used assays are second messenger assays that monitor changes in signal transduction and cell proliferation assays that result in changes in growth rate of cells [5]. Biochemical assays are another kind of assay used in HTS.…”

Section: Assay Development and Verificationmentioning

confidence: 99%

“…Commonly used ones are fluorescence resonance energy transfer (FRET), fluorescence polarization (FP), homogeneous time resolved fluorescence (HTRF), etc. [5]. A comparison of cell based and biochemical assays has been reviewed by Moore & Rees [8].…”

Section: Assay Development and Verificationmentioning

confidence: 99%

“…An assay is then developed that can be used to screen small molecule chemical libraries The whole process of HTS can be divided into steps of target identification, assay design, primary and secondary screens, data analysis and identification of hits (Figure 1). The role of HTS is not only limited to identifying new compounds but is also useful in assaying current drugs and their derivatives to improve activity and functioning [5]. With advancement in the human genome project and synthesis of new chemical compounds, the role of HTS has become even more important in the fight against cancer.…”

Section: Introductionmentioning

confidence: 99%

“…The role of HTS is not only limited to identifying new compounds but is also useful in assaying current drugs and their derivatives to improve activity and functioning [5]. With advancement in the human genome project and synthesis of new chemical compounds, the role of HTS has become even more important in the fight against cancer.…”

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

High Throughput Screening of Small Molecule Library: Procedure, Challenges and Future

Shukla¹

2016

JCPCR

View full text Add to dashboard Cite

High-throughput screening (HTS) of small molecules is used to identify and characterize chemical compounds based on their response on particular assays. The screened compounds can be further used as tools to study complex molecular pathways involved in progression of cancers and potential candidates can be further developed as drugs. Testing of vast number of compounds and fast readout technologies for assays in a timely manner has made this procedure a popular drug-discovery process, which is widely used in the pharmaceutical industry. However, the procedure of screening is a multi-step process and is prone to give false positive and false negative results. Assurance of quality and good analysis of results play critical role in finding a true product. Technological hardware like robotic plate handling is critical for the procedure. Reagents like antibodies and recombinant proteins can also make the whole procedure very expensive. Increased number of available compounds and molecular targets has raised the requirements for even faster procedures, more sensitive assays to run and even smaller sample size assays for screening. Development of new methods like Droplet-based cell encapsulation technology has given hope for a better future of HTS. Keywords: High-throughput screening (HTS); Small molecules; Target identification; Assay design IntroductionCancer kills around 7.6 million people worldwide every year and about a half million people in the US annually. Early detection and more effective chemotherapy have improved cure rate among patients. However, patients diagnosed with advanced stage cancers still have very few options for treatment. It has been shown that there are short and long term adverse effects of chemotherapy. Both adult and pediatric cancer survivors face significant health burdens including but not limited to impaired end-organ function, risk of secondary cancers and shortened life expectancies [1,2].Development of personalized medicine strategy is becoming more popular. It focuses on identifying drugs that can target a molecular pathway or more specifically a protein involved in an uncontrolled or disrupted signaling pathway leading to the progression of particular cancer. Genetics studies are confirming addictions and weaknesses of cancer cells on such pathways and specific molecules. With this approach, normal tissues are spared from getting targeted by toxic chemotherapies.Drug discovery programs start to find a cure for a disease, which does not have suitable treatment available. Data generated by primary research suggest involvement of specific proteins in the progression of diseases and can be used as target for drug development [3]. An assay is then developed that can be used to screen small molecule chemical libraries The whole process of HTS can be divided into steps of target identification, assay design, primary and secondary screens, data analysis and identification of hits (Figure 1). The role of HTS is not only limited to identifying new compounds but is also useful in ass...

show abstract

Section: Assay Development and Verificationmentioning

confidence: 99%

Section: Assay Development and Verificationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

High Throughput Screening of Small Molecule Library: Procedure, Challenges and Future

Shukla¹

2016

JCPCR

View full text Add to dashboard Cite

show abstract

“…An example of a strategy is utilization of a longer emission half life following excitation while maintaining high control in signal collection (18) as well as the measurement of a fluorescent signal at a shorter emission wavelength than that of the excitation (19).…”

Section: Sensitivitymentioning

confidence: 99%

Ligand Binding Assays in the 21st Century Laboratory: Platforms

Spriggs

Zhong

Safavi

et al. 2012

AAPS J

View full text Add to dashboard Cite

Array‐Based High‐Throughput Screening in Mouse Embryonic Stem Cells with shRNAs

Wang

Lin

et al. 2013

CP Stem Cell Biology

View full text Add to dashboard Cite

High‐throughput short‐hairpin RNA (shRNA) lentivirus screening is a powerful tool for identifying multiple functional regulators in embryonic stem cells (ESCs). shRNA libraries can efficiently down‐regulate target genes persistently with high efficiency. The concurrent measurement of relative cell number by alamarBlue (AB) assay and undifferentiated ESC markers via an alkaline phosphatase (ALP) activity assay in the same cell culture well provides an efficient and economical way to pinpoint factors crucial for ESC pluripotency and/or expansion. Most of the renewal pathways affect ALP activity. Thus, multiple positive and negative regulators can be identified by this method. In addition, morphological changes and/or the expression levels of specific pluripotency or differentiation markers examined by immunofluorescence can be used as secondary screens for target‐gene selection. In summary, we describe an efficient way to identify multiple regulators of ESC renewal using shRNAs. Curr. Protoc. Stem Cell Biol. 26:5C.3.1‐5C.3.19. © 2013 by John Wiley & Sons, Inc.

show abstract

Overview of High‐Throughput Screening

Cited by 62 publications

References 127 publications

High Throughput Screening of Small Molecule Library: Procedure, Challenges and Future

High Throughput Screening of Small Molecule Library: Procedure, Challenges and Future

Ligand Binding Assays in the 21st Century Laboratory: Platforms

Array‐Based High‐Throughput Screening in Mouse Embryonic Stem Cells with shRNAs

Contact Info

Product

Resources

About