High throughput screening (hts) copy

hts

1. High Throughput Screening (HTS) PRESENTED BY: IQRAR AHMAD (M.PHARM SECOND SEMESTER) DEPARTMENT OF PHARMACEUTICAL CHEMISTRY R.C PATEL INSTITUTE OF PHARMACEUTICAL EDUCATION AND RESEARCH,SHIRPUR 1

2. High Throughput Screening (HTS) HTS is process by which large number of compounds are rapidly tested for their ability to modify the properties of a selected biological target. 2

3. Introduction High Throughput Screening (HTS) is a drug-discovery process widely used in the pharmaceutical industry. It leverages automation to quickly assay the biological or biochemical activity of a large number of drug-like compounds. 3

4. It is a useful for discovering ligands for receptors, enzymes, ion-channels or other pharmacological targets, or pharmacologically profiling a cellular or biochemical pathway of interest. 4

5. Goal of HTS Goal is to identify ‘hits’ or ‘leads’ - affect target in desired manner active at fairly low concenteration (  more likely to show specificity) - new structure HTS = 50,000-100,000 compounds screened per day!!! 5

6. Detection Methods in HTS: Spectroscopy Mass Spectrometry Chromatography Calorimetry X-ray diffraction Microscopy Radioactive methods 6

7. Spectroscopy in HTS: Fluorescence Spectroscopy Total internal reflection fluorescence (TIRF) Nuclear magnetic resonance (NMR) Absorption and luminescence sp. Fourier transformed infrared sp. (FTIR) Light scattering 7

8. Chromatography in HTS: Gas chromatography (GC) Thin layer chromatography Liquid chromatography (HPLC) Ion Exchange chromatography Reverse phase chromatography Hydrophobic interaction chromatography Affinity chromatography 8

9. Calorimetry in HTS: Isothermal titration Calorimetry (ITC) Differential scanning Calorimetry (DSC) 9

10. Advantages of HTS High sensitivity of assay (single molecule detection) High speed of assay (automation) Fast data processing of results Reproducibility 10

11. Disadvantages: High cost Low data quality Local contamination Need of relatively pure product 11

12. Uses of HTS: To screen for all kind of novel biological active compounds (libraries): Natural products Combinatorial Libraries (peptides, chemicals…) Biological libraries To screen Micro arrays such as: DNA chips RNA chips Protein chips 12

13. Newer method in HTS: High-Throughput, Fluorescence-Based Screening For screening, expressed proteins are labelled either as fusions with green fluorescent protein (GFP)or through translational incorporation of a fluorescent amino acid derivative, BODIPY-FL-Lysine. 13

14. REFRENCES: “ Medicnal chemistry” by ashutosh kar fifth revised and expanded edition new age international publication,reprint 2011 Review On: High-Throughput Screening Is An Approach To Drug Discovery by Ashok A. Hajare , Sachin S. American Journal Of Pharmatech Research Text book of Lead Generation Approaches In Drug Discovery by Zoran Rankovic 14

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