Table.
A summary of the phenotypic high-throughput drug screens discussed in this review. See the text for a detailed description of individual screens.
| Phenomenon Investigated | Cell or Organism | Reagent and Assay | Chemical Library | Most Notable Findings | Ref. |
|---|---|---|---|---|---|
| Cell Cycle Progression | A549 Cells | Phospho-Nucleolin Immunoblotting | 16,320 DIVERSet Compounds (ChemBridge) | 139 Compounds Affected Mitosis | Mayer 1999 |
| Embryonic Development | Zebrafish Embryos | Visual Inspection | 1,100 DIVERSet Compounds (ChemBridge) | One Compound Caused 2:1 Atrio-Ventricular Block | Peterson 2000 |
| Exocytosis | BSC1 Fibroblasts | Fluorescent Surface Glycoprotein Export | 10,240 DIVERSet Compounds (ChemBridge) | 32 Compounds Inhibited Exocytosis | Feng 2003 |
| Cholesterol Transfer to HDL | CHO Cells Expressing SR-B1 | Cell Uptake of DiI-HDL | 16,230 DIVERSet Compounds (ChemBridge) | Five Compounds Inhibited HDL Uptake | Nieland 2002 |
| Cholesterol Efflux | HepG2 Cells | ABCA1 Promoter- Luciferase Reporter Assay | 2,600 Compounds | Ten Compounds Increased ABCA1 Expression (Two Anthracycline Antibiotics) | Gao 2008 |
| Foam Cell Formation | J774 Cells | Cell Uptake of DiI- oxLDL | 480 ICCB Known Bioactives (Biomol) | Inhibitors Of NF-κβ, Src Kinases, PKC, PLC, JNK, Actin Polymerization | Etzion 2009 |
| Aortic Coarctation | Zebrafish Embryos | Gridlock Mutant Embryos, Visual Inspection | 5,000 DIVERSet Compounds (ChemBridge) | Two Compounds Restored Normal Circulation By Increasing VEGF | Peterson 2004 |
| Embryonic FGF Signaling | Zebrafish Embryos | Transgene: FGF Signaling Induced EGFP Expression | 5,000 Compounds (From NCI Diversity Set, MicroSource Discovery Systems, ChemDiv) | One Compound (BCI) Increased FGF Signaling, Also Increased Cardiomyogenesis | Molina 2009 |
| Cardiac Differentiation Of Stem Cells | Embryonic Carcinoma P19 Cells | ANF Promoter- Luciferase Reporter Assay | 100,000 Compound Heterocycle Library | 35 Compounds Increased ANF And MHC Expression, Cardiogenol C Most Potent | Wu 2004 |
| Cardiac Differentiation Of Stem Cells | Embryonic Carcinoma P19 Cells | Nkx2.5 Promoter- Luciferase Reporter Assay | 147,000 Compound UTSW Chemical Library | 1,600 Compounds Increased Nkx2.5 Expression, Multiple Sulfonyl-Hydrazone Hits | Sadek 2008 |
| Dorsalization Of Embryos | Zebrafish Emrbyos | Visual Inspection | 7,570 Compounds (From ChemBridge, MicroSource Discovery Systems, Sigma-Aldrich) | Dorsomorphin Promoted Dorsalization, BMP Type 1 Receptor Antagonist, Promoted ES Cell Cardiomyogenesis | Yu et al. 2008 |
| Cardiomyocyte Calcineurin Signaling | H9C2 Cells | MCIP1 Promoter- Luciferase Reporter Assay | 20,000 Compounds (Myogen Library) | 21 Compounds Increased MCIP1 Expression, One Compound (PAMH) With Serotonin-Like Activity | Bush 2004 |
| Oxidant Stress- Induced Cardiomyocyte Death | H9C2 Cells | H2O2-Treated H9C2 Cells, MTT Assay | 1,280 LOPAC Compounds (Sigma- Aldrich) | Many Compounds Inhibited H9C2 Cell Death, Including PARP Inhibitors | Gero 2007 |