HighThroughput Screening Core Facility at CUBoulder Wei Wang

High-Throughput Screening Core Facility at CU-Boulder Wei Wang 06 -01 -2015

HTS Core Facility Mission and Services Our mission is to promote chemical biology research and drug discovery at CU-Boulder and surrounding areas. We offer assistance on all steps involved in typical drug-discovery processes: 1. Assay development and validation 2. High-throughput screening 3. Data analysis, validation and lead identification 4. Structure and activity relationship (SAR) studies and large-scale production 5. In silico screen (we offer access to Schrodinger Suite ) and post-screen cheminformatic analysis

Compound Libraries and Instrumentation - FDA-approved drug library: 1, 200 compounds (Prestwick Chemical) Kinase- or protease-targeted library: 2, 100 compounds (Biofocus) Drug-like diversity library: 14, 400 compounds (Maybridge Hit. Finder v 11) Drug-like diversity library: 10, 000 compounds (Chem. Bridge) Drug-like diversity library: 10, 000 compounds (Tim. Tec)

Summary of Recent Screens (I) Screen for inhibitors of Pin. K 1 -Parkin pathway (Liu Lab) Screen for agonists of Toll-like receptors (Yin Lab) Screen for molecules that selectively potentiate the activity of β-lactam antibiotics in MRSA (Wang Lab) Screen for agonists of TLR 5 (Yin Lab) Screen for antagonists of TLR 5 (Yin Lab) Screen for agonists of TLR 3 (Yin Lab) Screen for antagonists of TLR 8 (Yin Lab) Library Assay Optimization Test Pilot HTS Hits Run Screen Validation Kinase- & protease-targeted Maybridge Indole alkaloids Maybridge

Summary of Recent Screens (II) Screen for JHDM 1 -class-selective inhibitors (Facility and Wang Lab) Library Assay Test Optimization Run Maybridge Screen for agonists of TLR 2 Maybridge (Yin Lab) Screen for antagonist of TLR 2 Maybridge (Yin Lab) Screen for antagonists of TLR 7 Maybridge (Yin Lab) Screen for compounds that disrupt replication of salmonella inside host Maybridge macrophages (Detweiler Lab) Screen for compounds that block MED 1 Maybridge and Tra interaction (Taatjies Lab) Screen for offshoots of type 1 IFN signaling pathway that is responsible for FDA-approved suppressing response to IFNg drug library (Lenz Lab) Pilot HTS Hits Screen Validation

Awarded Grants and Funding Opportunities Year 2013 Award Lab Golfers Against Taatjes and Cancer Award Wang 2014 Bioscience Discovery Johnson Evaluation Grant 2015 Innovative Seed Grant Detweiler 2012 -7 NIH R 21/R 33 Lenz Institute Dept. of Chem & Biochem Institute of Behavioral Genetics MCDB Dept. of Immunology and Microbiology, CU Anschutz NIH high throughput screening funding opportunities: • Development of Assays for High-Throughput Screening for Use in Probe and Pretherapeutic Discovery (R 01) (PAR-13 -364) • High Throughput Screening (HTS) to Discover Chemical Probes (R 21) (PAR-14 -283) • High Throughput Screening (HTS) to Discover Chemical Probes (R 01) (PAR-14 -284)

Contact Us Xiang Wang Director E-mail: xiang. wang@colorado. edu Office: 303 492 6266 UCB 215 Department of Chemistry and Biochemistry University of Colorado-Boulder, CO 80303 Wei Wang Manager E-mail: wang. wei@colorado. edu Office: 303 492 8740