SC4: Phenotypic Screening and Chemical Probe Development

Monday, September 21, 12:00-3:00 pm

Detailed Agenda:

Phenotypic Drug Discovery:  A Couple of Snippets from Current Thinking

Case Study: Using affinity chromatography and cross linking to uncover an orphan GPCR targeted by N-docosahexaenoylethanolamine, the ethanaloamide of the omega-3 fatty acid DHA, that enhances neurite growth and glutamatergic synaptic activity in neurons.

Introduction to the Yeast Three Hybrid System: Discuss a classic case form literature where Chidley et al.  identify Sepiapterin Reductase (SPR) as a target for the anti-inflammatory drug Sulfasalazine with Y3H.

Introduction to Drug Affinity Responsive Target Stability (DARTS): POC studies and using DARTS to unravel eIF4 as a potential target for resveratrol by Lomenick et al.

Unraveling the MOA for oxazolidinone antibiotics: Crosslinking with RNA and crystal structure.

Activity Based Probe (ABP) : Basic Design; ABP identifies MAGL as a highly  expressed target in aggressive human cancer cells and in tumor lipogenesis; ABP Protein Profiling for Metalloproteases; Chemical genetic screen with ABPs to identify drug target in Toxoplasma gondii

SILAC

Focused Screening with Drug Library at NIH: Repurposing of antihistamine chlorcyclizine for HCV

Focused Screening with Drug Library and patient cells: δ-Tocopherol for Cholesterol Storage Disorders

Early stage phenotypic screening in stem cells in may predict clinical outcome: kenpaullone and ALS

Case Study: Stem Cells in Late Stage Phenotypic Screening; ML198: A non-inhibitory small molecule that increases reduces accumulation in Gaucher and Parkinson cells.

Case Study: Discovering Compounds that Reduce the Perinucleolar Compartment (PNC), a Biomarker for Metastasis

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