Hit Identification Program
Once a potential disease target has been identified, a hit molecule is required that will serve as both a tool to validate the target in in vitro and in vivo model systems and as a starting point to develop therapeutic compounds. Hits can be identified from high-throughput screening at our high-throughput/high-content chemical genomics screening facility or structure based approaches such as cyro-electron microscopy at our Cryo-EM facility and x-ray crystallography at our macromolecular crystallography facility.
The Institute for Drug Discovery has assisted faculty to identify hit molecules by providing these funding opportunities:
2024 High-Throughput/High-Content Chemical Genomics Screening Facility Credit Winning Proposals
| Faculty | Project Description |
| Mark C. Hall | Screening of inhibitors of Cdc14 protein phosphatase, a novel antifungal drug target |
| Dan Flaherty | HTS for covalent inhibitors of Ubiquitin C-terminal Hydrolase L3 |
| Yini Li | Large-scale drug screen for C9ORF72-associated familial ALS and FTD |
2023 High-Throughput/High-Content Chemical Genomics Screening Facility Credit Winning Proposals
| Faculty | Project Description |
| Chris Rice | Central Nervous System (CNS) permeable drug discovery against pathogenic free-living amoebae (pFLA) |
| Rong Huang | Discovery of Small Molecule Binders of FEM1C |
2022 High-Throughput/High-Content Chemical Genomics Screening Facility Credit Winning Proposals
| Faculty | Project Description |
| Yuk Fai Leung | In Vivo Drug Screening for Retinitis Pigmentosa with Zebrafish Visual Behavior |
2021 High-Throughput/High-Content Chemical Genomics Screening Facility Credit Winning Proposals
| Faculty | Project Description |
| Zhong-Yin Zhang | Identification and characterization of SHP2 covalent inhibitors |
2018 High-Throughput/High-Content Chemical Genomics Screening Facility Credit Winning Proposals
| Faculty | Project Description |
| Danzhou Yang | Discovery of Small Molecules that Selectively Inhibit DDX5 Unfolding of c-MYC G-quadruplex |
| Herman Sintim | High throughput screening for c-di-AMP metabolism enzymes inhibitors |
| Robert Stahelin | A High Throughput Screen of Ebola Virus Entry Inhibitors |
| Darci Trader | Rpn-13 Competitive FP Screening Grant 2018 |
| Mohamed Seleem | Identification of Small Molecules that Target the Azole Resistome in Candida |
| Rong Huang | Discovery of Small Molecule Inhibitors for N-terminal Acetyltransferase D |
| ChengDeng Hu | Discovery of inhibitors to disrupt the interaction of PRMT5 with its cofactor pICln for prostate cancer treatment |
| Benita Sjogren | Development of a Nano-Glo Assay to Screen for Modulators of Regulator of G Protein Signaling 10 (RGS10) |
| Yang Yang | Finding compounds that can protect against chemotherapy-induced peripheral neuropathy |
2017 High-Throughput/High-Content Chemical Genomics Screening Facility Credit Winning Proposals
| Faculty | Project Description |
| Andrea Kasinski | Identification of small molecules that can increase the levels of the mature microRNA (miRNA) let-7 |
| Andy Mesecar | Discovery and Development of Ubiquitin Specific Protease Inhibitors as Anti-Cancer Leads |
| Angeline Lyon | Identification of Small Molecule Allosteric Modulators of Phospholipase Cβ |
| Chris Rochet | Identification of small-molecule inhibitors of alpha-synuclein-mediated vesicle permeabilization |
| Chun-Ju Chang | Discovery of cancer stem cell fate manipulating compounds as new anti-cancer drugs |
| Danzhou Yang | Discovery of Small Molecules that Bind Selectively to the c-MYC Promoter G-quadruplex |
| Dan Flaherty | Identification of Inhibitors for Ubiquitin C-terminal Hydrolase L1 |
| Robert Geahlen | Developing inhibitors of P-body formation and EMT by targeting DDX6 |
| Jer-Yen Yang | Identifying novel GLI1 inhibtors for cancer therapeutics |
| Kavita Shah | High-throughput Screening for Identifying and Validating Small molecule Inhibitors of LIMK2 kinase |
| Val Watts | Identification of AC8 inhibitors for alcoholism and anxiety disorders |
| Richard van Rijn | β-arrestin1 biased delta opioid receptor agonists for treatment of stroke and seizures. |
| Yuk Fai Leung | In Vivo Drug Screening for Retinitis Pigmentosa with Zebrafish |