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:

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