Hit to Lead Program
In order to advance a hit molecule into a therapeutic lead, many of the compounds attributes must be optimized including solubility, potency, pharmacokinetics, toxicity, etc. These development activities require expertise from a broad interdisciplinary group including biologists, chemists, formulators, and toxicologists to name but a few. A number of core facilities who can help with this type of testing can be found on our affiliated scientific core facilities page.The Institute for Drug Discovery has assisted faculty in advancing initial "hit" drugs by providing these funding opportunities:
2024 Hit-to-Lead and External Advisory Board Winning Proposals
| Faculty | Project Description |
| Dan Flaherty | Hit-to-lead optimization of irreversible P. falciparum PI4K inhibitors. |
| Ryan Altman | (–)-TAN-67: Characterizing DMPK/Tox and Efficacy in an In Vivo Model for Alcohol Misuse and Alcohol Use Disorder |
| Severin Schneebeli | Small-molecule and Peptide PAC1 Antagonists for Migraine Prevention and Treatment |
| Betsy Parkinson, Chris Rice, and Bryon Drown | First-in-class bacterial peptide hits as potential novel anti-Balamuthia mandrillaris therapeutics. |
| Doug LaCount | Inhibition of Ebola virus replication with dominantly interfering virus-derived peptides |
| Graham Cooks | Discovery of SULT2B1b inhibitors for cancer treatment |
2023 Hit-to-Lead and External Advisory Board Winning Proposals
| Faculty | Project Description |
| Rong Huang | Development of potent and selective PRMT1 inhibitor as a novel treatment for fibrosis |
| Tonglei Li | Artificial Intelligence in Drug Research by Kernelization of Quantum Information |
| Herman Sintim | Novel Haspin Inhibitors |
| P.V. Ramachandran | Target Identification of a potent, lead molecule, AAMLA-4, to treat Clostridiodes difficile infection (CDI) |
| Seung-Oe Lim | Development of a new immunotherapeutic antibody for Alzheimer’s Disease |
| Andrea Kasinski | Ligand-mediated delivery of fully-modified miR-34a for the treatment of lung and breast cancers |
2022 Hit-to-Lead and External Advisory Board Winning Proposals
| Faculty | Project Description |
| Mark C. Hall | Exploring Cdc14 phosphatase as a novel antifungal drug target |
| Chittaranjan Das | Development of PROTAC ligands for HECT-type E3 ligases |
| Yang Yang | Developing a first-in-class dual-Adeno Associated Virus (dual-AAV) based gene therapy to treat SCN2A deficient monogenic autism spectrum disorder (ASD) |
| Seung-Oe Lim | Development of a new immunotherapeutic anti-human PD-L1/HA bispecific antibody for flaming up the tumor immune microenvironment |
| Dan Flaherty | Preclinical evaluation and IND enabling studies for inhibitors of vancomycin-resistant enterococci (VRE) |
| Zhong-Yin Zhang | Small molecule inhibitors of PTPN22 for cancer immunotherapy |
2020 Hit-to-Lead and External Advisory Board Winning Proposals
| Faculty | Project Description |
| John Tesmer | Selective Inhibition of G Protein- Coupled Receptor Kinases |
| Yoon Yeo | Systemic therapy of sepsis by vitamin D/polymyxin B nanoparticles |
| Seema Mattoo | Manipulating AMPylation: Identification of small molecule interventions to regulate the activity of the human Fic protein, HYPE/FicD |
| Jeremey Lohman | Discovery of acetyl-CoA carboxylase futile cycle inducers as drug leads |
| Herman Sintim | A best-in-class FLT3 inhibitor with activity against collaborating RET kinase as third line treatment for acute myeloid leukemia |
| Dan Flaherty | Lead Identification of inhibitor for adenylyl cyclase type 1 for the treatment of chronic pain |
2019 Hit-to-Lead and External Advisory Board Winning Proposals
| Faculty | Project Description |
| Herman Sintim | LR (37/67KDa Laminin Receptor) |
| Mingji Dai | Inhibitors of BAF chromatin remodeling complexes |
| Val Watts and Dan FLaherty | Identification of AC8 inhibitors for alcoholism and alcohol use disorders (AUDs) |