Development and Use of O-linked beta-N-acetylglucosamine (O-GlcNAc) Transferase (OGT) Inhibitors for Multiple Conditions, Including Cancer

This technology includes the development and use of small molecules that inhibit O-linked beta-N-acetylglucosamine (O-GlcNAc) transferase (OGT) for a variety of pathologies, including Alzheimer's disease, cancer, cancer, diabetes, and neurodegenerative disorders the treatment of cancer and as a potential antiviral. OGT is a ubiquitous enzyme that catalyzes the transfer of N-acetylglucosamine (GlcNAc) to the serine or threonine residues of nuclear and cytoplasmic proteins.

Minibody for Conditioning prior to Hematopoietic Stem Cell and Progenitor Cell Transplantation

Patient conditioning is a critical initial step in hematopoietic stem and progenitor cell (HSPC) transplantation procedures to enable marrow engraftment of infused cells. Conditioning regimens have traditionally been achieved by delivering cytotoxic doses of chemotherapeutic agents and radiation. However, these regimens are associated with significant morbidity and mortality, and cannot be used safely in elderly or subjects with comorbidities.

New Antimalarial Chemotypes Discovered Through Chemical Methodology and Library Development

This technology includes three new compound classes displaying either differential or comprehensive antimalarial activity across geographically diverse lines. These compounds were identified from a quantitative high throughput screen of a novel chemical library with unique chemical complexity and are potential candidates for treating malaria.

Discovery of an imidazo[1,2-a]pyridines with Anticancer Properties

This technology includes a series of imidazo[1,2-a]pyridines with potent inhibition of FLT3, which retains potent binding and activity against FLT3 tyrosine kinase domain and gatekeeper mutations. This chemotype exhibits superior anti-leukemic activity against the common clinically-relevant FLT3-mutant acute myeloid leukemia (AML) in vitro and in vivo. Tyrosine kinase domain mutations are a common cause of acquired resistance to FLT3 inhibitors used to treat FLT3-mutant AML. This invention builds upon an earlier IP position with new analogs.

Discovery of an imidazo[1,2-a]pyridines with Anticancer Properties

This technology includes a series of imidazo[1,2-a]pyridines with potent inhibition of FLT3, which retains potent binding and activity against FLT3 tyrosine kinase domain and gatekeeper mutations. This chemotype exhibits superior anti-leukemic activity against the common clinically-relevant FLT3-mutant acute myeloid leukemia (AML) in vitro and in vivo. Tyrosine kinase domain mutations are a common cause of acquired resistance to FLT3 inhibitors used to treat FLT3-mutant AML. This invention builds upon an earlier IP position with new analogs.

Small Molecule Anti-cancer Agents that Stabilize the MYC-G-Quadruplex

The proto-oncogene c-Myc is deregulated and overexpressed in ~70% of all cancers. Thus, c-Myc is an attractive therapeutic target since disrupting c-Myc activity could be used as pan-chemotherapy. Beyond cancer, Myc is also a positive effector of tissue inflammation, and its function has been implicated in the pathophysiology of heart failure. Because c-Myc is a transcription factor, a rationally designed small molecule targeting c-Myc would be required to exhibit significant specificity.

Treatment of Periodontal Disease via ENPPI Inhibition

This technology focuses on enhancing cementum production, a key component in treating periodontal regression. The method involves inhibiting ectonucleotide pyrophosphatase phosphodiesterases (ENPP1), enzymes that play a significant role in mineralization processes. Pyrophosphate (PPi) is known to impede the growth of hydroxyapatite crystals, essential for mineralization. ENPP1 catalyzes the hydrolysis of ATP, generating PPi, which then hinders mineralization.

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