Therapeutics

Latest Innovations
In vivo Active Inhibitors of FOXM1 for the Treatment of Breast Cancer Triple Negative Breast Cancer (TNBC) constitutes about 10-20% of all diagnosed breast cancers and is known to be more aggressive and difficult to treat. TNBC lacks the... Read More Triple Negative Breast Cancer (TNBC) constitutes about 10-20% of all diagnosed breast cancers and is known to be more aggressive and difficult to treat. TNBC lacks the three most common types of receptors: estrogen receptor (ER), progesterone receptor (PR) and HER2 receptor. There is a great need to find therapies targeted against TNBC due to the challenge it presents. The transcription factor, FOXM1, is implicated in several types of cancers including breast – its inhibition affects many important downstream targets essential in cancer. However, there are no effective compounds with in vivo activity against FOXM1. A group of investigators from the University of Illinois at Urbana-Champaign, led by Dr. John Katzenellenbogen, have developed novel FOXM1 inhibitors that have shown activity against cancer and may be a potential therapeutic for TNBC. They first developed a fluorescent probe for screening FOXM1 inhibitors and, furthermore, synthesized novel compounds that have demonstrated good bioavailability both orally and subcutaneously. Studies in mice have shown suppression of breast tumor growth and inhibition of Tamoxifen-resistant breast cancer cell proliferation.
Novel Endocannabinoid Therapeutics Therapeutic endocannabinoid derivatives showing an increased half-life and enhanced anti-migratory properties. These compounds retain the anti-inflammatory, anti-cancerous... Read More Therapeutic endocannabinoid derivatives showing an increased half-life and enhanced anti-migratory properties. These compounds retain the anti-inflammatory, anti-cancerous, anti-angiogenic, and anti-platelet aggregatory properties and are predicted to have minimal side-effects.
Dearomative carboamination and its application in synthesis of anticancer agents New synthesis method for isocarbostyril alkaloids based on dearomative carboamination of the benzene ring. This is the shortest and most efficient method known to date,... Read More New synthesis method for isocarbostyril alkaloids based on dearomative carboamination of the benzene ring. This is the shortest and most efficient method known to date, enabling further synthesis of novel derivatives with improved metabolic activity, stability, and aqueous solubility.
Converting Gram-Positive Antibiotics to Gram-Negative Bacteria Dr. Hergenrother from the University of IL has developed a method to convert compounds of Gram-positive antibiotics to Gram-negative antibiotics. This method and... Read More Dr. Hergenrother from the University of IL has developed a method to convert compounds of Gram-positive antibiotics to Gram-negative antibiotics. This method and compound of matter are assisted by machine learning algorithm used for finding the characteristics of successful Gram-negative antibiotics. This invention offers wide-variety of Gram-negative antibiotic compounds for patients.
Isocarbostyril Alkaloids and Functionalization Thereof Dr. Sarlah from the University of Illinois has synthesized novel analogs and isotopologs of the anticancer isocarbostyril alkaloids... Read More Dr. Sarlah from the University of Illinois has synthesized novel analogs and isotopologs of the anticancer isocarbostyril alkaloids lycoricidine and narciclasine. Currently, isocarbostyril alkaloids are low in natural abundance and have poor aqueous solubility. These new synthetic compounds exhibit improved metabolic activity, stability, and/or aqueous solubility. Enantioselective Synthesis of Isocarbostyril Alkaloids and Analogs Using Catalytic Dearomative Functionalization of Benzene. Bingham, et al. Dec 6, 2018.
An Epitope- and Structure-based Shigella MEFA (multiepitope fusion antigen) Protein Induces Broad Antibody Responses against Shigella spp Dr. Zhang from the University of Illinois has developed a promising candidate protein for a vaccine against Shigellosis, an infectious gastrointestinal disease caused by... Read More Dr. Zhang from the University of Illinois has developed a promising candidate protein for a vaccine against Shigellosis, an infectious gastrointestinal disease caused by Shigella bacteria. The protein is a multiepitope fusion antigen (MEFA), incorporating virulence factors which are conserved across multiple Shigella serotypes. When administered to animals, this fusion protein induces protection against Shigella epithelial cell invasion. Since virulence factors from multiple serotypes are included in the fusion protein, this protection can be extended to the various Shigella serotypes.
An Epitope and Structure-based Shigella MEFA (multiepitope fusion antigen) Protein Induces Broad Antibody Responses Against Shigella spp Dr. Zhang from the University of Illinois has developed a promising candidate protein for a vaccine against Shigellosis, an infectious gastrointestinal disease caused by... Read More Dr. Zhang from the University of Illinois has developed a promising candidate protein for a vaccine against Shigellosis, an infectious gastrointestinal disease caused by Shigella bacteria. The protein is a multiepitope fusion antigen (MEFA), incorporating virulence factors which are conserved across multiple Shigella serotypes. When administered to animals, this fusion protein induces protection against Shigella epithelial cell invasion. Since virulence factors from multiple serotypes are included in the fusion protein, this protection can be extended to the various Shigella serotypes.
Fusidic Acid Derivatives with New Antibacterial Activity Dr. Paul Hergenrother fhas developed a new series of broad spectrum fusidic acid derivatives. Designed using two distinct methodologies, these fusidic acid derivatives... Read More Dr. Paul Hergenrother fhas developed a new series of broad spectrum fusidic acid derivatives. Designed using two distinct methodologies, these fusidic acid derivatives feature unique side chains and demonstrate improved MIC values when compared with fusidic acid. One series of derivatives displays antibiotic activity against Gram-negative ESKAPE pathogens, including in clinical isolates of P. aeruginosa. The prodrug displays low toxicity in mammalian cells and human serum experiments suggest that it is less protein bound than Fusidic Acid. A second series of derivatives displays potent activity against clinical isolates of Staphylococcus aureus and Enterococcus faecium and an improved resistance profile in vitro and in vivo when compared to fusidic acid. Additionally, these derivatives display in vivo efficacy against an FA-resistant strain of Staphylococcus aureus in a mouse infection model.
Split Prime Editing Platforms Dr. Pablo Perez-Pinera has developed a method to divide prime editing tools into smaller components that are small enough to be delivered in adeno-associated viruses, an... Read More Dr. Pablo Perez-Pinera has developed a method to divide prime editing tools into smaller components that are small enough to be delivered in adeno-associated viruses, an FDA-approved vehicle for therapeutic use. Prime editors have recently shown great promise as gene editing tools with greater specificity and fewer off-target effects than existing CRISPR-Cas based methods. This technology has potential as a research tool as well as a therapeutic strategy.
A Multivalent Cholera Multiepitope Fusion Antigen (MEFA) and Application for Development of Effective Vaccines for Cholera Dr. Zhang from the University of Illinois has developed a promising candidate protein for a vaccine against cholera. Cholera is an acute, diarrheal illness caused... Read More Dr. Zhang from the University of Illinois has developed a promising candidate protein for a vaccine against cholera. Cholera is an acute, diarrheal illness caused by infection of the intestine with the toxigenic bacterium Vibrio cholerae. The protein is a multiepitope fusion antigen (MEFA), incorporating virulence factors which are conserved across multiple Vibrio serotypes. When administered to animals, the cholera MEFA is broadly immunogenic and induces protective antibodies against Vibrio. Since virulence factors from multiple serotypes are included in the fusion protein, this protection can be extended to the various Vibrio serotypes.