Small Molecules

Latest Innovations
Algorithm Modified Deoxynybomycin for the Treatment of Gram-Negative Bacteria Dr. Hergenrother from the University of IL has developed a novel antibiotic that is effective against certain antibiotic-resistant gram-negative bacteria. His powerful... Read More Dr. Hergenrother from the University of IL has developed a novel antibiotic that is effective against certain antibiotic-resistant gram-negative bacteria. His powerful predictive algorithm determines accumulation of molecules in Gram-negative bacteria and enables conversion of known Gram-positive only antibiotics into novel compounds with Gram-negative potency.
A Pro-Apoptotic Microbial Community Network Enriched in the Tissue of IPF and Lung Cancer Patients Dr. Isaac Cann from the University of Illinois has identified biomarkers and therapeutic strategy for treatment of... Read More Dr. Isaac Cann from the University of Illinois has identified biomarkers and therapeutic strategy for treatment of idiopathic pulmonary fibrosis (IPF) and lung cancer. This strategy has the potential to dramatically improve the lives of millions patients throughout the world. It is the first know effective treatment route for IPF. The therapeutic strategy is based on the discovery of link between microbial community remodeling and IPF. Furthermore, the lung microbial community can induce excessive apoptosis of alveolar lining epithelial cells leading to lung carcinogenesis. Benefit • Treatment strategies including broad spectrum antibiotics may be effective for treating IPF and preventing lung cancer
Small Molecules With Antibacterial and Anticancer Activity Dr. Hergenrother from the University of Illinois at Urbana-Champaign has developed a series of topoisomerase inhibiting small molecules... Read More Dr. Hergenrother from the University of Illinois at Urbana-Champaign has developed a series of topoisomerase inhibiting small molecules with anticancer activity. These molecules possess comparable activity and selectivity to doxorubicin, a common cancer chemotherapy drug, across a range of cancer cell lines. These small molecules are a promising alternative to cardiotoxicity producing doxorubicin as a cancer chemotherapy drug. These molecules are also useful as broad-spectrum antibiotics capable of treating resistant bacteria strains (minimum inhibitory concentrations as low as 0.5 micrograms/mL for S. aureus and E. coli).
Ligand for Potential Treatment of Myotonic Dystrophy Type 1 (DM1) Dr. Zimmerman from the University of Illinois at Urbana-Champaign has developed an oligomeric ligand that can have potential... Read More Dr. Zimmerman from the University of Illinois at Urbana-Champaign has developed an oligomeric ligand that can have potential applications in the treatment of DM1. This Ligand on account of its multivalent nature, is an improvement over the previous small molecule (TF12039) designed by the inventor. The oligomeric ligand has been shown to rescue mis-splicing activity in DM1 cell models. Climbing defects in adult DM1 drosophila flies was also show to have been rescued on treatment with this oligomeric ligand.
Novel Endocannabinoid Therapeutics Dr. Aditi Das from the University of Illinois at Urbana-Champaign has developed a novel set of therapeutic endocannabinoid derivatives.... Read More Dr. Aditi Das from the University of Illinois at Urbana-Champaign has developed a novel set of therapeutic endocannabinoid derivatives. These derivatives retain the anti-inflammatory, anti-cancerous, anti-angiogenic, and anti-platelet aggregatory properties while having an increased half life. As these compounds are based off endogenous endocannabinoids it is predicted side-effects will be miminal. Importantly these derivatives show enhanced anti-migratory properties compared to the endogenous compound suggesting they will act as potent drugs.
In Vivo Active Inhibitors of FOXM1 for Suppression of Cancer Breast cancer is the leading cause of death among women all over the world. Hormonal therapy, sometimes also called anti-estrogen therapy, works by lowering the amount of... Read More Breast cancer is the leading cause of death among women all over the world. Hormonal therapy, sometimes also called anti-estrogen therapy, works by lowering the amount of estrogen in the body or blocking estrogen from attaching to the breast cancer cells. Triple negative breast cancer (TNBC) lacks the three most common types of receptors to fuel most breast cancer growth: ER, PR and HER-2. It constitutes about 10-20% of diagnosed breast cancers, can be more aggressive and difficult to treat and is more likely to spread and recur. There is great interest in finding targeted therapies against TNBC. The transcription factor FOXM1 has been pointed out as a potential target for several types of cancer (breast, prostate, ovary, lung ad GU tract); however, no effective therapies targeting FOXM1 have been developed so far. Inventors at the University have developed small molecule anticancer compounds that can inhibit the FOXM1 transcription factors, a known anticancer target, and are effective against breast cancer including a triple negative variant. These compounds have been tested in mouse models showing good bioavailability after oral or subcutaneous administration. The compound NB-72 labeled with a fluorescent probe was additionally used to developed an in vitro assay for screening of inhibitors against FOXM1. Publications Ziegler, Y., Laws, M.J., Sanabria Guillen, V. et al. Suppression of FOXM1 activities and breast cancer growth in vitro and in vivo by a new class of compounds. npj Breast Cancer5, 45 (2019). https://doi.org/10.1038/s41523-019-0141-7 https://patents.google.com/patent/US20210032193A1/
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.
Complex Compounds From the Natural Product Lycorine Dr. Hergenrother from the University of Illinois has created a diverse compound screening library from the synthetic scaffold lycorine. Lycorine is an alkaloid isolated... Read More Dr. Hergenrother from the University of Illinois has created a diverse compound screening library from the synthetic scaffold lycorine. Lycorine is an alkaloid isolated from Amaryllidaceae species and has demonstrated anti-cancer, anti-angiogenesis, anti-viral, anti-bacterial, anti-parasitic and anti-inflammatory activity. Through manipulation of the ring system, the Hergenrother lab has constructed more than 42 novel and diverse compounds to be used in a high throughput drug screen. Lycorine