Small Molecules

Latest Innovations
Powerful Biphosophonates for Treatment of Cancer, Bone Loss, and Infectious Disease Although there are already a few existing compounds for use in the treatment of bone diseases, these new compounds may have efficacy exceeding that of current... Read More Although there are already a few existing compounds for use in the treatment of bone diseases, these new compounds may have efficacy exceeding that of current commercial species. In some cases, existing treatments have high toxicity and low efficacy. These new compounds may, therefore, be better than existing therapeutic options. These new compounds can help restore the natural balance between normal bone destruction and replacement. They are also potential candidates for the treatment of cancer and infectious diseases as related compounds have been shown to kill tumor cells and parasites. They have been shown to stimulate T-Cells, assisting in the treatment of cancer and infectious diseases. They have multiple targets, some involved in regulating apoptosis, and displays increased potency, making it a possible cancer drug. Its improved cell availability lowers the effective dose and can lead to fewer side effects. These compounds make up a series of bisphosphonates useful for the treatment of bone-related diseases, cancer and infections caused by protozoa and bacteria. The compounds represent new compositions of matter. Current clinical Bisphosphonates contain a nitrogen atom that can be positively charged. The new compounds have positively charged P, As, Sb, S, Se or Te sites instead of nitrogen. They may have higher activity in treating a variety of diseases than existing compounds and may have lower toxicity than existing compounds. Applications Treatment of bone diseases, cancer and infections Benefits Increased potency, makes it a possible cancer therapeutic Improved cellular availability lowers the effective dose required and can lead to fewer side effects Potential higher activity in treating a variety of diseases than existing compounds May have lower toxicity than existing compounds
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).
PAC-1 combination therapy for Uveal Melanoma Dr. Hergenrother from the University of Illinois at Urbana-Champaign has developed a new synergistic combination therapy using the small... Read More Dr. Hergenrother from the University of Illinois at Urbana-Champaign has developed a new synergistic combination therapy using the small molecule PAC-1 and kinase inhibitors for treatment of uveal melanoma. There are no current targeted therapies against this type of cancer, making this combination treatment a promising one.
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 Toll-Like Receptor Inhibitors for Treatment of Inflammatory Disease Dr. Katzenellenbogen from the University of Illinois at Urbana-Champaign has developed a novel class of inhibitors capable of inhibiting Toll-like Receptor signaling.... Read More Dr. Katzenellenbogen from the University of Illinois at Urbana-Champaign has developed a novel class of inhibitors capable of inhibiting Toll-like Receptor signaling. These compounds will allow treatment of inflammatory diseases such as sepsis. Currently there are no TLR inhibitors on the market and this novel set of compounds show higher affinity than currently published compounds. In addition to high specificity for TLRs these compounds are also able to be derivatized for specificity to specific classes of TLRs.
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.
Novel Estrogen Receptor β (ERβ) Drugs for the Treatment of Multiple Sclerosis (MS) Currently available therapeutic agents approved for the treatment of multiple sclerosis (MS) reduce relapse rates, but do not reverse or prevent neurodegeneration nor... Read More Currently available therapeutic agents approved for the treatment of multiple sclerosis (MS) reduce relapse rates, but do not reverse or prevent neurodegeneration nor initiate myelin repair. There is thus a great need for effective therapies against MS. Scientists at the University of Illinois at Urbana-Champaign, led by Dr. John Katzenellenbogen, have developed novel chloroindazole analogs that show particular promise in promoting remyelination while reducing inflammatory cytokines in mice with experimental autoimmune encephalomyelitis (EAE). These novel MS drugs are specific for ERβ and have tremendous potential for the treatment of MS. The compounds are more superior to other estrogenic drugs due to their specificity for ERβ and lack of undesirable effects such as feminization and increased risk of cancer.
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.