Novel Inhibitors of Bacterial Growth
JHU REF: C13624
Invention novelty: Novel antibacterials that inhibit non-classical transpeptidases.
Value Proposition: Resistance to existing antibacterials is being reported at an alarming rate. Therefore, new antibacterials that work by inhibiting novel enzymes would be of high utility in treating bacterial infections. Johns Hopkins researchers (in collaboration with Rutgers University) have developed a number of novel inhibitors based on the carbapenem core, a subclass of beta-lactam. The core structure is complementary to the active site of non-classical transpeptidases, namely LD-transpeptidases that are cysteine peptidases that have not been exploited before for drug development as this enzyme class was only recently identified. Our inventors identified this enzyme class and hold rights to these enzymes for inhibition. The compounds acylate the catalytic amino acid residue of the enzyme resulting in covalent binding to the enzyme and permanently inhibiting it. We have tested these novel compounds and find that they are active against (at therapeutically valuable concentrations) against a range of high priority human bacterial pathogens. These pathogens include gram positives Acinetobacter baumannii, Enterobacter cloacae, Klebsiella pneumoniae, gram positives Enterococcus faecalis, Staphylococcus aureus (including methicillin resistant) and Mycobacterium tuberculosis. Novelties are:
- Inhibition of bacterial growth when bacteria are subjected to these molecules.
- Inhibits bacterial growth by targeting novel enzyme.
MAJOR RESULTS:
Johns Hopkins researchers have developed a series of compounds that are active against a range of bacterial pathogens important to human health. Therefore these compounds have the potential to be licensed for commercial development into antibiotics to treat bacterial infections in humans and animals.
DISEASE INDICATION
Infectious Diseases
ASSOCIATED PUBLICATIONS
None at This Time
TECHNOLOGY CLASSIFICATION
Primary Category: Therapeutics
Primary Subcategory: Small Molecules
ASSOCIATED REPORTS OF INVENTION (ROIs) AND INTELLECTUAL PROPERTY (IP) FILING NUMBERS
ROI #: C13624
TITLE: NOVEL INHIBITORS OF BACTERIAL GROWTH
STATUS: US Provisional
PRIORITY DATE: 1/29/2016
IP FILING NUMBERS: US 62/288,532
