University of Louisville Research Foundation, Inc

Advanced Cancer Therapeutics, LLC

Jason Chesney

Sucheta Telang

John Olaf Trent

Brian F Clem

Pooran Chand

Gilles Hugues Tapolsky

Joseph A Burlison

Jason B Meier

Nagaraju Miriyala

Methods and pharmaceutical compositions for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 4 (PFKFB4) and the treatment of cancer are described.

Compounds for the treatment of cancer

Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer). Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein.

Compounds, compositions, methods for treating diseases, and methods for preparing compounds

Selective PFKFB4 inhibitors for the treatment of cancer

Some embodiments of the invention include inventive compounds. Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer). Further embodiments include methods for making the inventive compounds. Other embodiments include PFKFB4 inhibitors and methods of using the same that can target neoplastic cells, including, such as, mechanisms within those cells that relate to the use of the glycolytic pathway. In other embodiments, small molecule PFKFB4 inhibitors are used to disrupt the kinase domain of PFKFB4 and, in some instances, decrease the glucose metabolism and growth of human cancers. Additional embodiments of the invention are also discussed herein.

Inhibitors for the treatment of cancer and related methods

Small molecule inhibitors of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) having the following formula: Formula (1) are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting PFK.FB3 enzymatic activity, methods of inhibiting glycolytic flux, and methods of treating tumors by administering an effective amount of a Formula I compound. 

Small molecule inhibitors of PFKFB3 and glycolytic flux and their methods of use as anti-cancer therapeutics

Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.

Small molecule choline kinase inhibitors, screening assays, and methods for treatment of neoplastic disorders

A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.

Family of PFKFB3 inhibitors with anti-neoplastic activities

Methods of reducing expression of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) and methods of treating a cancer in a cell are provided, the methods including contacting a cell with an effective amount of a PFKFB4 inhibitor. Short hairpin RNA (shRNA) and small interfering RNA (siRNA) inhibitors of PFKFB4 and their methods of use are also provided.

PFKFB4 inhibitors and methods of using the same

A methods and compounds for inhibiting 6-phosphofructo-2-kinase /fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.

Growing community of inventors

Louisville, KY, United States of America

Jason Chesney