University of South Florida

The Penn State Research Foundation

Megan M Barber

Roman Manetsch

David Lawrence Flanigan

Lindsey Neil Shaw

Renee Marie Fleeman

Whittney Burda

Hong-Gang Wang

Kurt Steven Van Horn

Niranjan Kumar Namelikonda

Katya Pavlova Nacheva

Jeremiah Dwayne Tipton

Kenichiro Doi

Iredia David Iyamu

Sameer Shamrao Kulkarni

Methods of identifying target binding molecules by target guided synthesis are provided. The methods include providing two or more fragments capable of reacting to form the target binding molecule and mixing the fragments with the target. The methods can be used to identify target binding molecules that bind targets such as proteins or nucleic acids, including those that bind shallow binding pockets on the surface of such targets. The methods are applied to the Bcl-XL and Mcl-1 proteins from the Bcl-2 family of proteins. Using thio acid and sulfonyl azide fragments capable of reacting through sulfo-click chemistry, new acyl sulfonamides are identified that bind one or both of the Bcl-XL and Mcl-1 proteins. Pharmaceutical formulations of these target binding molecules are also provided.

Target binding molecules identified by kinetic target-guided synthesis

Described herein are quinazoline-based compounds and formulations thereof. In some embodiments, the compounds and/or formulations thereof can be effective to inhibit and/or kill. Also described herein are methods of treating a subject in need thereof by administering to the subject in need thereof a quinazoline-based compound and/or formulation thereof to the subject in need thereof.

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Growing community of inventors

Parrish, FL, United States of America

Megan M Barber