Title:
TARGET BINDING MOLECULES IDENTIFIED BY KINETIC TARGET-GUIDED SYNTHESIS
Document Type and Number:
WIPO Patent Application WO/2015/021134
Kind Code:
A3
Abstract:
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 o both of the Bcl-XL and Mcl-1 proteins. Pharmaceutical formulations of these target binding molecules are also provided.
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Inventors:
MANETSCH ROMAN (US)
NACHEVA KATYA PAVLOVA (US)
FLANIGAN DAVID LAWRENCE (US)
NAMELIKONDA NIRANJAN KUMAR (US)
IYAMU IREDIA DAVID (US)
KULKARNI SAMEER SHAMRAO (CH)
BARBER MEGAN M (US)
TIPTON JEREMIAH DWAYNE (US)
WANG HONG-GANG (US)
DOI KENICHIRO (US)
NACHEVA KATYA PAVLOVA (US)
FLANIGAN DAVID LAWRENCE (US)
NAMELIKONDA NIRANJAN KUMAR (US)
IYAMU IREDIA DAVID (US)
KULKARNI SAMEER SHAMRAO (CH)
BARBER MEGAN M (US)
TIPTON JEREMIAH DWAYNE (US)
WANG HONG-GANG (US)
DOI KENICHIRO (US)
Application Number:
PCT/US2014/049916
Publication Date:
April 02, 2015
Filing Date:
August 06, 2014
Export Citation:
Assignee:
UNIV SOUTH FLORIDA (US)
PENN STATE RES FOUND (US)
PENN STATE RES FOUND (US)
International Classes:
C40B30/10; A01N33/26; A61K31/165
Other References:
NACHEVA ET AL.: "Development of a Bio-Molecular Fluorescent Probe Used in Kinetic Target- Guided Synthesis for the Identification of Inhibitors of Enzymatic and Protein-Protein Interaction Targets.", PH. D. DISSERTATION UNIVERSITY OF SOUTH FLORIDA., January 2012 (2012-01-01), TAMPA, FL, XP055277744, Retrieved from the Internet
KULKARNI ET AL.: "Screening of protein-protein interaction modulators via sulfo-click kinetic target -guided synthesis.", ACS CHEM BIOL, vol. 6, no. 7, 15 July 2011 (2011-07-15), pages 724 - 732, XP055277757
KULKARNI ET AL.: "Screening of protein-protein interaction modulators via sulfo-click kinetic target -guided synthesis.", ACS CHEM BIOL, vol. 6, no. 7, 15 July 2011 (2011-07-15), pages 724 - 732, XP055277757
Attorney, Agent or Firm:
LINDER, Christopher B. et al. (LLP400 Interstate North Parkway, Suite 150, Atlanta GA, US)
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