US 12,138,301 B2
Compounds including a mutant KRAS sequence and a lipid and uses thereof
Peter C. Demuth, Medford, MA (US); Julian Adams, Boston, MA (US); and Martin Steinbuck, Boston, MA (US)
Assigned to Elicio Therapeutics, Inc., Boston, MA (US)
Appl. No. 16/977,155
Filed by Elicio Therapeutics, Inc., Cambridge, MA (US)
PCT Filed Mar. 1, 2019, PCT No. PCT/US2019/020404
§ 371(c)(1), (2) Date Sep. 1, 2020,
PCT Pub. No. WO2019/169332, PCT Pub. Date Sep. 6, 2019.
Claims priority of provisional application 62/637,879, filed on Mar. 2, 2018.
Prior Publication US 2021/0060149 A1, Mar. 4, 2021
Int. Cl. A61K 39/00 (2006.01); A61K 39/39 (2006.01); A61K 47/54 (2017.01); A61K 47/60 (2017.01); A61P 35/00 (2006.01); C07K 7/00 (2006.01); C12N 9/14 (2006.01); C12N 9/96 (2006.01)
CPC A61K 39/001164 (2018.08) [A61K 39/39 (2013.01); A61K 47/543 (2017.08); A61K 47/60 (2017.08); A61P 35/00 (2018.01); C12N 9/14 (2013.01); C12N 9/96 (2013.01); C12Y 306/05002 (2013.01); A61K 2039/545 (2013.01); A61K 2039/55561 (2013.01)] 34 Claims
 
1. A compound comprising a mutant KRAS sequence and a lipid, wherein the mutant KRAS sequence is conjugated to the lipid by a linker, and (i) the linker comprises one or more polyethylene glycol blocks, (ii) the lipid is 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE), and (iii) the mutant KRAS sequence consists of an amino acid sequence selected from the group consisting of CYKLVVVGADGVGKSALTI (SEQ ID NO:1), CYKLVVVGAVGVGKSALTI (SEQ ID NO:2), CYKLVVVGARGVGKSALTI (SEQ ID NO:3), CYKLVVVGAAGVGKSALTI (SEQ ID NO:4), CYKLVVVGASGVGKSALTI (SEQ ID NO:5), CYKLVVVGACGVGKSALTI (SEQ ID NO:6), CYKLVVVGAGDVGKSALTI (SEQ ID NO:7), CYKLVVVGATGVGKSALTI (SEQ ID NO:22), YKLVVVGADGVGKSALTI (SEQ ID NO:23), YKLVVVGAVGVGKSALTI (SEQ ID NO:24), YKLVVVGARGVGKSALTI (SEQ ID NO:25), YKLVVVGAAGVGKSALTI (SEQ ID NO:26), YKLVVVGASGVGKSALTI (SEQ ID NO:27), YKLVVVGACGVGKSALTI (SEQ ID NO:28), YKLVVVGATGVGKSALTI (SEQ ID NO:29), and YKLVVVGAGDVGKSALTI (SEQ ID NO:30).