US 12,268,749 B2
Cell-penetrating peptides
Matthew Wood, Oxford (GB); Raquel Manzano, Zargoza (ES); Caroline Godfrey, Oxford (GB); Graham McClorey, Oxford (GB); Richard Raz, London (GB); Michael Gait, Cambridge (GB); Andrey Arzumanov, Cambridge (GB); Liz O'Donovan, Ballyanly (IE); Gareth Hazell, Oxford (GB); Ashling Holland, Oxford (GB); and Miguel Varela, Oxford (GB)
Assigned to Oxford University Innovation Limited, Oxford (GB); and United Kingdom Research and Innovation, Swindon (GB)
Appl. No. 17/266,939
Filed by Oxford University Innovation Limited, Oxford (GB); and United Kingdom Research and Innovation, Swindon (GB)
PCT Filed Aug. 9, 2019, PCT No. PCT/GB2019/052247
§ 371(c)(1), (2) Date Feb. 8, 2021,
PCT Pub. No. WO2020/030927, PCT Pub. Date Feb. 13, 2020.
Claims priority of application No. 1812972 (GB), filed on Aug. 9, 2018.
Prior Publication US 2021/0299263 A1, Sep. 30, 2021
Int. Cl. A61K 47/64 (2017.01); C07K 7/08 (2006.01); C07K 14/00 (2006.01); C12N 15/113 (2010.01)
CPC A61K 47/645 (2017.08) [C07K 7/08 (2013.01); C07K 14/00 (2013.01); C12N 15/113 (2013.01); C07K 2319/10 (2013.01); C12N 2310/11 (2013.01); C12N 2310/3513 (2013.01); C12N 2320/32 (2013.01)] 22 Claims
 
1. A cell-penetrating peptide consisting of the amino acid sequence
 
 (SEQ ID NO: 27)
 
 RBRRBRRFQILYRBRBR,
 
 
 
 (SEQ ID NO: 31)
 
 RBRRBRRYQFLIRBRBR,
 
 
 
 (SEQ ID NO: 32)
 
 RBRRBRRILFQYRBRBR,
 
 
 
 (SEQ ID NO: 35)
 
 RBRRBRFQILYBRBR,
 
 
 
 (SEQ ID NO: 37)
 
 RBRRBRRFQILYRBHBH,
 
 
 
 (SEQ ID NO: 38)
 
 RBRRBRRFQILYHBHBR,
 
 
 
 (SEQ ID NO: 44)
 
 RBRRBRFQILYRBHBH,
 
 
 
 (SEQ ID NO: 29)
 
 RBRRBRFQILYRRBRBR,
 
 
 
 (SEQ ID NO: 30)
 
 RBRBRFQILYRBRRBRR,
 
 
 
 (SEQ ID NO: 33)
 
 RBRRBRFQILYRBRBR,
 
 
 
 (SEQ ID NO: 36)
 
 RBRRBFQILYRBRBR,
 
 
 
 (SEQ ID NO: 39)
 
 RBRRBRRFQILYHBRBH,
 
 
 
 (SEQ ID NO: 40)
 
 RBRRBRRYQFLIRBHBH,
 
 
 
 (SEQ ID NO: 41)
 
 RBRRBRRILFQYRBHBH,
 
 
 
 (SEQ ID NO: 42)
 
 RBRHBHRFQILYRBRBR,
 
 
 
 (SEQ ID NO: 52)
 
 RBRRBRRFQILYHBHBH,
 
 
 
 (SEQ ID NO: 104)
 
 RBRRBRWWWBRBR,or
 
 
 
 (SEQ ID NO: 105)
 
 RBRRBRWWPWWBRBR,
wherein B in the amino acid sequences is beta-alanine, and wherein the N-terminus of the cell-penetrating peptide is optionally acetylated, methylated, trifluoroacetylated, trifluoromethylsullfonylated, or methylsulfonylated.