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. Author manuscript; available in PMC: 2023 May 2.
Published in final edited form as: Mol Pharm. 2022 Apr 11;19(5):1378–1388. doi: 10.1021/acs.molpharmaceut.1c00924

Table 1.

Structures and Cytosolic Entry Efficiencies of CPP12 Analogs

graphic file with name nihms-1810200-t0006.jpg
Peptide No. Peptide Sequencea Cytosolic Entry at
10% FBS (MFINF, %)b 		Cytosolic Entry at 1%
FBS (MFINF, %)b
X = Y = Z =
CPP12 Phe D-Phe 2-Nal 100 100
CPP12-1 Phe D-Phe 1-Nal 69 ± 9 105 ± 16
CPP12-2 Phe D-Phe Bta 375 ± 48 85 ± 7
CPP12-3 Phe D-Fpa 2-Nal 59 ± 12 83 ± 2
CPP12-4 Phe D-2-Pya 2-Nal 29 ± 9 35 ± 5
CPP12-5 Phe D-4-Pya 2-Nal 115 ± 18 36 ± 5
CPP12-6 Phe D-Tyr 2-Nal 32 ± 15 30 ± 12
CPP12-7 Fpa D-Phe 2-Nal 74 ± 9 86 ± 15
CPP12-8 2-Pya D-Phe 2-Nal 27 ± 8 41 ± 16
CPP12-9 4-Pya D-Phe 2-Nal 22 ± 9 57 ± 18
CPP12-10 Tyr D-Phe 2-Nal 25 ± 15 44 ± 10
a

Bta, L-3-benzothienylalanine; Fpa, L-4-fluorophenylalanine; D-Fpa, D-4-fluorophenylalanine; 1-Nal, L-1-naphthylalanine; 2-Nal, L-2-naphthylalanine; 2-Pya, L-2-pyridylalanine; D-2-Pya, D-2-pyridylalanine; 4-Pya, L-4-pyridylalanine; D-4-Pya, D-4-pyridylalanine.

b

All values are relative to that of CPP12 (100%) and represent the mean ± SD of three independent experiments.