Table 1. List of CPPs that were Conjugated to PMO and Tested in the eGFP Assaya.
CPP name | CPP class | amino acid sequence | theoretical net charge | activity relative to PMO |
---|---|---|---|---|
arginine-12 | cationic | RRRRRRRRRRRR | 12 | 10.4 |
MPG | amphipathic | GLAFLGFLGAAGSTMGAWSQPKKKRKV | 5 | 7.5 |
Bac7 | proline rich | RRIRPRPPRLPRPRPRPLPFPRPG | 9 | 6.1 |
TAT | cationic | RKKRRQRRR | 8 | 6.0 |
arginine-10 | cationic | RRRRRRRRRR | 10 | 5.8 |
DPV6 | cationic | GRPRESGKKRKRKRLKP | 9 | 5.4 |
S413-PVrev | amphipathic | ALWKTLLKKVLKAPKKKRKV | 9 | 5.2 |
HRSV | cationic | RRIPNRRPRR | 6 | 4.9 |
HTLV-II Rex | cationic | TRRQRTRRARRNR | 8 | 4.7 |
L-2 | amphipathic | HARIKPTFRRLKWKYKGKFW | 9 | 4.6 |
melittin | amphipathic | GIGAVLKVLTTGLPALISWIKRKRQQ | 5 | 4.5 |
DPV15 | cationic | LRRERQSRLRRERQSR | 6 | 4.3 |
arginine-9 | cationic | RRRRRRRRR | 9 | 4.2 |
penetratin | cationic | RQIKIWFQNRRMKWKK | 7 | 4.2 |
yeast GCN4 | cationic | KRARNTEAARRSRARKLQRMKQ | 9 | 4.2 |
PDX-1 | cationic | RHIKIWFQN RRM KWKK | 8 | 4.1 |
arginine-8 | cationic | RRRRRRRR | 8 | 4.0 |
BMV Gag | cationic | KMTRAQRRAAARRNRWTAR | 8 | 3.9 |
SynB1 | amphipathic | RGGRLSYSRRRFSTSTGR | 6 | 3.9 |
knotted-1 | cationic | KQINNWFINQRKRHWK | 6 | 3.8 |
IVV-14 | hydrophobic | KLWMRWYSPTTRRYG | 4 | 3.7 |
W/R | amphipathic | RRWWRRWRR | 6 | 3.5 |
engrailed-2 | cationic | SQIKIWFQN KRAKIKK | 6 | 3.4 |
DPV15b | cationic | GAYDLRRRERQSRLRRRERQSR | 7 | 3.3 |
yeast PrP6 | cationic | TRRNKRNRIQEQLNRK | 6 | 3.3 |
DPV7 | cationic | GKRKKKGKLGKKRDP | 8 | 3.2 |
HoxA-13 | cationic | RQVTIWFQNRRVKEKK | 5 | 3.1 |
AIP6 | amphipathic | RLRWR | 3 | 2.9 |
(PPR)5 | cationic | PPRPPRPPRPPRPPR | 5 | 2.7 |
CAYH | CAYHRLRRC | 4 | 2.6 | |
DPV10 | cationic | SRRARRSPRHLGSG | 6 | 2.5 |
(PPR)4 | amphipathic | PPRPPRPPRPPR | 4 | 2.4 |
P22 N | cationic | NAKTRRHERRRKLAIER | 7 | 2.4 |
DPV1047 | cationic | VKRGLKLRHVRPRVTRMDV | 7 | 2.4 |
SVM4 | amphipathic | LYKKGPAKKGRPPLRGWFH | 7 | 2.2 |
cp21N(12–29) | cationic | TAKTRYKARRAELIAERR | 5 | 2.1 |
SVM3 | amphipathic | KGTYKKKLMRIPLKGT | 6 | 2.1 |
(PPR)3 | amphipathic | PPRPPRPPR | 3 | 1.9 |
SVM2 | RASKRDGSWVKKLHRILE | 5 | 1.9 | |
buforin 2 | amphipathic | TRSSRAGLQWPVGRVHRLLRK | 7 | 1.9 |
SVM1 | FKIYDKKVRTRVVKH | 6 | 1.7 | |
SAP | amphipathic | VRLPPPVRLPPPVRLPPP | 3 | 1.7 |
435b | hydrophobic | GPFHFYQFLFPPV | 1 | 1.7 |
Pept1 | hydrophobic | PLILLRLLRGQF | 2 | 1.7 |
YTA2 | YTAIAWVKAFIRKLRK | 5 | 1.5 | |
Pep-1 | Amphipathic | KETWWETWWTEWSQ PKKRKV | 2 | 1.4 |
EB-1 | amphipathic | LIRLWSHLIHIWFQNRRLKWKKK | 9 | 1.4 |
pyrrhocoricin | proline rich | VDKGSYLPRPTPPRPIYNRN | 3 | 1.4 |
AN(1–22) | cationic | MDAQTRRRERRAEKQAQWKAAN | 4 | 1.4 |
439a | hydrophobic | GSPWGLQHHPPRT | 3 | 1.3 |
MAP | amphipathic | KLALKALKALKAALKLA | 5 | 1.3 |
Bip | hydrophobic | IPALK | 1 | 1.3 |
Bip | hydrophobic | VPALR | 1 | 1.3 |
pVEC | amphipathic | LLIILRRRIRKQAHAHSK | 8 | 1.2 |
YTA4 | IAWVKAFIRKLRKGPLG | 5 | 1.2 | |
K-FGF + NLS | amphipathic | AAVLLPVLLAAPVQRKRQKLP | 4 | 1.2 |
HN-1 | hydrophobic | TSPLNIHNGQKL | 2 | 1.2 |
Bip | hydrophobic | VPTLK | 1 | 1.2 |
Bip | hydrophobic | VSALK | 1 | 1.1 |
VT5 | amphipathic | DPKGDPKGVTVTVTVTVTGKGDPKPD | 0 | 0.8 |
transportan 10 | amphipathic | AGYLLGKINLKALAALAKKIL | 4 | 0.8 |
SAP(E) | amphipathic | VELPPPVELPPPVELPPP | –3 | 0.8 |
CADY | amphipathic | GLWRALWRLLRSLWRLLWRA | 5 | 0.6 |
PreS2-TLM | amphipathic | PLSSIFSRIGDP | 0 | 0.6 |
Each previously reported CPP was synthesized, purified, and conjugated to PMO IVS2-654. The conjugates were tested for functional PMO activity in the HeLa-654 cell assay. Individual CPPs are ranked by their activity relative to unconjugated PMO.