TABLE 1.
Names, sequences, and antiviral activities of TAT peptides
| Peptide (charge)a | Sequenceb | Activityc
|
||
|---|---|---|---|---|
| Entry inhibitiond | Cellular resistancee | Virus inactivationf | ||
| TAT0 (+9) | NH2GRKKRRQRRRCONH2 | 1.0 | >1,200* | >1,200 |
| TAT-Pd0 (+9) | NH2GRKKRRQRRRPCONH2 | 0.7 | >1,200* | 1,050 |
| TAT-Cd0 (+9) | NH2GRKKRRQRRRCCONH2 | 0.9 (SH), 0.6 (SS) | 1.1-2.4 (SH), 0.4 (SS) | 200-330 (SH), 34 (SS) |
| TAT-Cd− (+8) | NH2GRKKRRQRRRCCOOH | 2.5 | 5.4-10 | 150-290 |
| bTAT-Cd− (+7) | b-GRKKRRQRRRCCOOH | 2.1 | ND | ND |
| TAT-C0 (+9) | NH2GRKKRRQRRRCCONH2 | 0.9 (SH) | 3.9-6.7 (SH) | 390 (SH) |
| bTAT-C0 (+8) | b-GRKKRRQRRRCCONH2 | 5.7 | ND | ND |
| n50,51TAT-C0 (+7) | NH2GRnnRRQRRRCCONH2 | 9.6 | 92 | 115 (SH) |
| TAT-C− (+8) | NH2GRKKRRQRRRCCOOH | 3.1 | 3.3-4.5 | 96-110 |
| n50,51TAT-C− (+6) | NH2GRnnRRQRRRCCOOH | 34-48 | >1,200* | ∼900 |
| n55,56TAT-C− (+6) | NH2GRKKRRQnnRCCOOH | 48 | 230 | ∼900 |
| bn55,56TAT-C− (+5) | b-GRKKRRQnnRCCOOH | 37 | ND | ND |
Names have superscripts indicating whether the C terminus bears a carboxyl group (−) or an amide (0). Numbers in parentheses refer to the nominal net charge of the peptides at neutral pH.
Amino acid sequences are given in single-letter code. Norleucine is represented by “n.” Boldface type indicates d-enantiomers. In some peptides, the N-terminal amino group is replaced by biotin-aminohexanoyl (b).
All activities are given as micromolar EC50s obtained from single dose-response curves based on triplicate determinations at each peptide concentration (cf. Fig. 1, 4, and 6). In some cases, the range of EC50s obtained from multiple response curves is indicated. Activities of cysteine-substituted peptides refer to the monomeric (SH) or dimeric (SS) forms of peptides or to mixtures of the two (unmarked, in monomeric concentrations). Asterisks indicate that cellular susceptibility to infection is enhanced rather than inhibited at or below a peptide concentration of 1,200 μM (see Fig. 6). ND, not determined.
Virus is attached to cells for 1 h at 4°C, peptide is added, and cultures are infected for 1 h at 37°C.
Cells are exposed to peptide for 1 h at 37°C, rinsed, and infected for 1 h at 37°C.
Virions are exposed to peptides for 1 h at 37°C and then diluted or pelleted to remove free peptide prior to infection for 1 h at 37°C.