TABLE 3.
Effect of LP-52-selected resistance mutations on the helical interaction and binding stability of diverse fusion inhibitorsa
| Peptide complex | [θ]222 | Helix content (%) | Tm (°C) |
|---|---|---|---|
| T20+N39 | −8201 | 24.9 | NA |
| T20+N39V562A | −4836 | 14.7 | NA |
| T20+N39V562M | −4588 | 13.9 | NA |
| LP-52+N39 | −23162 | 70.2 | 61.1 |
| LP-52+N39V562A | −12143 | 36.8 | 45.4 |
| LP-52+N39V562M | −14978 | 45.4 | 50.7 |
| LP-80+N39 | −20960 | 63.5 | 62.8 |
| LP-80+N39V562A | −11406 | 34.6 | 39.1 |
| LP-80+N39V562M | −13426 | 40.7 | 50.6 |
| LP-83+N39 | −20647 | 62.6 | 68.4 |
| LP-83+N39V562A | −14578 | 44.2 | 58.4 |
| LP-83+N39V562M | −15897 | 48.2 | 58 |
| LP-19+N36 | −23907 | 72.4 | 51.3 |
| LP-19+N36V562A | −23282 | 70.6 | 46.6 |
| LP-19+N36V562M | −22782 | 69 | 51.2 |
| C34+N36 | −16114 | 48.8 | 45.9 |
| C34+N36V562A | −11260 | 34.1 | 39.3 |
| C34+N36V562M | −13230 | 40.1 | 42.1 |
| C34E657G+N36 | −14886 | 45.1 | 37.1 |
| C34E657G+N36V562A | −10618 | 32.2 | 31.7 |
| C34E657G+N36V562M | −9443 | 28.6 | 34.1 |
a
[θ]222, mean residue ellipticity at 222 nm; Tm, melting point melting temperature defined as the midpoint of the thermal unfolding transition; NA, not applicable.