TABLE 1.

Association rate constants of interactions between the HIV-1 proteases and ligands

Enzyme	Inhibitor	No.of atoms	M−1s−1	M−1s−1
Wild-type	Amprenavir	70	>5.00 × 106
	Indinavir	94	2.4 × 106 ± 0.3 × 106
	Saquinavir	100	1.1 × 106 ± 0.2 × 106
	Substrate	∼150	104–10 6
Mutant	Amprenavir	70	>5.00 × 106	>5.00 × 106
L90M	Indinavir	94	>5.00 × 106	∼2.4 × 106
	Saquinavir	100	1.7 × 106 ± 0.7 × 106	∼1.1 × 106
	Substrate	∼150	n.a.	∼104–106
Mutant	Amprenavir	70	3.3 × 106 ± 0.8 × 106	>5.00 × 106
G48V	Indinavir	94	2.3 × 106 ± 0.6 × 106	∼2.4 × 106
	Saquinavir	100	2.1 × 106 ± 0.7 × 106	∼1.1 × 106
	Substrate	∼150	n.a.	∼104–106
Mutant	Amprenavir	70	1.0 × 106 ± 0.1 × 106	∼106
G48V/V82A/I84V/L90M	Indinavir	94	7.2 × 105 ± 0.5 × 105	∼3.4 × 105
	Saquinavir	100	3.3 × 105 ± 1.1 × 105	∼1.5 × 105
	Substrate	∼150	n.a.	∼103–105

The experimental values of HIV drugs are taken from an article by Shuman et al. (29) and the data of the substrates are from references of Katoh et al. (5) and Szeltner et al. (46) (n.a., not available).