Table 2.

Selected highly resistant protease mutants and Kd for Darunavir.

Protease	Kd DRV (nM)	Relative Kd	Amino acid substitutions
Wild type	0.005	1.0
PR20†	41.000	8200	Q7K, L10F, I13V, I15V, D30N, V32I, L33F, E35D, M36I, S37N, I47V, I54L, Q58E, I62V, L63P, A71V, I84V, N88D, L89T, L90M
P51†‡	37.000	7400	L10I, I15V, K20R, L24I, V32I, I33F, M36I, M46L, I54M, I63P, K70Q, V82I, I84V, L89M
PRdrv1§	15.000	3000	L10I, M36V, M46L, I54V, I62V, L63P, A71V, V82A, I84V, L90M
PRdrv2§	0.750	150	T12V, I13V, I15V, K20M, V32I, L33F, K43T, I54L, K55N, I62V, L63P, A71V, I72V, G73S, V77I, V82L, I84V, L89V, L90M
PRdrv3§	0.004	0.82	I13V, K20R, V32I, L33F, E35D, M36I, R41K, K43T, I47V, I54M, I62V, L63V, A71V, I72T, G73S, T74P, V82L, L89V, I93L
PRdrv4§	35.000	7000	L10F, I13V, D30N, K45I, I50L, L63P, A71I, V77I, N88D
PRdrv5§	0.370	74	L10I, I13V, K14R, V32I, L33F, K43T, M46I, I47V, I54L, I62V, L63P, A71T, I72T, G73T, V77I, P79S, I84V, L90M
PRdrv6§	1.800	360	L10I, I13V, G16E, L33F, M36L, N37T, P39S, K45R, M46L, I54V, K55R, I62V, L63P, A71V, G73D, V82T, I84V, L89V, L90M, I93L

Comparison of drug resistant HIV protease variants bearing multiple substitutions and the DRV binding affinity measured by isothermal titration calorimetry. Assays used different conditions, and may not be directly comparable to each other. Major mutations from Table 1 are shown in bold and underlined.

^†Data taken from [42].

^‡Selected in vitro. Other mutants are from clinical isolates.

^§Data taken from [41].