Table 1.

Clinical inhibitors and resistance mutations in HIV-1 protease.

Amino acid	L	V	G	K	L	V	D	L	E	M	K	M	I	G	I	F	I	Q	D	I	L	I	H	A	G	T	L	V	V	N	I	I	N	L	L	I
Location	10	11	16	20	24	32	30	33	34	36	43	46	47	48	50	53	54	58	60	62	63	64	69	71	73	74	76	77	82	83	84	85	88	89	90	93
Inhibitor
Saquinavir 1995	I				I									V			V			V				V	S			I	A		V				M
	R																L							T					F
	V																												T
																													S
	10			20	24	32				36		46					54							71	73		76	77	82		84				90
Indinavir 1996	I			M	I	I				I		I						V						V	S		V	I	A		V				M
	R			R								L												T	A				F
	V																												T
	10						30			36		46												71				77	82		84		88		90
Nelfinavir 1997 * w/o RTV	F						N			I		I												V				I	A		V		D		M
	I											L												T					F				S
																													T
																													S
	10					32						46	47		50		54								73		76		82		84				90
Fosamprenavir 1999, 2003	F					I						I	V		V		L								S		V		A		V				M
	I											L					V												F
	R																M												S
	V																												T
	10			20	24	32		34				46	47		50	53	54				63			71	73		76		82		84				90
Lopinavir 2000	F			M	I	I		F				I	V		V	L	V				P			V	S		V		A		V				M
	I			R								L	A				L							T					F
	R																A												T
	V																M												S
																	T
																	S
	10		16	20	24	32		34	34	36		46		48	50	53	54		60	62		64		71	73				82		84	85	88		90	93
Atazanavir 2003 *w/ and w/o RTV	I		E	R	I	I		I	Q	I		I		V	V	L	L		E	V		L		V	C				A		V	V	S		M	L
	F			M				F		L		L				Y	V					M		I	S				T							M
	V			I				V		V							M					V		T	T				F
	C			T													T							L	A				I
				V													A
	10							34		36	43	46	47				54	58					69			74			82	83	84			89
Tipranavir 2005	V							F		I	T	L	V				A	E					K			P			L	D	V			I
										L							M						R						E					M
										V							V																	V
		11				32		33					47		50		54									74	76				84			89
Darunavir 2006		I				I		F					V		V		M									P	V				V			V
																	L

Clinical inhibitors are shown with the year of approval. Major mutations are in bold and underlined.

Clinical inhibitors (PIs) and the sites of their drug resistant mutations in HIV protease. PIs are used with ritonavir unless stated.

Adapted from [21].