Table 1 FPTase β mutation description... | American Society of Hematology

Table 1

FPTase β mutation description

Mutation	Cellular IC₅₀, μM	Immunoblot IC₅₀, μM	Smallest distance from lonafarnib, Å
Wild-type	0.15	0.8	—
P152S	0.05	1.7	7.3
I107V*	0.13	1	10.1
A155S	0.13	1.1	7.6
V242I	0.36	1.3	13.5
G241E†	1.1	5	11.8
C95R†	1.1	4	3.1‡
Y361H†	> 10	> 10	3.1‡
Y361L†	10.3	> 10	3.1‡
Y361S†	> 10	> 10	3.1‡
W106R†	> 10	> 10	3.4‡

Mutation	Cellular IC₅₀, μM	Immunoblot IC₅₀, μM	Smallest distance from lonafarnib, Å
Wild-type	0.15	0.8	—
P152S	0.05	1.7	7.3
I107V*	0.13	1	10.1
A155S	0.13	1.1	7.6
V242I	0.36	1.3	13.5
G241E†	1.1	5	11.8
C95R†	1.1	4	3.1‡
Y361H†	> 10	> 10	3.1‡
Y361L†	10.3	> 10	3.1‡
Y361S†	> 10	> 10	3.1‡
W106R†	> 10	> 10	3.4‡

— indicates not applicable.

Identified in a patient—not by FPTase mutagenesis.

Significant resistance in soft agar colony-forming assay (P< .05).

Distance less than 4 Å from drug to residue.