Table 2. Effect of FTase inhibitors on... | American Society of Hematology

Table 2.

Effect of FTase inhibitors on intact cells

Compound	Cell type	RASmutation	Ras activation	IC₅₀ μmol/L	Reference nos.
L-731,734	Fibroblasts	v-RAS	+	1	128
L-739,749	Rat-1 fibroblasts		+	2.5	130
					167
	JMML cells		+	1-10	132
B581	NIH3T3 cells	f-RAS	+	−	138
BZA-5B	Rat-1 cells	H-RAS	+	−	125, 126
BZA-2B					166, 167
B956, B1086	Human tumor cell lines	H-RAS	+	0.2-0.7	144
		N-RAS	+	3-7
		K-RAS	+	1.7-50
SCH44342	Cos cells	H-RAS	+	−	145
	Various human tumor cell lines	H-, N-, K-RAS	+/−	1	136
L-744,832	JMML cells		+	1-10	132
Compound no. 46	NIH3T3	H-RAS	+	0.19	187
FTI-277	Glioma cell lines			2.5-15.5	142
Compound no. 10	Rat-1 cells	v-RAS	+	2.5-5	185
Compound 5m	NIH3T3 cells	H-RAS-F	+	0.18	186
FTS^*	Rat-1 cells	N-RAS	+	30-40^*	188
	Human melanoma cell lines	N-RAS	+/−	100^*

Compound	Cell type	RASmutation	Ras activation	IC₅₀ μmol/L	Reference nos.
L-731,734	Fibroblasts	v-RAS	+	1	128
L-739,749	Rat-1 fibroblasts		+	2.5	130
					167
	JMML cells		+	1-10	132
B581	NIH3T3 cells	f-RAS	+	−	138
BZA-5B	Rat-1 cells	H-RAS	+	−	125, 126
BZA-2B					166, 167
B956, B1086	Human tumor cell lines	H-RAS	+	0.2-0.7	144
		N-RAS	+	3-7
		K-RAS	+	1.7-50
SCH44342	Cos cells	H-RAS	+	−	145
	Various human tumor cell lines	H-, N-, K-RAS	+/−	1	136
L-744,832	JMML cells		+	1-10	132
Compound no. 46	NIH3T3	H-RAS	+	0.19	187
FTI-277	Glioma cell lines			2.5-15.5	142
Compound no. 10	Rat-1 cells	v-RAS	+	2.5-5	185
Compound 5m	NIH3T3 cells	H-RAS-F	+	0.18	186
FTS^*	Rat-1 cells	N-RAS	+	30-40^*	188
	Human melanoma cell lines	N-RAS	+/−	100^*

Several FTase inhibitors have been demonstrated to revert specifically the Ras-transformed phenotype and anchorage-independent growth in fibroblasts and human tumor cell lines. Cell growth inhibition may be a result of induction of apoptosis or arrest in the G1 phase of the cell cycle.

+ indicates positive for activated Ras; −, negative for activated Ras.

FTS, S-farnesylthiosalicyclic acid, is an inhibitor of PPMTase.

View Large

This Feature Is Available To Subscribers Only