181045-83-0
Chemical Structure
GGTI-297
- CAS No.: 181045-83-0
- Formula:C26H31N3O3S
- Molecular Weight:465.61
IUPAC Name: (4-(((R)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzoyl)-L-leucine
InChIKey: PKMVDYSKPDHRLR-KOSHJBKYSA-N
SMILES: CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O
Biological Activity: GGTI-297 is a geranylgeranyl transferase I (GGTase-1) inhibitor with IC50 values of 56 nM and 203 nM for GGTase-1 and fanesyl transferase (FTase), respectively. GGTI-297 inhibits the processing of the geranylgeranylated protein Rap1A without affecting the farnesylated protein H-Ras[1][2].
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GGTI-297 | GGTI-297 is a geranylgeranyl transferase I (GGTase-1) inhibitor with IC50 values of 56 nM and 203 nM for GGTase-1 and fanesyl transferase (FTase), respectively. GGTI-297 inhibits the processing of the geranylgeranylated protein Rap1A without affecting the farnesylated protein H-Ras. | |||||||||||||||||||||
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- [1]. Y Qian, et al. Selective inhibition of type-I geranylgeranyltransferase in vitro and in whole cells by CAAL peptidomimetics. Bioorg Med Chem. 1998 Mar;6(3):293-9. [Content Brief]
- [2]. J Sun, et al. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts. Oncogene. 1998 Mar;16(11):1467-73. [Content Brief]
Keywords
