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(20S)-19,20,21,22-tetrahydro-19-oxo-5H-18,20-ethano-12,14-etheno-6,10-metheno-18H-benz[d]imidazo[4,3-k][1,6,9,12]oxatriaza-cyclooctadecosine-9-carbonitrile
- Development stage
- Preclinical
- Modality
- Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
01
Overview
This compound is a synthetic macrocyclic lactam classified as a macrolactam and phenylpropanoid/polyketide derivative[1][7]. It is an experimental small molecule inhibitor that targets protein farnesyltransferase/geranylgeranyltransferase type 1 subunit alpha and protein farnesyltransferase subunit beta—key enzymes involved in the post-translational modification (prenylation) of proteins such as RAS family GTPases[8]. By inhibiting these enzymes' activity (farnesylation/geranylgeranylation), the drug disrupts proper localization and function of oncogenic RAS proteins implicated in cancer cell growth and survival.
- Other names
- (5R)-30-Oxo-19-oxa‑2‑6‑10‑12-tetraazahexacyclo[18.6.2.1²⁵.1¹⁴¹⁸.0⁸¹².0²³²⁷]triaconta‑1(27),8 ,10 ,14(29),15 ,17 ,20(28),21 ,23 ,25-decaene‑17-carbonitrile
02
Targets
FNTA (Protein farnesyltransferase/geranylgeranyltransferase Type-1 subunit alpha)GGTase I (Geranylgeranyl transferase type I)FNTB (Farnesyltransferase beta subunit)
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