LaminB1 also undergoes some forms of post-translational modifications, such as
farnesylation [29], phosphorylation, glycosylation, and sumoylation [30], which are linked to the significant conformational changes of their target proteins [31].
Lonafarnib blocks the
farnesylation of progerin and has been dosed in over 80 children with Progeria at Boston Children's Hospital in Phase 1/2 and Phase 2 studies funded by The Progeria Research Foundation.
Lonafarnib blocks the
farnesylation of progerin and has been dosed in over 80 children at Boston's Children Hospital in Phase 1/2 and Phase 2 studies.
Tipifarnib is an inhibitor of
farnesylation, a key cell signalling process implicated in cancer initiation and resistance to standard therapies.
A hypothesis on the mechanism of inhibition in anticancer activity indicates that SQ reduces the activity of the HMG-CoA reductase enzyme by limiting the steps towards normal cholesterol synthesis and intermediate stages where geranyl diphosphate (GDP) and farnesyl diphosphate (FDP) produce important substrates for the biosynthesis of ubiquinones and for the prenylation (
farnesylation) of proteins.
Kondo et al., "C-terminal
farnesylation of UCH-L1 plays a role in transport of Epstein-Barr virus primary oncoprotein LMP1 to exosomes," mSphere, vol.
Since isoprenoids, such as geranylgeranyl pyrophosphate and farnesyl pyrophosphate, are able to revert rosuvastatin effect on PAI-1 expression, protein geranylation or/and
farnesylation could be one involved mechanism [69].
Kirschmeier, "The farnesyl transferase inhibitor (FTI) SCH66336 (lonafarnib) inhibits Rheb
farnesylation and mTOR signaling.
Molecular tailoring of
farnesylation for plant drought tolerance and yield protection.
In in vitro studies of inhibition by DHEA of protein geranylation and
farnesylation (together referred to as protein isoprenylation), we had demonstrated that the block to protein isoprenylation could be relieved by the addition of the isoprene donor geraniol [6, 7].
Lu, "Zoledronate blocks geranylgeranylation not
farnesylation to suppress human osteosarcoma U2OS cells metastasis by EMT via Rho A activation and FAK-inhibited JNK and p38 pathways," Oncotarget, vol.