prenylation


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pre·nyl·a·tion

(pre'nil-ā'shŭn),
The covalent addition of prenyl and multiprenyl residues to a macromolecule.
Farlex Partner Medical Dictionary © Farlex 2012
References in periodicals archive ?
The Company's lead program is in Phase 3, developing lonafarnib, a first-in-class prenylation inhibitor for the treatment of Hepatitis Delta Virus (HDV) infection.
Heterocycle-containing bisphosphonates cause apoptosis and inhibit bone resorption by preventing protein prenylation: evidence from structure-activity relationships in J774 macrophages.
[16] Blockage of the cholesterol synthetic pathway affects not only cholesterol synthesis but also other processes, such as the synthesis of isoprenoids, lipid intermediates necessary for protein prenylation; dolichol phosphate, which is involved in protein glycosylation; and ubiquinone, which is involved in respiratory chain activity.
Lonafarnib is a first-in-class, orally active inhibitor of farnesyltransferase, an enzyme involved in the modification of proteins through a process called prenylation.
Lonafarnib is a first-in-class, orally active inhibitor of farnesyltransferase, an enzyme involved in the modification of proteins through a process called prenylation. Lonafarnib has been granted Orphan Drug designation for Progeria by FDA and EMA and Breakthrough and Rare Pediatric Disease designation by FDA.
Lonafarnib is a well-characterized, late-stage, orally active inhibitor of farnesyltransferase, an enzyme involved in modification of proteins through a process called prenylation. 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.
Several studies have documented that the inhibition of protein prenylation is behind the muscle injury and results in the induction of pro-apoptotic pathways.
This latter is necessary for prenylation (the addition of a hydrophobic compound) of small GTPases, the loss of which causes activation of the inflammasome and release of IL-1[beta] [6].
Statins inhibit the PI3K pathway through the suppression of protein prenylation, activating PKA and consequently suppressing leptin expression in 3T3-L1 cells.
Dahari et al., "Oral prenylation inhibition with lonafarnib in chronic hepatitis D infection: a proofof-concept randomised, double-blind, placebo-controlled phase 2A trial," The Lancet Infectious Diseases, vol.
Baranova, "Prenylation of viral proteins by enzymes of the host: Virus-driven rationale for therapy with statins and FT/GGT1 inhibitors," BioEssays, vol.
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.