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An inhibitor of S-palmitoylation by DHHC is 2-Bromopalmitate (2-BP). 2-BP is a nonspecific inhibitor that also halts many other lipid-processing enzymes. [7]
GANTs, or GLI inhibitors, were discovered at the National Cancer Institute. [45] GANT-58 and GANT-61 have both been shown to inhibit the GLI-mediated activation of genes. GANT-61 effectively reduced the DNA -binding affinity of GLI1 and GLI2 in multiple cancer cell lines, including rhabdomyosarcoma , [ 46 ] osteosarcoma , [ 47 ] neuroblastoma ...
Farnesyltransferase inhibitors have been developed to stop the farnesylation of Ras and therefore weaken its affinity to membranes. [2] Other inhibitors are targeting the palmitoylation cycle of Ras through inhibiting depalmitoylation by acyl-protein thioesterases, potentially leading to a destabilization of the Ras cycle. [33]
The protein palmitoylation is a reversible process. ... "Palmitoyl acyltransferase assays and inhibitors (Review)". Molecular Membrane Biology. 26 (1): 5 ...
Some members of the family such as ZDHHC3 and ZDHHC7 enhance palmitoylation of proteins such as PSD-95, SNAP-25, GAP43, Gαs. Others such as ZDHHC9 showed specificity only toward the H-Ras protein. [3] However, a recent study questions the involvement of classical enzyme-substrate recognition and specificity in the palmitoylation reaction. [4]
Palmitoylation. S-palmitoylation (i.e. attachment of palmitic acid) is a reversible protein modification in which a palmitic acid is attached to a specific cysteine residue via thioester linkage. [2] [11] The term S-acylation can also be used when other medium and long fatty acids chains are also attached to palmitoylated proteins.
Skeletal formula of tipifarnib (R115777), a farnesyltransferase inhibitor that reached Phase III clinical trials. The farnesyltransferase inhibitors (FTIs) are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras (protein), which is commonly abnormally active in cancer.
Skeletal formula of the prenyl group. Prenylation (also known as isoprenylation or lipidation) is the addition of hydrophobic molecules to a protein or a biomolecule.It is usually assumed that prenyl groups (3-methylbut-2-en-1-yl) facilitate attachment to cell membranes, similar to lipid anchors like the GPI anchor, though direct evidence of this has not been observed.