Alkyl and Aryl Transferases
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Subject Areas on Research
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3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
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A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity.
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A phase II window trial of procarbazine and topotecan in children with high-grade glioma: a report from the children's oncology group.
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Aberrant dolichol chain lengths as biomarkers for retinitis pigmentosa caused by impaired dolichol biosynthesis.
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Absence of the CAAX endoprotease Rce1: effects on cell growth and transformation.
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COQ2 nephropathy: a newly described inherited mitochondriopathy with primary renal involvement.
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Caged protein prenyltransferase substrates: tools for understanding protein prenylation.
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Characterization of a zinc finger DNA-binding protein expressed specifically in Petunia petals and seedlings.
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Characterization of cis-regulatory regions responsible for developmental regulation of the gibberellin biosynthetic gene GA1 in Arabidopsis thaliana
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Cocrystal structure of protein farnesyltransferase complexed with a farnesyl diphosphate substrate.
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Control of antiviral innate immune response by protein geranylgeranylation.
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Conversion of Tyr361 beta to Leu in mammalian protein farnesyltransferase impairs product release but not substrate recognition.
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Conversion of protein farnesyltransferase to a geranylgeranyltransferase.
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Crystal structure of farnesyl protein transferase complexed with a CaaX peptide and farnesyl diphosphate analogue.
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Crystal structure of protein farnesyltransferase at 2.25 angstrom resolution.
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Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity.
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Crystallographic analysis of CaaX prenyltransferases complexed with substrates defines rules of protein substrate selectivity.
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Crystallographic analysis reveals that anticancer clinical candidate L-778,123 inhibits protein farnesyltransferase and geranylgeranyltransferase-I by different binding modes.
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Della proteins and gibberellin-regulated seed germination and floral development in Arabidopsis.
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Developmental regulation of the gibberellin biosynthetic gene GA1 in Arabidopsis thaliana.
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Discovery of geranylgeranyltransferase-I inhibitors with novel scaffolds by the means of quantitative structure-activity relationship modeling, virtual screening, and experimental validation.
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Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis.
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Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
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Effects of pharmacologic inhibition of protein geranylgeranyltransferase type I on aqueous humor outflow through the trabecular meshwork.
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Elevated DNA polymerase alpha, DNA polymerase beta, and DNA topoisomerase II in a melphalan-resistant rhabdomyosarcoma xenograft that is cross-resistant to nitrosoureas and topotecan.
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Enzymology and biology of CaaX protein prenylation.
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Evidence for a catalytic role of zinc in protein farnesyltransferase. Spectroscopy of Co2+-farnesyltransferase indicates metal coordination of the substrate thiolate.
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Expression of functional bacterial undecaprenyl pyrophosphate synthase in the yeast rer2{Delta} mutant and CHO cells.
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Farnesylation of YDJ1p is required for function at elevated growth temperatures in Saccharomyces cerevisiae.
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Farnesylation of nonpeptidic thiol compounds by protein farnesyltransferase.
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Farnesyltransferase inhibitors alter the prenylation and growth-stimulating function of RhoB.
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GGTase-I deficiency reduces tumor formation and improves survival in mice with K-RAS-induced lung cancer.
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Genetic characterization and functional analysis of the GID1 gibberellin receptors in Arabidopsis.
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Genetic variants in PDSS1 and SLC16A6 of the ketone body metabolic pathway predict cutaneous melanoma-specific survival.
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H-Ras peptide and protein substrates bind protein farnesyltransferase as an ionized thiolate.
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High affinity for farnesyltransferase and alternative prenylation contribute individually to K-Ras4B resistance to farnesyltransferase inhibitors.
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High level expression of mammalian protein farnesyltransferase in a baculovirus system. The purified protein contains zinc.
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Identification of a cysteine residue essential for activity of protein farnesyltransferase. Cys299 is exposed only upon removal of zinc from the enzyme.
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Influence of metal ions on substrate binding and catalytic activity of mammalian protein geranylgeranyltransferase type-I.
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Inhibition of purified p21ras farnesyl:protein transferase by Cys-AAX tetrapeptides.
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Intraarterial O6-benzylguanine enables the specific therapy of nitrosourea-resistant intracranial human glioma xenografts in athymic rats with 1,3-bis(2-chloroethyl)-1-nitrosourea.
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Isolation of protein prenyltransferases from bovine brain and baculovirus expression system.
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Kinetic analysis of zinc ligand mutants of mammalian protein farnesyltransferase.
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Kinetic studies of protein farnesyltransferase mutants establish active substrate conformation.
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Kinetics of protein farnesyltransferase: sigmoidal vs hyperbolic behavior as a function of assay conditions.
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Ligation of the alpha2M* signaling receptor regulates synthesis of cytosolic phospholipase A2.
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Long-Chain Polyprenols Promote Spore Wall Formation in Saccharomyces cerevisiae.
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Lysine(164)alpha of protein farnesyltransferase is important for both CaaX substrate binding and catalysis.
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Mammalian protein geranylgeranyltransferase. Subunit composition and metal requirements.
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Mechanisms of protein prenylation and role in G protein function.
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New fungal metabolite geranylgeranyltransferase inhibitors with antifungal activity.
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Non-peptidic, non-prenylic inhibitors of the prenyl protein-specific protease Rce1.
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Nonsyndromic Retinitis Pigmentosa in the Ashkenazi Jewish Population: Genetic and Clinical Aspects.
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Overexpression of AtCPS and AtKS in Arabidopsis confers increased ent-kaurene production but no increase in bioactive gibberellins.
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Phase I and pharmacokinetic study of lonafarnib, SCH 66336, using a 2-week on, 2-week off schedule in patients with advanced solid tumors.
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Phase II and pharmacodynamic study of the farnesyltransferase inhibitor R115777 as initial therapy in patients with metastatic pancreatic adenocarcinoma.
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Post-prenylation-processing enzymes as new targets in oncogenesis.
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Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I.
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Prenylated c17orf37 induces filopodia formation to promote cell migration and metastasis.
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Prenylation and G protein signaling.
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Properties and kinetic mechanism of recombinant mammalian protein geranylgeranyltransferase type I.
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Protein Geranylgeranyltransferase Type 1 as a Target in Cancer.
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Protein farnesyltransferase and geranylgeranyltransferase share a common alpha subunit.
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Protein farnesyltransferase in embryogenesis, adult homeostasis, and tumor development.
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Protein farnesyltransferase.
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Protein farnesyltransferase: kinetics of farnesyl pyrophosphate binding and product release.
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Protein prenylation: unique fats make their mark on biology.
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Protein prenyltransferases.
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Proteolysis-independent downregulation of DELLA repression in Arabidopsis by the gibberellin receptor GIBBERELLIN INSENSITIVE DWARF1.
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Rapid analysis of protein farnesyltransferase substrate specificity using peptide libraries and isoprenoid diphosphate analogues.
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Reaction path of protein farnesyltransferase at atomic resolution.
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Recessive-interfering mutations in the gibberellin signaling gene SLEEPY1 are rescued by overexpression of its homologue, SNEEZY.
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Resistance mutations at the lipid substrate binding site of Plasmodium falciparum protein farnesyltransferase.
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Restricted substrate specificity for the geranylgeranyltransferase-I enzyme in Cryptococcus neoformans: implications for virulence.
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Role of farnesyltransferase in ABA regulation of guard cell anion channels and plant water loss.
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Structure of mammalian protein geranylgeranyltransferase type-I.
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Structure of protein geranylgeranyltransferase-I from the human pathogen Candida albicans complexed with a lipid substrate.
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Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase.
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Structures of Cryptococcus neoformans protein farnesyltransferase reveal strategies for developing inhibitors that target fungal pathogens.
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Substitution of cadmium for zinc in farnesyl:protein transferase alters its substrate specificity.
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Substrate binding is required for release of product from mammalian protein farnesyltransferase.
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Synthesis of isomeric 3-piperidinyl and 3-pyrrolidinyl benzo[5,6]cyclohepta[1,2-b]pyridines: sulfonamido derivatives as inhibitors of Ras prenylation.
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The Arabidopsis F-box protein SLEEPY1 targets gibberellin signaling repressors for gibberellin-induced degradation.
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The Arabidopsis GA1 locus encodes the cyclase ent-kaurene synthetase A of gibberellin biosynthesis.
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The Arabidopsis SLEEPY1 gene encodes a putative F-box subunit of an SCF E3 ubiquitin ligase.
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The GA2 locus of Arabidopsis thaliana encodes ent-kaurene synthase of gibberellin biosynthesis.
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The LS locus of pea encodes the gibberellin biosynthesis enzyme ent-kaurene synthase A.
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The RAM1 gene encoding a protein-farnesyltransferase beta-subunit homologue is essential in Cryptococcus neoformans.
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The basis for K-Ras4B binding specificity to protein farnesyltransferase revealed by 2 A resolution ternary complex structures.
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The crystal structure of human protein farnesyltransferase reveals the basis for inhibition by CaaX tetrapeptides and their mimetics.
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The farnesyl protein transferase inhibitor SCH66336 is a potent inhibitor of MDR1 product P-glycoprotein.
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The synergistic combination of the farnesyl transferase inhibitor lonafarnib and paclitaxel enhances tubulin acetylation and requires a functional tubulin deacetylase.
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Thematic review series: lipid posttranslational modifications. Structural biology of protein farnesyltransferase and geranylgeranyltransferase type I.
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cDNA cloning and expression of rat and human protein geranylgeranyltransferase type-I.