Human isoprenoid synthase enzymes as therapeutic targets.

PubWeight™: 0.86‹?›

🔗 View Article (PMC 4106277)

Published in Front Chem on July 22, 2014

Authors

Jaeok Park1, Alexios N Matralis2, Albert M Berghuis3, Youla S Tsantrizos4

Author Affiliations

1: Department of Biochemistry, McGill University Montreal, QC, Canada.
2: Department of Chemistry, McGill University Montreal, QC, Canada.
3: Department of Biochemistry, McGill University Montreal, QC, Canada ; Department of Microbiology and Immunology, McGill University Montreal, QC, Canada.
4: Department of Biochemistry, McGill University Montreal, QC, Canada ; Department of Chemistry, McGill University Montreal, QC, Canada.

Articles cited by this

(truncated to the top 100)

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev (2001) 36.00

Regulation of the mevalonate pathway. Nature (1990) 18.25

Initial genome sequencing and analysis of multiple myeloma. Nature (2011) 17.28

Statins and risk of incident diabetes: a collaborative meta-analysis of randomised statin trials. Lancet (2010) 14.24

Endocrine therapy plus zoledronic acid in premenopausal breast cancer. N Engl J Med (2009) 13.74

Small GTP-binding proteins. Physiol Rev (2001) 9.52

Risk of incident diabetes with intensive-dose compared with moderate-dose statin therapy: a meta-analysis. JAMA (2011) 8.24

Clinical features of metastatic bone disease and risk of skeletal morbidity. Clin Cancer Res (2006) 7.83

Statins and the risk of dementia. Lancet (2000) 5.65

The HSP70 chaperone machinery: J proteins as drivers of functional specificity. Nat Rev Mol Cell Biol (2010) 5.37

Upregulation of endothelial nitric oxide synthase by HMG CoA reductase inhibitors. Circulation (1998) 5.11

First-line treatment with zoledronic acid as compared with clodronic acid in multiple myeloma (MRC Myeloma IX): a randomised controlled trial. Lancet (2010) 5.04

Atherosclerosis, apolipoprotein E, and prevalence of dementia and Alzheimer's disease in the Rotterdam Study. Lancet (1997) 5.04

Breast-cancer adjuvant therapy with zoledronic acid. N Engl J Med (2011) 4.51

Statin therapy is associated with reduced neuropathologic changes of Alzheimer disease. Neurology (2007) 3.67

Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther (2001) 3.59

K- and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors. J Biol Chem (1997) 3.21

The GSK3 hypothesis of Alzheimer's disease. J Neurochem (2007) 3.16

The discovery and development of HMG-CoA reductase inhibitors. J Lipid Res (1992) 3.02

Bisphosphonates: the first 40 years. Bone (2011) 3.01

Structure-based maximal affinity model predicts small-molecule druggability. Nat Biotechnol (2007) 2.93

Prelamin A, Zmpste24, misshapen cell nuclei, and progeria--new evidence suggesting that protein farnesylation could be important for disease pathogenesis. J Lipid Res (2005) 2.88

Metabolic control of YAP and TAZ by the mevalonate pathway. Nat Cell Biol (2014) 2.84

A tagging-via-substrate technology for detection and proteomics of farnesylated proteins. Proc Natl Acad Sci U S A (2004) 2.74

The molecular mechanism of nitrogen-containing bisphosphonates as antiosteoporosis drugs. Proc Natl Acad Sci U S A (2006) 2.73

Nonpeptide antigens, presentation mechanisms, and immunological memory of human Vgamma2Vdelta2 T cells: discriminating friend from foe through the recognition of prenyl pyrophosphate antigens. Immunol Rev (2007) 2.46

Frequency and risk factors associated with osteonecrosis of the jaw in cancer patients treated with intravenous bisphosphonates. J Bone Miner Res (2008) 2.42

The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members. Clin Cancer Res (2007) 2.27

Rho GTPases, statins, and nitric oxide. Circ Res (2005) 2.21

Regulation of product chain length by isoprenyl diphosphate synthases. Proc Natl Acad Sci U S A (1996) 2.13

Crystal structure of human squalene synthase. A key enzyme in cholesterol biosynthesis. J Biol Chem (2000) 2.08

Studies on the biosynthesis of cholesterol. XX. Steric course of decarboxylation of 5-pyrophosphomevalonate and of the carbon to carbon bond formation in the biosynthesis of farnesyl pyrophosphate. J Biol Chem (1966) 2.08

Structural basis for bisphosphonate-mediated inhibition of isoprenoid biosynthesis. J Biol Chem (2003) 2.06

Gamma/delta T-cell stimulation by pamidronate. N Engl J Med (1999) 2.04

Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases. Proc Natl Acad Sci U S A (2007) 2.00

Structural basis for the exceptional in vivo efficacy of bisphosphonate drugs. ChemMedChem (2006) 1.90

Zaragozic acids: a family of fungal metabolites that are picomolar competitive inhibitors of squalene synthase. Proc Natl Acad Sci U S A (1993) 1.89

The relationship between the chemistry and biological activity of the bisphosphonates. Bone (2011) 1.86

Effect of statins on Alzheimer's disease biomarkers in cerebrospinal fluid. J Alzheimers Dis (2006) 1.82

Lipophilic bisphosphonates as dual farnesyl/geranylgeranyl diphosphate synthase inhibitors: an X-ray and NMR investigation. J Am Chem Soc (2009) 1.75

Reduction of osteonecrosis of the jaw (ONJ) after implementation of preventive measures in patients with multiple myeloma treated with zoledronic acid. Ann Oncol (2008) 1.74

Simvastatin is associated with a reduced incidence of dementia and Parkinson's disease. BMC Med (2007) 1.72

Yeast farnesyl-diphosphate synthase: site-directed mutagenesis of residues in highly conserved prenyltransferase domains I and II. Proc Natl Acad Sci U S A (1994) 1.69

A new endogenous ATP analog (ApppI) inhibits the mitochondrial adenine nucleotide translocase (ANT) and is responsible for the apoptosis induced by nitrogen-containing bisphosphonates. Br J Pharmacol (2006) 1.67

Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): tetramic, tetronic acids and dihydropyridin-2-ones. Bioorg Med Chem Lett (2008) 1.57

Direct demonstration of geranylgeranylation and farnesylation of Ki-Ras in vivo. J Biol Chem (1997) 1.57

Decreased occurrence of osteonecrosis of the jaw after implementation of dental preventive measures in solid tumour patients with bone metastases treated with bisphosphonates. The experience of the National Cancer Institute of Milan. Ann Oncol (2008) 1.56

The purification of 3,3-dimethylallyl- and geranyl-transferase and of isopentenyl pyrophosphate isomerase from pig liver. Biochem J (1967) 1.51

Analysis of the eukaryotic prenylome by isoprenoid affinity tagging. Nat Chem Biol (2009) 1.50

Structure and mechanism of the farnesyl diphosphate synthase from Trypanosoma cruzi: implications for drug design. Proteins (2006) 1.47

Osteonecrosis of the jaw and bisphosphonate treatment for osteoporosis. Bone (2008) 1.44

Zoledronic acid influences growth, migration and invasive activity of prostate cancer cells in vitro. Prostate Cancer Prostatic Dis (2012) 1.43

Nitrogen-containing bisphosphonates as carbocation transition state analogs for isoprenoid biosynthesis. Biochem Biophys Res Commun (1999) 1.39

Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase. J Med Chem (2008) 1.37

Cortical senile plaques in coronary artery disease, aging and Alzheimer's disease. Neurobiol Aging (1991) 1.37

The crystal structure of human geranylgeranyl pyrophosphate synthase reveals a novel hexameric arrangement and inhibitory product binding. J Biol Chem (2006) 1.32

Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery. Nat Chem Biol (2010) 1.30

Coronary artery disease, hypertension, ApoE, and cholesterol: a link to Alzheimer's disease? Ann N Y Acad Sci (1997) 1.26

Synthesis and biological activity of isoprenoid bisphosphonates. Bioorg Med Chem (2006) 1.25

The aging brain and cognition: contribution of vascular injury and aβ to mild cognitive dysfunction. JAMA Neurol (2013) 1.25

The neurite retraction induced by lysophosphatidic acid increases Alzheimer's disease-like Tau phosphorylation. J Biol Chem (1999) 1.24

Differential prenyl pyrophosphate binding to mammalian protein geranylgeranyltransferase-I and protein farnesyltransferase and its consequence on the specificity of protein prenylation. J Biol Chem (1997) 1.23

Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents. J Med Chem (2002) 1.22

Squalestatin 1, a potent inhibitor of squalene synthase, which lowers serum cholesterol in vivo. J Biol Chem (1992) 1.19

Biodistribution and plasma protein binding of zoledronic acid. Drug Metab Dispos (2008) 1.19

Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines. Oncogene (1997) 1.18

Colloidal aggregation affects the efficacy of anticancer drugs in cell culture. ACS Chem Biol (2012) 1.17

The pharmacokinetics and pharmacodynamics of zoledronic acid in cancer patients with varying degrees of renal function. J Clin Pharmacol (2003) 1.16

alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase. J Med Chem (1996) 1.15

The antiresorptive effects of a single dose of zoledronate persist for two years: a randomized, placebo-controlled trial in osteopenic postmenopausal women. J Clin Endocrinol Metab (2008) 1.14

Farnesyl pyrophosphate synthetase. Mechanistic studies of the 1'-4 coupling reaction with 2-fluorogeranyl pyrophosphate. J Biol Chem (1978) 1.11

Regulation of the brain isoprenoids farnesyl- and geranylgeranylpyrophosphate is altered in male Alzheimer patients. Neurobiol Dis (2009) 1.09

A comparative study of the in vitro antioxidant activity of statins. Int J Cardiol (2003) 1.09

Lipid-lowering properties of TAK-475, a squalene synthase inhibitor, in vivo and in vitro. Br J Pharmacol (2003) 1.07

Massive production of farnesol-derived dicarboxylic acids in mice treated with the squalene synthase inhibitor zaragozic acid A. Arch Biochem Biophys (1998) 1.06

Synthesis of novel 4,1-benzoxazepine derivatives as squalene synthase inhibitors and their inhibition of cholesterol synthesis. J Med Chem (2002) 1.05

Targeting the undruggable proteome: the small molecules of my dreams. Chem Biol (2010) 1.03

RPR 107393, a potent squalene synthase inhibitor and orally effective cholesterol-lowering agent: comparison with inhibitors of HMG-CoA reductase. J Pharmacol Exp Ther (1997) 1.03

Lipophilic pyridinium bisphosphonates: potent gammadelta T cell stimulators. Angew Chem Int Ed Engl (2010) 1.03

Synthesis and biological evaluation of a series of aromatic bisphosphonates. Bioorg Med Chem (2010) 1.03

How do bisphosphonates inhibit bone metastasis in vivo? Neoplasia (2010) 1.03

Crystallization and partial characterization of prenyltransferase from avian liver. Biochemistry (1975) 1.02

Farnesyl diphosphate synthase inhibitors from in silico screening. Chem Biol Drug Des (2013) 1.02

Bisphosphonates for postmenopausal osteoporosis. Bone (2011) 1.01

Blunted Akt/FOXO signalling and activation of genes controlling atrophy and fuel use in statin myopathy. J Physiol (2008) 1.01

Phase II trial of tipifarnib plus neoadjuvant doxorubicin-cyclophosphamide in patients with clinical stage IIB-IIIC breast cancer. Clin Cancer Res (2009) 1.00

Squalene synthase: a critical enzyme in the cholesterol biosynthesis pathway. Clin Genet (2008) 0.98

Isoprenoids, small GTPases and Alzheimer's disease. Biochim Biophys Acta (2010) 0.98

A peptide prodrug approach for improving bisphosphonate oral absorption. J Med Chem (2000) 0.98

Biomedical applications of bisphosphonates. J Control Release (2013) 0.98

Indirect stimulation of human Vγ2Vδ2 T cells through alterations in isoprenoid metabolism. J Immunol (2011) 0.97

Squalene synthase: structure and regulation. Prog Nucleic Acid Res Mol Biol (2001) 0.97

1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate. J Med Chem (1995) 0.97

Bisphosphonates induce autophagy by depleting geranylgeranyl diphosphate. J Pharmacol Exp Ther (2011) 0.97

Effects of induction and maintenance plus long-term bisphosphonates on bone disease in patients with multiple myeloma: the Medical Research Council Myeloma IX Trial. Blood (2012) 0.96

Lately, it occurs to me what a long, strange trip it's been for the farnesyltransferase inhibitors. J Clin Oncol (2006) 0.96

Design and synthesis of active site inhibitors of the human farnesyl pyrophosphate synthase: apoptosis and inhibition of ERK phosphorylation in multiple myeloma cells. J Med Chem (2012) 0.95

Targeting of therapeutic agents to bone to treat metastatic cancer. Adv Drug Deliv Rev (2005) 0.95

Reduced expression of the mevalonate pathway enzyme farnesyl pyrophosphate synthase unveils recognition of tumor cells by Vgamma9Vdelta2 T cells. J Immunol (2009) 0.95

Current progress in Structure-Based Rational Drug Design marks a new mindset in drug discovery. Comput Struct Biotechnol J (2013) 0.95