ATR-101 inhibits cholesterol efflux and cortisol secretion by ABC transporters, causing cytotoxic cholesterol accumulation in adrenocortical carcinoma cells.

PubWeight™: 0.75‹?›

🔗 View Article (PMID 28710789)

Published in Br J Pharmacol on July 14, 2017

Authors

Veronica Elizabeth Burns1, Tom Klaus Kerppola1

Author Affiliations

1: Department of Biological Chemistry, University of Michigan, Ann Arbor, MI, 48109-0650.

Articles cited by this

The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. Nucleic Acids Res (2015) 10.66

The Concise Guide to PHARMACOLOGY 2015/16: Enzymes. Br J Pharmacol (2015) 5.96

Experimental design and analysis and their reporting: new guidance for publication in BJP. Br J Pharmacol (2015) 5.43

Niemann-Pick disease type C. Orphanet J Rare Dis (2010) 4.86

Cellular cholesterol trafficking and compartmentalization. Nat Rev Mol Cell Biol (2008) 4.29

Macrophage ABCA1 and ABCG1, but not SR-BI, promote macrophage reverse cholesterol transport in vivo. J Clin Invest (2007) 4.20

The LDL receptor. Arterioscler Thromb Vasc Biol (2009) 3.78

ACAT inhibition and progression of carotid atherosclerosis in patients with familial hypercholesterolemia: the CAPTIVATE randomized trial. JAMA (2009) 3.33

The Concise Guide to PHARMACOLOGY 2015/16: Transporters. Br J Pharmacol (2015) 2.74

Disruption of the acyl-CoA:cholesterol acyltransferase gene in mice: evidence suggesting multiple cholesterol esterification enzymes in mammals. Proc Natl Acad Sci U S A (1996) 2.70

Unsaturated fatty acids inhibit transcription of the sterol regulatory element-binding protein-1c (SREBP-1c) gene by antagonizing ligand-dependent activation of the LXR. Proc Natl Acad Sci U S A (2001) 2.65

High density lipoprotein deficiency and foam cell accumulation in mice with targeted disruption of ATP-binding cassette transporter-1. Proc Natl Acad Sci U S A (2000) 2.64

Transport of lipids from golgi to plasma membrane is defective in tangier disease patients and Abc1-deficient mice. Nat Genet (2000) 2.26

Mitotane Inhibits Sterol-O-Acyl Transferase 1 Triggering Lipid-Mediated Endoplasmic Reticulum Stress and Apoptosis in Adrenocortical Carcinoma Cells. Endocrinology (2015) 2.14

Integrated genomic characterization of adrenocortical carcinoma. Nat Genet (2014) 1.81

Early steps in steroidogenesis: intracellular cholesterol trafficking. J Lipid Res (2011) 1.71

The Concise Guide to PHARMACOLOGY 2015/16: Nuclear hormone receptors. Br J Pharmacol (2015) 1.62

Rapid regulation of steroidogenesis by mitochondrial protein import. Nature (2002) 1.55

Cholesterol, the central lipid of mammalian cells. Curr Opin Cell Biol (2010) 1.54

Functional loss of ABCA1 in mice causes severe placental malformation, aberrant lipid distribution, and kidney glomerulonephritis as well as high-density lipoprotein cholesterol deficiency. Am J Pathol (2000) 1.50

Effects of the acyl coenzyme A:cholesterol acyltransferase inhibitor avasimibe on human atherosclerotic lesions. Circulation (2004) 1.45

ATP binding cassette transporter G1 (ABCG1) is an intracellular sterol transporter. Proc Natl Acad Sci U S A (2011) 1.41

Coexistence of foam cells and hypocholesterolemia in mice lacking the ABC transporters A1 and G1. Circ Res (2007) 1.27

Crystallization of free cholesterol in model macrophage foam cells. Arterioscler Thromb Vasc Biol (1999) 1.19

Altered cholesterol metabolism in Niemann-Pick type C1 mouse brains affects mitochondrial function. J Biol Chem (2005) 1.18

Role of multidrug resistance P-glycoproteins in cholesterol esterification. J Biol Chem (1997) 1.18

Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide. J Lipid Res (2004) 1.15

Cellular pathology of homozygous familial hypercholesterolemia. Am J Pathol (1979) 1.15

Sterol regulation of metabolism, homeostasis, and development. Annu Rev Biochem (2011) 1.08

Comprehensive Pan-Genomic Characterization of Adrenocortical Carcinoma. Cancer Cell (2016) 1.06

Functional expression and characterization of the human ABCG1 and ABCG4 proteins: indications for heterodimerization. Biochem Biophys Res Commun (2004) 1.05

Bile salt-dependent efflux of cellular phospholipids mediated by ATP binding cassette protein B4. Hepatology (2007) 1.01

Multidrug resistance (MDR1) P-glycoprotein enhances esterification of plasma membrane cholesterol. J Biol Chem (1999) 0.98

Variability in P-glycoprotein inhibitory potency (IC₅₀) using various in vitro experimental systems: implications for universal digoxin drug-drug interaction risk assessment decision criteria. Drug Metab Dispos (2013) 0.96

ABCB1 (MDR1)-type P-glycoproteins at the blood-brain barrier modulate the activity of the hypothalamic-pituitary-adrenocortical system: implications for affective disorder. Neuropsychopharmacology (2003) 0.95

Overexpression of MDR1 in an intestinal cell line results in increased cholesterol uptake from micelles. Biochem Biophys Res Commun (2000) 0.94

A-ring modified steroidal azoles retaining similar potent and slowly reversible CYP17A1 inhibition as abiraterone. J Steroid Biochem Mol Biol (2014) 0.93

Inhibition of Acyl-CoA: cholesterol acyltransferase (ACAT), overexpression of cholesterol transporter gene, and protection of amyloid β (Aβ) oligomers-induced neuronal cell death by tricyclic pyrone molecules. J Med Chem (2012) 0.91

Reevaluation of the role of the multidrug-resistant P-glycoprotein in cellular cholesterol homeostasis. J Lipid Res (2005) 0.88

Targeted disruption of the mouse mdr1b gene reveals that steroid hormones enhance mdr gene expression. J Biol Chem (1993) 0.87

Flux analysis of cholesterol biosynthesis in vivo reveals multiple tissue and cell-type specific pathways. Elife (2015) 0.86

Expression of scavenger receptor class B type 1 (SR-BI) promotes microvillar channel formation and selective cholesteryl ester transport in a heterologous reconstituted system. Proc Natl Acad Sci U S A (2001) 0.85

Anti-atherogenic effects of the acyl-CoA:cholesterol acyltransferase inhibitor, avasimibe (CI-1011), in cultured primary human macrophages. Atherosclerosis (2002) 0.85

Deficiency in the Lipid Exporter ABCA1 Impairs Retrograde Sterol Movement and Disrupts Sterol Sensing at the Endoplasmic Reticulum. J Biol Chem (2015) 0.84

ACAT inhibitors: the search for a novel and effective treatment of hypercholesterolemia and atherosclerosis. Prog Med Chem (2002) 0.83

ATP synthesis, mitochondrial function, and steroid biosynthesis in rodent primary and tumor Leydig cells. Biol Reprod (2011) 0.83

Lysosomal acid lipase deficiency: diagnosis and treatment of Wolman and Cholesteryl Ester Storage Diseases. Pediatr Endocrinol Rev (2014) 0.83

Domestication Effects on Stress Induced Steroid Secretion and Adrenal Gene Expression in Chickens. Sci Rep (2015) 0.83

Inhibition of acyl-coenzyme A:cholesterol acyltransferase stimulates cholesterol efflux from macrophages and stimulates farnesoid X receptor in hepatocytes. Exp Mol Med (2008) 0.83

Biochemical alterations in guinea pig adrenal cortex following administration of PD 132301-2, an inhibitor of acyl-CoA:cholesterol acyltransferase. Life Sci (1995) 0.82

Inhibition of ACTH action on cultured bovine adrenal cortical cells by 2,3,7,8-tetrachlorodibenzo-p-dioxin through a redistribution of cholesterol. J Biol Chem (1986) 0.81

Mineralocorticoid insufficiency due to suramin therapy. Cancer (1996) 0.81

Toxicologic effects of a novel acyl-CoA:cholesterol acyltransferase inhibitor in cynomolgus monkeys. Toxicol Pathol (1995) 0.81

Structure-activity relationship for inhibition of CYP11B1-dependent glucocorticoid synthesis in Y1 cells by aryl methyl sulfones. Pharmacol Toxicol (1998) 0.80

Future directions in the diagnosis and medical treatment of adrenocortical carcinoma. Endocr Relat Cancer (2015) 0.80

Adrenal reserve in renal transplant recipients with cyclosporine, azathioprine, and prednisone immunosuppression. Transplantation (1990) 0.79

CYP46A1, the rate-limiting enzyme for cholesterol degradation, is neuroprotective in Huntington's disease. Brain (2016) 0.79

alpha-Substituted malonester amides: tools to define the relationship between ACAT inhibition and adrenal toxicity. J Med Chem (1998) 0.78

Efficacy and safety of mitotane in the treatment of adrenocortical carcinoma: A retrospective study in 34 Belgian patients. Ann Endocrinol (Paris) (2016) 0.76

Mitochondrial regulation of macrophage cholesterol homeostasis. Free Radic Biol Med (2015) 0.76

Inhibitory effect of synthetic progestins, 4-MA and cyanoketone on human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene-isomerase activity. J Steroid Biochem Mol Biol (1990) 0.76

Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 3. Discovery of a novel series of N-alkyl-N-[(fluorophenoxy)benzyl]-N'-arylureas with weak toxicological effects on adrenal glands. J Med Chem (1998) 0.76

Effect of 4-aminopyrazolopyrimidine and aminoglutethimide on cholesteryl metabolism and steroidogenesis in the rat adrenal. Endocrinology (1978) 0.76

Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 7. Development of a series of substituted N-phenyl-N'-[(1-phenylcyclopentyl)methyl]ureas with enhanced hypocholesterolemic activity. J Med Chem (1994) 0.76

Subacute toxicity of a novel inhibitor of acyl-CoA: cholesterol acyltransferase in beagle dogs. Fundam Appl Toxicol (1993) 0.76

Effects of intravenous and oral verapamil upon pressor and adrenal steroidogenic responses in normal man. J Clin Endocrinol Metab (1983) 0.76

Clinical and molecular review of atypical congenital adrenal hyperplasia. Ann Pediatr Endocrinol Metab (2015) 0.76

Short-term effects of ACTH on the low-density lipoprotein receptor mRNA level in rat and hamster adrenals. J Mol Endocrinol (1991) 0.76

Lack of toxic effects of F 12511, a novel potent inhibitor of acyl-coenzyme A: cholesterol O-acyltransferase, on human adrenocortical cells in culture. Biochem Pharmacol (2001) 0.76

ATR-101, a Selective and Potent Inhibitor of Acyl-CoA Acyltransferase 1, Induces Apoptosis in H295R Adrenocortical Cells and in the Adrenal Cortex of Dogs. Endocrinology (2016) 0.76

Difference between normal and WHHL rabbits in susceptibility to the adrenal toxicity of an acyl-CoA:cholesterol acyltransferase inhibitor, FR145237. Toxicol Appl Pharmacol (1996) 0.76

Inhibitors of acyl-Coa:cholesterol acyltransferase. 4. A novel series of urea ACAT inhibitors as potential hypocholesterolemic agents. J Med Chem (1993) 0.75

ATR-101 disrupts mitochondrial functions in adrenocortical carcinoma cells and in vivo. Endocr Relat Cancer (2016) 0.75