Therapeutic potential of CPT I inhibitors: Cardiac gene transcription as a target

Expert Opinion on Investigational Drugs

Volumn 11, Issue 3, 2002, Pages 345-356

  Zarain Herzberg, Angel ^a   Rupp, Heinz ^a  

^a UNIVERSIDAD NACIONAL AUTÓNOMA DE MÉXICO   (Mexico)

Author keywords

2 tetradecylglycidic acid; Carnitine palmitoyl transferase; Etomoxir; Gene expression; Heart failure; Myosin; Promoter; Sarcoplasmic reticulum; SERCA; Transcription factor

Indexed keywords

5 (4 CHLOROPHENYL) 2 (4 METHYLPHENYLSULFONYL) 4 PENTYNOIC ACID; ACYL COENZYME A; ACYLTRANSFERASE INHIBITOR; ADENOSINE TRIPHOSPHATASE (CALCIUM); ANTIDIABETIC AGENT; CALCINEURIN INHIBITOR; CARNITINE PALMITOYLTRANSFERASE; CLOMOXIR; CYCLOSPORIN A; ETOMOXIR; GLUCOSE; LIOTHYRONINE; MYOSIN HEAVY CHAIN; PALMOXIRIC ACID; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PHOSPHATASE; PHOSPHATE; PHOSPHOLAMBAN; PIRINIXIC ACID; SDZ CPI 975; TACROLIMUS; UNCLASSIFIED DRUG; ATP2A2 PROTEIN, HUMAN; ATP2A2 PROTEIN, MOUSE; ATP2A2 PROTEIN, RAT; ENZYME INHIBITOR; EPOXIDE; SARCOPLASMIC RETICULUM CALCIUM TRANSPORTING ADENOSINE TRIPHOSPHATASE;

ANIMAL MODEL; DRUG MECHANISM; DRUG TARGETING; ENZYME INHIBITION; FATTY ACID OXIDATION; GENE EXPRESSION REGULATION; GENETIC TRANSCRIPTION; HEART FAILURE; HEART FUNCTION; HEART MUSCLE; HEART MUSCLE CELL; HEART WORK; HUMAN; HYPERTROPHY; HYPOTHESIS; INSULIN DEPENDENT DIABETES MELLITUS; MITOCHONDRION; MOUSE; NONHUMAN; PROMOTER REGION; PROTEIN EXPRESSION; RABBIT; RAT; REVIEW; SARCOPLASMIC RETICULUM; SIGNAL TRANSDUCTION; ANIMAL; CONGESTIVE HEART FAILURE; DRUG ANTAGONISM; DRUG EFFECT; ENZYMOLOGY; GENETICS; MOLECULAR GENETICS; SEQUENCE HOMOLOGY; TRANSACTIVATION;

ANIMALS; CALCIUM-TRANSPORTING ATPASES; CARNITINE O-PALMITOYLTRANSFERASE; ENZYME INHIBITORS; EPOXY COMPOUNDS; GENE EXPRESSION REGULATION, ENZYMOLOGIC; HEART FAILURE, CONGESTIVE; HUMANS; MICE; MOLECULAR SEQUENCE DATA; MYOCYTES, CARDIAC; MYOSIN HEAVY CHAINS; RABBITS; RATS; SARCOPLASMIC RETICULUM; SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES; SEQUENCE HOMOLOGY, AMINO ACID; TRANS-ACTIVATION (GENETICS);

EID: 0036195453     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.11.3.345     Document Type: Review

References (78)

1. Inhibition of mitochondrial carnitine palmitoyl transferase by 2-tetradecylglycidic acid (McN-3802) (preliminary communication)
2. Synthesis and hypoglycemic activity of phenylalkyloxiranecarboxylic acid derivatives
3. Decrease of fatty acid oxidation, ketogenesis and gluconeogenesis in isolated perfused rat liver by phenylalkyl oxirane carboxylate (B 807-27) due to inhibition of CPT I (EC 2.3.1.21)
4. Improvement of myocardial function and metabolism in diabetic rats by the carnitine palmitoyl transferase inhibitor Etomoxir
5. Effects of the carnitine-acyltransferase inhibitor etomoxir on insulin sensitivity, energy expenditure and substrate oxidation in NIDDM
6. Pioglitazone hydrochloride monotherapy improves glycemic control in the treatment of patients with Type 2 diabetes: A 6-month randomized placebo-controlled dose-response study
7. Hypoglycemic effects of a novel fatty acid oxidation inhibitor in rats and monkeys
8. Effects of carnitine palmitoyltransferase I inhibitors on hepatic hypertrophy
9. Transcriptional modulators targeted at fuel metabolism of hypertrophied heart
10. First clinical trial with etomoxir in patients with chronic congestive heart failure
11. Etomoxir: A new approach to treatment of chronic heart failure
12. Heart failure: The ironic failure of success
13. Control of cardiac myosin heavy chain gene expression
14. Calcium regulatory proteins and their alteration by transgenic approaches
15. SERCA pump level is a critical determinant of Ca(2+)homeostasis and cardiac contractility
16. Diastolic dysfunction of the heart: Pharmacological strategies for modulating calcium sequestration of the sarcoplasmic reticulum
17. Diastolic dysfunction: Pathophysiology, clinical features and assessment with radionuclide methods
18. Relation between myocardial function and expression of sarcoplasmic reticulum Ca(2+)-ATPase in failing and nonfailing human myocardium
19. Sarcoplasmic reticulum function and carnitine palmitoyltransferase-1 inhibition during progression of heart failure
20. Signaling pathways responsible for fetal gene induction in the failing human heart: Evidence for altered thyroid hormone receptor gene expression
21. Regulation of thyroid hormone receptor isoforms in physiological and pathological cardiac hypertrophy
22. Development of a thyroid hormone analogue for the treatment of congestive heart failure
23. Prevention of abnormal sarcoplasmic reticulum calcium transport and protein expression in post-infarction heart failure using 3,5-diiodothyropropionic acid (DITPA)
24. Remodelling of the myocyte at a molecular level - Relationship between myosin isozyme population and sarcoplasmic reticulum
25. Diabetes-like action of intermittent fasting on sarcoplasmic reticulum Ca2+-pump ATPase and myosin isoenzymes can be prevented by sucrose
26. Differences in glucagon-like peptide-1 and GIP responses following sucrose ingestion
27. Sucrose feeding prevents changes in myosin isoenzymes and sarcoplasmic reticulum Ca2+-pump ATPase in pressure-loaded rat heart
28. Influence of diet and carnitine palmitoyltransferase I inhibition on myosin and sarcoplasmic reticulum
29. Modification of subcellular organelles in pressure-overloaded heart by etomoxir, a carnitine palmitoyltransferase I inhibitor
30. CPT-1 inhibition by etomoxir has a chamber-related action on cardiac sarcoplasmic reticulum and isomyosins
31. Dietary medium-chain triglycerides can prevent changes in myosin and SR due to CPT-1 inhibition by etomoxir
32. Modification of sarcoplasmic reticulum gene expression in pressure overload cardiac hypertrophy by etomoxir
33. Differential influences of carnitine palmitoyltransferase-1 inhibition and hyperthyroidism on cardiac growth and sarcoplasmic reticulum phosphorylation
34. Etomoxir improves left ventricular performance of pressure-overloaded rat heart
35. Differential influence of fasting and BM13.907 treatment on growth and phenotype of pressure overloaded rat heart
36. Etomoxir-induced PPARα-modulated enzymes protect during acute renal failure
37. Deactivation of peroxisome proliferator-activated receptor-α during cardiac hypertrophic growth
38. Diabetes mellitus and hypothyroidism induce changes in myosin isoenzyme distribution in the rat heart-do alterations in fuel flux mediate these changes?
39. Substituted 2-oxiranecarboxylic acids: A new group of candidate hypoglycaemic drugs
40. 2+-ATPase
41. 2+-ATPase gene
42. 2+-ATPase and myosin heavy chain alpha gene expression in cardiac myocytes. Delineation of cis-active DNA elements that confer thyroid hormone but not to retinoic acid
43. 2+-ATPase (SERCA2) gene promoter
44. Structure and organization of the mouse Atp2a2 gene encoding the sarco(endo)plasmic reticulum Ca2+-ATPase 2 (SERCA2) isoforms
45. 2+-ATPase gene promoter are required for expression in Sol8 muscle cells
46. 2+-ATPase (SERCA2) gene
47. Mechanism of doxorubicin-induced inhibition of sarcoplasmic reticulum Ca(2+)-ATPase gene transcription
48. TAFII250, Egr-1 and D-type cyclin expression in mice and neonatal rat cardiomyocytes treated with doxorubicin
49. Early growth response protein 1 (Egr-1): Prototype of a zinc-finger family of transcription factors
50. A role for Sp and nuclear receptor transcription factors in a cardiac hypertrophic growth program
51. Calcineurin plays a critical role in pressure overload-induced cardiac hypertrophy
52. Calcineurin plays a critical role in the development of pressure overload-induced cardiac hypertrophy
53. 2+-ATPase gene
54. 2+-ATPase gene. Demonstration that retinoid X receptor binds 5′ to thyroid hormone receptor in response element 1
55. 2+-adenosine triphosphatase gene is increased by 3,5,3′-triiodothyronine receptor isoform-specific interactions with the myocyte-specific enhancer factor-2a
56. Sarcoplasmic reticulum proteins in heart failure
57. 2+-ATPase during progression of left ventricular hypertrophy
58. 2+-ATPase gene is regulated at the transcriptional level during compensated left ventricular hypertrophy in the rat
59. Transcription of the SERCA2 gene is decreased in pressure-overloaded hearts: A study using in vivo direct gene transfer into living myocardium
60. 2+-ATPase (SERCA2) gene promoter activity is decreased in response to severe left ventricular pressure-overload hypertrophy in rat hearts
61. 2+-ATPase (SERCA2) gene in pressure-overloaded heart: A study using in vivo direct gene transfer into living myocardium
62. Activation of the MKK6-p38-MAPK pathway in cardiac myocytes prolongs the decay phase of the contractile calcium transient, downregulates SERCA2 expression and activates NF-AT-dependent gene expression in contraction-dependent manner
63. PPAR signaling in the control of cardiac energy metabolism
64. p38 Mitogen-activated Protein Kinase Activates Peroxisome Proliferator-activated Receptor alpha. A potential role in the cardiac metabolic stress response
65. 2+-ATPase gene expression in cultured vascular smooth-muscle cells: Role of glucose-6-phosphate
66. Long-chain fatty acid-induced changes in gene expression in neonatal cardiac myocytes
67. Identification of a contractile-responsive element in the cardiac alpha-myosin heavy chain gene
68. Regulation of cardiac alpha-myosin heavy chain gene transcription by a contractile-responsive E-box binding protein
69. Myosin isoenzyme expression in rat ventricle: Effects of thyroid hormone analogs, catecholamines, glucocorticoids and high carbohydrate diet
70. Myosin isoenzyme distribution and Ca+2-activated myosin ATPase activity in the rat heart is influenced by fructose feeding and triiodothyronine
71. Endoplasmic reticulum stress-induced formation of transcription factor complex ERSF including NF-Y (CBF) and activating transcription factors 6alpha and 6beta that activates the mammalian unfolded protein response
72. Glucose-regulated protein 78 (GRP78) is elevated in embryonic mouse heart and induced following hypoglycemic stress
73. The sarco/endoplasmic reticulum calcium-ATPase 2b is an endoplasmic reticulum stress-inducible protein
74. Regulation of SERCA Ca2+ pump expression by cytoplasmic Ca2+ in vascular smooth muscle cells
75. Sarco/endoplasmic reticulum calcium ATPase-2 (SERCA2) expression is regulated by ATF6 during the endoplasmic reticulum stress response: Intracellular signaling of calcium stress in a cardiac myocyte model system
76. Reactivation of peroxisome proliferator-activated receptor alpha is associated with contractile dysfunction in hypertrophied rat heart
77. Transcriptional regulation of metabolic processes: Implications for cardiac metabolism
78. Genetics of energetics: Transcriptional responses in cardiac metabolism