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Isozyme-nonselective N-substituted bipiperidylcarboxamide acetyl-CoA carboxylase inhibitors reduce tissue malonyl-CoA concentrations, inhibit fatty acid synthesis, and increase fatty acid oxidation in cultured cells and in experimental animals.

Harwood HJ Jr, Petras SF, Shelly LD, Zaccaro LM, Perry DA, Makowski MR, Hargrove DM, Martin KA, Tracey WR, Chapman JG, Magee WP, Dalvie DK, Soliman VF, Martin WH, Mularski CJ, Eisenbeis SA.

J Biol Chem. 2003 Sep 26;278(39):37099-111. Epub 2003 Jul 3.


Acetyl-CoA carboxylase inhibition for the treatment of metabolic syndrome.

Harwood HJ Jr.

Curr Opin Investig Drugs. 2004 Mar;5(3):283-9. Review.


Malonyl-CoA content and fatty acid oxidation in rat muscle and liver in vivo.

Chien D, Dean D, Saha AK, Flatt JP, Ruderman NB.

Am J Physiol Endocrinol Metab. 2000 Aug;279(2):E259-65.


Treating the metabolic syndrome: acetyl-CoA carboxylase inhibition.

Harwood HJ Jr.

Expert Opin Ther Targets. 2005 Apr;9(2):267-81. Review.


Continuous fatty acid oxidation and reduced fat storage in mice lacking acetyl-CoA carboxylase 2.

Abu-Elheiga L, Matzuk MM, Abo-Hashema KA, Wakil SJ.

Science. 2001 Mar 30;291(5513):2613-6.


LKB1 and the regulation of malonyl-CoA and fatty acid oxidation in muscle.

Thomson DM, Brown JD, Fillmore N, Condon BM, Kim HJ, Barrow JR, Winder WW.

Am J Physiol Endocrinol Metab. 2007 Dec;293(6):E1572-9. Epub 2007 Oct 9.


Acetyl-CoA carboxylase regulation of fatty acid oxidation in the heart.

Saddik M, Gamble J, Witters LA, Lopaschuk GD.

J Biol Chem. 1993 Dec 5;268(34):25836-45.


Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.

Gu YG, Weitzberg M, Clark RF, Xu X, Li Q, Zhang T, Hansen TM, Liu G, Xin Z, Wang X, Wang R, McNally T, Zinker BA, Frevert EU, Camp HS, Beutel BA, Sham HL.

J Med Chem. 2006 Jun 29;49(13):3770-3. Erratum in: J Med Chem. 2006 Aug 10;49(16):5028. Zinker, Bradley A [added]; Frevert, Ernst U [added]; Camp, Heidi [corrected to Camp, Heidi S].


Hepatic de novo lipogenesis is present in liver-specific ACC1-deficient mice.

Harada N, Oda Z, Hara Y, Fujinami K, Okawa M, Ohbuchi K, Yonemoto M, Ikeda Y, Ohwaki K, Aragane K, Tamai Y, Kusunoki J.

Mol Cell Biol. 2007 Mar;27(5):1881-8. Epub 2007 Jan 8. Erratum in: Mol Cell Biol. 2007 May;27(9):3556.


Acetyl-CoA carboxylase involvement in the rapid maturation of fatty acid oxidation in the newborn rabbit heart.

Lopaschuk GD, Witters LA, Itoi T, Barr R, Barr A.

J Biol Chem. 1994 Oct 14;269(41):25871-8.


Malonyl-CoA and the regulation of fatty acid oxidation in soleus muscle.

Alam N, Saggerson ED.

Biochem J. 1998 Aug 15;334 ( Pt 1):233-41.


MEDICA 16 inhibits hepatic acetyl-CoA carboxylase and reduces plasma triacylglycerol levels in insulin-resistant JCR: LA-cp rats.

Atkinson LL, Kelly SE, Russell JC, Bar-Tana J, Lopaschuk GD.

Diabetes. 2002 May;51(5):1548-55.


Fatty acid synthase inhibition in human breast cancer cells leads to malonyl-CoA-induced inhibition of fatty acid oxidation and cytotoxicity.

Thupari JN, Pinn ML, Kuhajda FP.

Biochem Biophys Res Commun. 2001 Jul 13;285(2):217-23. Erratum in: Biochem Biophys Res Commun 2002 Jul 12;295(2):570.


Gene expression analysis in rats treated with experimental acetyl-coenzyme A carboxylase inhibitors suggests interactions with the peroxisome proliferator-activated receptor alpha pathway.

Waring JF, Yang Y, Healan-Greenberg CH, Adler AL, Dickinson R, McNally T, Wang X, Weitzberg M, Xu X, Lisowski A, Warder SE, Gu YG, Zinker BA, Blomme EA, Camp HS.

J Pharmacol Exp Ther. 2008 Feb;324(2):507-16. Epub 2007 Nov 19.


Expression, purification, and characterization of human and rat acetyl coenzyme A carboxylase (ACC) isozymes.

Cheng D, Chu CH, Chen L, Feder JN, Mintier GA, Wu Y, Cook JW, Harpel MR, Locke GA, An Y, Tamura JK.

Protein Expr Purif. 2007 Jan;51(1):11-21. Epub 2006 Jun 10.


Evidence for an anaplerotic/malonyl-CoA pathway in pancreatic beta-cell nutrient signaling.

Brun T, Roche E, Assimacopoulos-Jeannet F, Corkey BE, Kim KH, Prentki M.

Diabetes. 1996 Feb;45(2):190-8.


Effects of 5-iodotubercidin on hepatic fatty acid metabolism mediated by the inhibition of acetyl-CoA carboxylase.

García-Villafranca J, Castro J.

Biochem Pharmacol. 2002 Jun 1;63(11):1997-2000.


Metabolic response to an acute jump in cardiac workload: effects on malonyl-CoA, mechanical efficiency, and fatty acid oxidation.

Zhou L, Huang H, Yuan CL, Keung W, Lopaschuk GD, Stanley WC.

Am J Physiol Heart Circ Physiol. 2008 Feb;294(2):H954-60. Epub 2007 Dec 14.


Fatty acid oxidation and the regulation of malonyl-CoA in human muscle.

Båvenholm PN, Pigon J, Saha AK, Ruderman NB, Efendic S.

Diabetes. 2000 Jul;49(7):1078-83.


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