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Items: 11

1.

Targeting KRAS-dependent tumors with AZD4785, a high-affinity therapeutic antisense oligonucleotide inhibitor of KRAS.

Ross SJ, Revenko AS, Hanson LL, Ellston R, Staniszewska A, Whalley N, Pandey SK, Revill M, Rooney C, Buckett LK, Klein SK, Hudson K, Monia BP, Zinda M, Blakey DC, Lyne PD, Macleod AR.

Sci Transl Med. 2017 Jun 14;9(394). pii: eaal5253. doi: 10.1126/scitranslmed.aal5253. Erratum in: Sci Transl Med. 2017 Jul 26;9(400):.

PMID:
28615361
2.

Identification and design of a novel series of MGAT2 inhibitors.

Barlind JG, Buckett LK, Crosby SG, Davidsson Ö, Emtenäs H, Ertan A, Jurva U, Lemurell M, Gutierrez PM, Nilsson K, O'Mahony G, Petersson AU, Redzic A, Wågberg F, Yuan ZQ.

Bioorg Med Chem Lett. 2013 May 1;23(9):2721-6. doi: 10.1016/j.bmcl.2013.02.084. Epub 2013 Feb 27.

PMID:
23541669
3.

Diacylglycerol acyltransferase-1 inhibition enhances intestinal fatty acid oxidation and reduces energy intake in rats.

Schober G, Arnold M, Birtles S, Buckett LK, Pacheco-López G, Turnbull AV, Langhans W, Mansouri A.

J Lipid Res. 2013 May;54(5):1369-84. doi: 10.1194/jlr.M035154. Epub 2013 Feb 28.

4.

ACAT-selective and nonselective DGAT1 inhibition: adrenocortical effects--a cross-species comparison.

Floettmann JE, Buckett LK, Turnbull AV, Smith T, Hallberg C, Birch A, Lees D, Jones HB.

Toxicol Pathol. 2013;41(7):941-50. doi: 10.1177/0192623313477753. Epub 2013 Feb 20.

PMID:
23427273
5.

Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).

Barlind JG, Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD, Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD, Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson AU, Redzic A, Turnbull AV, Vinblad J.

J Med Chem. 2012 Dec 13;55(23):10610-29. doi: 10.1021/jm301296t. Epub 2012 Nov 21.

PMID:
23116186
6.

Intestinal DGAT1 deficiency reduces postprandial triglyceride and retinyl ester excursions by inhibiting chylomicron secretion and delaying gastric emptying.

Ables GP, Yang KJ, Vogel S, Hernandez-Ono A, Yu S, Yuen JJ, Birtles S, Buckett LK, Turnbull AV, Goldberg IJ, Blaner WS, Huang LS, Ginsberg HN.

J Lipid Res. 2012 Nov;53(11):2364-79. doi: 10.1194/jlr.M029041. Epub 2012 Aug 21.

7.

Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.

McCoull W, Addie MS, Birch AM, Birtles S, Buckett LK, Butlin RJ, Bowker SS, Boyd S, Chapman S, Davies RD, Donald CS, Green CP, Jenner C, Kemmitt PD, Leach AG, Moody GC, Gutierrez PM, Newcombe NJ, Nowak T, Packer MJ, Plowright AT, Revill J, Schofield P, Sheldon C, Stokes S, Turnbull AV, Wang SJ, Whalley DP, Wood JM.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):3873-8. doi: 10.1016/j.bmcl.2012.04.117. Epub 2012 May 2.

PMID:
22608962
8.

DGAT1 deficiency decreases PPAR expression and does not lead to lipotoxicity in cardiac and skeletal muscle.

Liu L, Yu S, Khan RS, Ables GP, Bharadwaj KG, Hu Y, Huggins LA, Eriksson JW, Buckett LK, Turnbull AV, Ginsberg HN, Blaner WS, Huang LS, Goldberg IJ.

J Lipid Res. 2011 Apr;52(4):732-44. doi: 10.1194/jlr.M011395. Epub 2011 Jan 3.

9.

DGAT1 inhibitors as anti-obesity and anti-diabetic agents.

Birch AM, Buckett LK, Turnbull AV.

Curr Opin Drug Discov Devel. 2010 Jul;13(4):489-96. Review.

PMID:
20597032
10.

Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor.

Birch AM, Birtles S, Buckett LK, Kemmitt PD, Smith GJ, Smith TJ, Turnbull AV, Wang SJ.

J Med Chem. 2009 Mar 26;52(6):1558-68. doi: 10.1021/jm801507v.

PMID:
19256504
11.

Diacylglycerol acyltransferases: Potential roles as pharmacological targets.

Zammit VA, Buckett LK, Turnbull AV, Wure H, Proven A.

Pharmacol Ther. 2008 Jun;118(3):295-302. doi: 10.1016/j.pharmthera.2008.03.010. Epub 2008 Apr 11. Review.

PMID:
18508126

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