De Schoolmeester J - Search Results

1

An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia.

Poucher SM, Freeman S, Loxham SJ, Convey G, Bartlett JB, De Schoolmeester J, Teague J, Walker M, Turnbull AV, Charles AD, Carey F, Berg S. Poucher SM, et al. Among authors: de schoolmeester j. Br J Pharmacol. 2007 Dec;152(8):1239-47. doi: 10.1038/sj.bjp.0707502. Epub 2007 Oct 15. Br J Pharmacol. 2007. PMID: 17934512 Free PMC article.

2

Glucagon challenge in the rat: a robust method for the in vivo assessment of Glycogen phosphorlyase inhibitor efficacy.

Loxham SJ, Teague J, Poucher SM, De Schoolmeester J, Turnbull AV, Carey F. Loxham SJ, et al. Among authors: de schoolmeester j. J Pharmacol Toxicol Methods. 2007 Jan-Feb;55(1):71-7. doi: 10.1016/j.vascn.2006.03.005. Epub 2006 Mar 27. J Pharmacol Toxicol Methods. 2007. PMID: 16713718

3

Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.

Goldberg FW, Dossetter AG, Scott JS, Robb GR, Boyd S, Groombridge SD, Kemmitt PD, Sjögren T, Gutierrez PM, deSchoolmeester J, Swales JG, Turnbull AV, Wild MJ. Goldberg FW, et al. J Med Chem. 2014 Feb 13;57(3):970-86. doi: 10.1021/jm4016729. Epub 2014 Jan 27. J Med Chem. 2014. PMID: 24422550

4

Continuous inhibition of 11β-hydroxysteroid dehydrogenase type I in adipose tissue leads to tachyphylaxis in humans and rats but not in mice.

Morentin Gutierrez P, Gyte A, deSchoolmeester J, Ceuppens P, Swales J, Stacey C, Eriksson JW, Sjöstrand M, Nilsson C, Leighton B. Morentin Gutierrez P, et al. Br J Pharmacol. 2015 Oct;172(20):4806-16. doi: 10.1111/bph.13251. Epub 2015 Oct 8. Br J Pharmacol. 2015. PMID: 26218540 Free PMC article. Clinical Trial.

5

Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 reduces food intake and weight gain but maintains energy expenditure in diet-induced obese mice.

Wang SJ, Birtles S, de Schoolmeester J, Swales J, Moody G, Hislop D, O'Dowd J, Smith DM, Turnbull AV, Arch JR. Wang SJ, et al. Among authors: de schoolmeester j. Diabetologia. 2006 Jun;49(6):1333-7. doi: 10.1007/s00125-006-0239-y. Epub 2006 Apr 13. Diabetologia. 2006. PMID: 16612591

6

11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors still improve metabolic phenotype in male 11β-HSD1 knockout mice suggesting off-target mechanisms.

Harno E, Cottrell EC, Yu A, DeSchoolmeester J, Gutierrez PM, Denn M, Swales JG, Goldberg FW, Bohlooly-Y M, Andersén H, Wild MJ, Turnbull AV, Leighton B, White A. Harno E, et al. Endocrinology. 2013 Dec;154(12):4580-93. doi: 10.1210/en.2013-1613. Epub 2013 Oct 29. Endocrinology. 2013. PMID: 24169553 Free PMC article.

7

11-Dehydrocorticosterone causes metabolic syndrome, which is prevented when 11β-HSD1 is knocked out in livers of male mice.

Harno E, Cottrell EC, Keevil BG, DeSchoolmeester J, Bohlooly-Y M, Andersén H, Turnbull AV, Leighton B, White A. Harno E, et al. Endocrinology. 2013 Oct;154(10):3599-609. doi: 10.1210/en.2013-1362. Epub 2013 Jul 5. Endocrinology. 2013. PMID: 23832962

8

Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).

Scott JS, Bowker SS, Deschoolmeester J, Gerhardt S, Hargreaves D, Kilgour E, Lloyd A, Mayers RM, McCoull W, Newcombe NJ, Ogg D, Packer MJ, Rees A, Revill J, Schofield P, Selmi N, Swales JG, Whittamore PR. Scott JS, et al. J Med Chem. 2012 Jun 28;55(12):5951-64. doi: 10.1021/jm300592r. Epub 2012 Jun 19. J Med Chem. 2012. PMID: 22691057

9

Novel acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329).

Scott JS, deSchoolmeester J, Kilgour E, Mayers RM, Packer MJ, Hargreaves D, Gerhardt S, Ogg DJ, Rees A, Selmi N, Stocker A, Swales JG, Whittamore PR. Scott JS, et al. J Med Chem. 2012 Nov 26;55(22):10136-47. doi: 10.1021/jm301252n. Epub 2012 Nov 7. J Med Chem. 2012. PMID: 23088558

10

Differences between men and women in the regulation of adipose 11β-HSD1 and in its association with adiposity and insulin resistance.

DeSchoolmeester J, Palming J, Persson T, Pereira MJ, Wallerstedt E, Brown H, Gill D, Renström F, Lundgren M, Svensson MK, Rees A, Eriksson JW. DeSchoolmeester J, et al. Diabetes Obes Metab. 2013 Nov;15(11):1056-60. doi: 10.1111/dom.12137. Epub 2013 Jun 20. Diabetes Obes Metab. 2013. PMID: 23701286

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