Bibliography
- FLEGAL KM, GRAUBARD BI, WILLIAMSON DF et al.: Excess deaths associated with underweight, overweight and obesity. JAMA (2005) 293:1861-1867.
- DALLMAN MF, STRACK AM, AKANA SF et al.: Feast and famine: critical role of glucocorticoids with insulin in daily energy flow. Front. Neuroendocrinol. (1993) 14:303-347.
- SAPOLSKY RM, ROMERO LM, MUNCK AV: How do glucocorticoids influence stress response? Integrating permissive, suppressive, stimulatory and preparative actions. Endocr. Rev. (2000) 21:55-89.
- JAMIESON PM, WALKER BR, CHAPMAN KE et al.: 11β-hydroxysteroid dehydrogenase type 1 is a predominant 11β-reductase in the intact perfused rat liver. J. Endocrinol. (2000) 165:685-692.
- ODERMATT A, ATANASOV AG, BALAZS Z et al.: Why is 11β-hydroxysteroid dehydrogenase type 1 facing the endoplasmic reticulum lumen? Physiological relevance of the membrane topology of 11β-HSD1. Mol. Cell. Endorcinol. (2006) 248:15-23.
- BANHEGYI G, BENEDETTI A, FULCERI R et al.: Cooperativity between 11β-hydroxysteroid type 1 and hexose-6-phosphate dehydrogenase in the lumen of the endoplasmic reticulum. J. Biol. Chem. (2004) 27:27017-27021.
- ATANASOV AG, NASHEV LG, SCHWEIZER RA et al.: Hexose-6-phosphate dehydrogenase determines the reaction direction of 11β-hydroxysteroid dehydrogenase type 1 as an oxoreductase. FEBS Lett. (2004) 571:129-133.
- EDWARDS CR, STEWART PM, BURT D et al.: Localisation of 11β-hydroxysteroid dehydrogenase – tissue specific protector of the mineralocorticoid receptor. Lancet (1988) 2:986-989.
- SECKL JR, WALKER BR: Minireview: 11β-hydroxysteroid dehydrogenase type 1 – a tissue-specific amplifier of glucocorticoid action. Endocrinology (2001) 142:1371-1376.
- MASUZAKI H, PATERSON J, SHINYAMA H et al.: A transgenic model of visceral obesity and the metabolic syndrome. Science (2001) 294:2166-2170.
- MASUZAKI H, YAMAMOTO H, KENYON CJ et al.: Transgenic amplificatioin of glucorticoid action in adipose tissue causes high blood pressure in mice. J. Clin. Invest. (2003) 112:83-90.
- PATERSON JM, MORTON NM, FIEVET C et al.: Metabolic syndrome without obesity: hepatic overexpression of 11β-hydroxysteroid dehydrogenase type 1 in transgenic mice. Proc. Natl. Acad. Sci. USA (2004) 101:7088-7093.
- KOTELEVTSEV Y, HOLMES MC, BURCHELL A et al.: 11β-hydroxysteroid dehydrogenase type 1 knockout mice show attenuated glucocorticoid-inducible responses and resist hyperglycemia on obesity or stress. Proc. Natl. Acad. Sci. USA (1997) 94:14924-14929.
- MORTON NM, HOLMES MC, FIEVET C et al.: Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11β-hydroxysteroid dehydrogenase type 1 mice. J. Biol. Chem. (2001) 276:41293-41300.
- WAMIL M, SECKL JR: Inhibition of 11β-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Drug Discov. Today (2007) 12:504-520.
- SWAAB DF, BAO AM, LUCASSEN PJ: The stress system in the human brain in depression and neurodegeneration. Ageing Res. Rev. (2005) 4:141-194.
- MEANEY MJ, O'DONNELL D, ROWE W et al.: Individual differences in hypothalamic–pituitary–adreanl activity in later life and hippocampal aging. Exp. Gerontol. (1995) 30:229-251.
- MOISAN MP, SECKL JR, EDWARDS CR: 11β-hydroxysteroid dehydrogenase bioactivity and messenger RNA expression in rat forebrain: localisation in hypothalamus, hippocampus, and cortex. Endocrinology (1990) 127:1450-1455.
- YAU JL, NOBLE J, KENYON CJ et al.: Lack of tissue glucocorticoid reactivation in 11β-hydroxysteroid dehydrogenase type 1 knockout mice ameriolates age-related learning impairments. Proc. Natl. Acad. Sci. USA (2001) 98:4716-4721.
- DHINGRA D, PARLE M, KULKAMI SK: Memory enhancing activity of Glycyrrhiza glabra in mice. J. Ethnopharmacol. (2004) 91:361-365.
- WANG M: Inhibitors of 11β-hydroxysteroid dehydrogenase type 1 for the treatment of metabolic syndrome. Curr. Opin. Invest. Drugs (2006) 7:319-323.
- FOTSCH C, ASKEW BC, CHEN JJ: 11β-hydroxysteroid dehydrogenase-1 as a therapeutic target for metabolic diseases. Expert Opin. Ther. Patents (2005) 15(3):289-303.
- OLSON S, ASTER SD, BROWN K et al.: Adamantyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1. Bioorg. Med. Chem. Lett. (2005) 15:4359-4362.
- HERMANOWSKI-VOSATKA A, BALKOVEC JM, CHENG K et al.: 11β-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice. J. Exp. Med. (2005) 202:517-527.
- GU X, DRAGOVIC J, KOO GC et al.: Discovery of 4-heteroarylbicyclo[2.2.2.] octyltriazoles as potent and selective inhibitors of 11β-HSD1: novel therapeutic agents for the treatment of metabolic syndrome. Bioorg. Med. Chem. Lett. (2005) 15:5266-5269.
- BERTHIAUME M, LAPLANTE M, FESTUCCIA WT et al.: 11β-HSD1 inhibition improves triglyceridemia through reduced liver VLDL secretion and partitions lipids towards oxidative tissues. Am. J. Physiol. Endocrinol. Metab. (2007) 293:E1045-E1052.
- ST JEAN DJ, YUAN C, BERCOT EA et al.: 2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11β-hydroxysteroid dehydrogenase type 1. J. Med. Chem. (2007) 5:429-432.
- VENIANT M, KOMOROWSKI R, CHEN M et al.: Effect of dosing regimen with an 11β-HSD1 inhibitor on the improvement of metabolic parameters in DIO mice Abstract 891-P: 67th Annual Meeting of Science Sess. American Diabetes Association, Chicago, USA (2007).
- FLANAGAN M: Metabolic milestones. Biocentury (2007) 15:A1-A25.
- SUTIN L, ANDERSSON S, BERQUIST L et al.: Oxazolones as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1. Bioorg. Med. Chem. Lett. (2007) 17:4837-4840.
- ROHDE JJ, PLIUSHCHEV MA, SORENSEN BK et al.: Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11β-hydroxysteroid dehydrogenase type 1 inhibitors. J. Med. Chem. (2007) 50:149-164.
- SORENSEN B, ROHDE J, WANG J et al.: Adamantane 11β-HSD1 inhibitors: application of an isocyanide multicomponent reaction. Bioorg. Med. Chem. Lett. (2006) 16:5958-5962.
- YEH VSC, PATEL JR, YONG H et al.: Synthesis and biological evaluation of heterocycle containing adamantane 11β-HSD1 inhibitors. Bioorg. Med. Chem. Lett. (2006) 16:5414-5419.
- SORENSEN B, WINN M, ROHDE J et al.: Adamantane sulfone and sulphonamide 11β-HSD1 inhibitors. Bioorg. Med. Chem. Lett. (2007) 17:527-532.
- PATEL JR, SHUAI Q, DINGES J et al.: Discovery of adamantane ethers as inhibitors of 11β-HSD1: synthesis and biological evaluation. Bioorg. Med. Chem. Lett. (2007) 17:750-755.
- SAHNI-ARYA B, FLYNN MJ, BERGERON L et al.: Cofactor-specific modulation of 11β-hydroxysteroid dehydrogenase 1 inhibitor potency. Biochim. Biophys. Acta (2007) 1774:1184-1191.
- ZHUO J, XU M, ZHANG C et al.: Discovery and synthesis of nipecotic amides as novel, potent and selective 11β-HSD1 inhibitors. 234th ACS National Meeting, Boston, USA (2007).
- WEBSTER SP, WARD P, BINNIE M et al.: Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors. Bioorg. Med. Chem. Lett. (2007) 17:2838-2843.
- LINDERS JT: Substituted adamantanamides as novel inhibitors of 11β-hydroxysteroid dehydrogenase type 1. 231st ACS National Meeting, Atlanta, USA (2006).
- BARF T, VALLGARDA J, EMOND R et al.: Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1. J. Med. Chem. (2002) 45:3813-3815.
- HOSFIELD DJ, WU Y, SKENE RJ et al.: Conformational flexibility in crystal structures of human 11β-HSD1 provide insights into glucocorticoid interconversion and enzyme regulation. J. Biol. Chem. (2005) 280:4639-4648.
- ZHANG J, OSSLUND TD, PLANT MH et al.: Crystal structure of murine 11β-hydroxysteroid dehydrogenase 1: an important therapeutic target for diabetes. Biochemistry (2005) 44:6948-6957.
- KIM KW, WANG Z, BUSBY J et al.: The role of tyrosine 177 in human 11β-hydroxysteroid dehydrogenase type 1 in substrate and inhibitor binding: an unlikely hydrogen bond donor for the substrate. Biochim. Biophys. Acta (2006) 1764:824-830.
- SANDEEP TC, YAU JL, MACLULLICH AM et al.: 11β-hydroxysteroid dehydrogenase inhibition improves cognitive function in healthy elderly men and type 2 diabetics. Proc. Natl. Acad. Sci. USA (2004) 101:6734-6739.
- ROCHA BA: 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibiton prolonged memory retention in mice. 231st ACS National Meeting, Atlanta, USA (2006).
Patents
- MERCK & CO., INC.: WO2004058741 (2004).
- MERCK & CO., INC.: WO2007047625 (2007).
- MERCK & CO., INC.: WO2005097759 (2005).
- MOCHIDA PHARMACEUTICAL CO. LTD: WO2006068199 (2006).
- MOCHIDA PHARMACEUTICAL CO. LTD: WO2006080533 (2006).
- MOCHIDA PHARMACEUTICAL CO. LTD: WO2007007688 (2007).
- ASTELLAS PHARMA, INC.: WO2006030805 (2006).
- ASTELLAS PHARMA, INC.: EP1790641 (2007).
- BRISTOL-MYERS SQUIBB CO.: WO2006135667 (2006).
- BRISTOL-MYERS SQUIBB CO.: WO2006135795 (2006).
- UNIV. EDINBURGH: WO2007029021 (2007).
- F HOFFMANN-LA ROCHE AG: WO2007025880 (2007).
- F HOFFMANN-LA ROCHE AG: WO2007025892 (2007).
- AMGEN, INC. & BIOVITRUM AG: WO2005116002 (2005).
- MERCK & CO., INC.: WO2005016877 (2005).
- AMGEN SF, LLC: WO2005095350 (2005).
- ABBOTT LABORATORIES: WO2005108368 (2005).
- ABBOTT LABORATORIES: WO2006074330 (2006).
- PFIZER, INC.: WO2006048750 (2006).
- PFIZER, INC.: WO2005108359 (2005).
- ABBOTT LABORATORIES: WO2006074244 (2006).
- JANSSEN PHARMACEUTICA NV: WO2006024627 (2006).
- INCYTE CORP.: WO2006002361 (2006).
- INCYTE CORP.: WO2006002350 (2006).
- INCYTE CORP.: WO2006002349 (2006).
- INCYTE CORP.: WO2005110992 (2005).
- NOVO NORDISK A/S: WO2007051810 (2007).
- ONO PHARMACEUTICAL CO. LTD: WO2005035534 (2005).
- NOVO NORDISK A/S: WO2006040329 (2006).
- INCYTE CORP.: WO2006055752 (2006).
- NOVO NORDISK A/S: WO2007051811 (2007).
- BRISTOL-MYERS SQUIBB CO.: WO2006113261 (2006).
- ASTRAZENECA AB: WO2005047250 (2005).
- SHIONOGI & CO. LTD: WO2006132197 (2006).
- INCYTE CORP.: WO2006020598 (2006).
- F HOFFMANN-LA ROCHE AG: WO2006094633 (2006).
- MERCK & CO., INC.: WO2006017542 (2006).
- STERIX LTD: WO2006100502 (2006).
- JANSSEN PHARMACEUTICA NV: WO2006024628 (2006).
- INCYTE CORP.: WO2006053024 (2006).
- ELI LILLY & CO.: WO2006049952 (2006).
- ELI LILLY & CO.: WO2006068991 (2006).
- ELI LILLY & CO.: WO2006068992 (2006).
- TAKEDA PHARMACEUTICAL CO. LTD: WO2006104280 (2006).
- JANSSEN PHARMACEUTICA NV: WO2005108360 (2005).
- JANSSEN PHARMACEUTICA NV: WO2005108361 (2005).
- PFIZER, INC.: WO2005060963 (2005).
- PFIZER, INC.: WO2006134467 (2006).
- PFIZER, INC.: WO2006106423 (2006).
- F HOFFMANN-LA ROCHE AG: WO2006010546 (2006).
- EVOTEC AG: WO2006048331 (2006).
- EVOTEC AG: WO2006050908 (2006).
- F HOFFMANN-LA ROCHE AG: WO2006000371 (2006).
- TAISHO PHARMACEUTICAL CO. LTD: WO2005097764 (2005).
- TAISHO PHARMACEUTICAL CO. LTD: WO2006051662 (2006).
- TAKEDA SAN DIEGO, INC.: WO2006066109 (2006).
- PFIZER, INC.: WO2006134481 (2006).
- F HOFFMANN-LA ROCHE AG: WO2006034804 (2006).
- STERIX LTD: WO2005103023 (2005).
- STERIX LTD: WO2005042513 (2005).
- EVOTEC AG: WO2006048330 (2006).
Website
- http://incyte.com/index.html Press Release, Incyte website.