119
Views
60
CrossRef citations to date
0
Altmetric
Review

New and improved glucocorticoid receptor ligands

, &
Pages 1527-1545 | Published online: 25 Nov 2005

Bibliography

  • KIRWAN JR, BALINT G, SZEBENYI B:Anniversary: 50 years of glucocorticoid treatment in rheumatoid arthritis. Rheumatology (1999) 38:100–102.
  • NEECK G: Fifty years of experience with cortisone therapy in the study and treatment of rheumatoid arthritis. Ann. NY Acad. Sci. (2002) 966:28–38.
  • JOELS M, VREUGDENHIL E: Corticosteroids in the brain. Cellular and molecular actions. MoL NeurobioL (1998) 17:87–108.
  • BODINE PV LITWACK G: The glucocorticoid receptor and its endogenous regulators. Receptor (1990) 1:83–119.
  • McEWEN BS, COIRINI H, SCHUMACHER M: Steroid effects on neuronal activity: when is the genome involved? Ciba Found Symp. (1990) 153:3-12 (Discussion 12–21).
  • WANG W, XING BR, CHEN YZ: [Fast modulation of glutamate and GABA receptor-mediate electrophysiological responses by glucocorticoid]. Sheng Li Hsueh Pao (1996) 48:551–556.
  • LU NZ, CIDLOWSKI JA: The origin and functions of multiple human glucocorticoid receptor isoforms. Ann. NY Acad. Sci. (2004) 1024:102–123.
  • GALIGNIANA MD, SCRUGGS JL, HERRINGTON J et al.: Heat shock protein 90-dependent (geldanamycin-inhibited) movement of the glucocorticoid receptor through the cytoplasm to the nucleus requires intact cytoskeleton. MoL EndocrinoL (1998) 12: 1903-1913.
  • JENKINS BD, PULLEN CB, BD: Novel glucocorticoid receptor coactivator effector mechanisms. Trends EndocrinoL Metab. (2001) 12:122–126.
  • BOUMPAS DT, CHROUSOS GP, WILDER RL, CUPPS TR, BALOW JE: Glucocorticoid therapy for immune-mediated diseases: basic and clinical correlates. Ann. Intern. Med. (1993) 119:1198–1208.
  • ORTH DN, KOVACS WJ: The adrenal cortex. In: Series the adrenal cortex. Wilson JD, Foster DW, Kronenberg HM, Larsen PR (Eds), W. B. Saunders Company, Philadelphia, USA (1998):517.
  • HEUCK C, HEICKENDORFF L, WOLTHERS OD: A randomised controlled trial of short term growth and collagen turnover in asthmatics treated with inhaled formoterol and budesonide. Arch. Dis. Child. (2000) 83:334–339.
  • DEEG HJ, HENSLEE-DOWNEY PJ: Management of acute graft-versus-host disease. Bone Marrow Transplant (1990) 6:1–8.
  • AXELROD L: Side effects of glucocorticoid therapy. In: Series side effects of glucocorticoid therapy. Schleimer RP, Claman HN, Oronsky AL (Eds), Academic Press, Inc., San Diego, USA (1989):377–408.
  • TBCDS: Acute adverse reactions to prednisone in relation to dosage.. PharmacoL Ther. (1972) 13:694–698.
  • BITRAN D, SHIEKH M, DOWD JA, DUGAN MM, RENDA P: Corticosterone is permissive to the anxiolytic effect that results from the blockade of hippocampal mineralocorticoid receptors. Biochem. Behav. (1998) 60:879–887.
  • TAPPY L, RANDIN D, P et al.: Mechanisms of dexamethasone-induced insulin resistance in healthy humans. J. Clin. Metab. (1994) 79:1063–1069.
  • LAAKSO M, EDELMAN SV, JM, BRECHTEL G, WALLACE P, BARON AD: Kinetics of in vivo muscle insulin-mediated glucose uptake in human obesity. Diabetes (1990) 39:965–974.
  • GRANNER DK, SASAKI K, CHU D: Multihormonal regulation of phosphoenolpyruvate carboxykinase gene transcription. The dominant role of insulin. Ann. IVY Acad. Sci. (1986) 478:175–190.
  • CONN HO, POYNARD T: Corticosteroids and peptic ulcer: meta-analysis of adverse events during steroid therapy. J. Intern. Med. (1994) 236:619–632.
  • BRINDLEY DN, MCCANN BS, NIAURA R, STONEY CM, SUAREZ EC: Stress and lipoprotein metabolism: modulators and mechanisms. Metabolism (1993) 42:3–15.
  • BREM AS: Insights into glucocorticoid-associated hypertension. Am. J. Kidney Dis. (2001) 37:1–10.
  • GONZALEZ-CADAVID NF, BHASIN S: Role of myostatin in metabolism.. Opin. Clin. Nutr. Metab. Care (2004) 7:451–457.
  • ••Useful review of muscle regulators andphysiology.
  • DIETHELM AG: Surgical management of complications of steroid therapy. Ann. Surg. (1977) 185:251–263.
  • ANSTEAD GM: Steroids, retinoids, and wound healing. Adv. Wound Care (1998) 11:277–285.
  • AUTIO P, OIKARINEN A. MELKKO J, RISTELI J, RISTELI L: Systemic glucocorticoids decrease the synthesis of type I and type III collagen in human skin in vivo, whereas isotretinoin treatment has little effect. Br. J. DermatoL (1994) 131:660–663.
  • BRAUCHLE M, FASSLER R, S: Suppression of keratinocyte growth factor expression by glucocorticoids in vitro and during wound healing. J. Invest. DermatoL (1995) 105:579–584.
  • LUKERT BP, KREAM BE: Clinical and basic aspects of glucocorticoid action in bone. In: Series clinical and basic aspects of action in bone. AcademicPress, Inc., Philadelphia, USA (1996).
  • RALSTON SH: Pathogenesis and management of corticosteroid-induced osteoporosis. Curr. Opin. Onc. Endo. Metab. Invest. Drugs (1999) 1:25–30.
  • ••Key discussion of the issues surroundingthe bone-related impact of steroids.
  • VAN STAA TP, LEUFKENS HG, ABENHAIM L, ZHANG B, COOPER C: Oral corticosteroids and fracture risk: relationship to daily and cumulative doses. Rheumatology (2000) 39:1383–1389.
  • PATSCHAN D, LODDENKEMPER K, BUTTGEREIT F: Molecular mechanisms of glucocorticoid-induced osteoporosis. Bone (2001) 29:498–505.
  • DEMPSTER DW: Bone in glucocorticoid-induced osteoporosis. J. Bone Miner. Res. (1989) 4:137–141.
  • CENTRELLA M, ROSEN V, WOZNEY JM, CASINGHINO SR, McCARTHY TL: Opposing effects by glucocorticoid and bone morphogenetic protein-2 in fetal rat bone cell cultures. J. Cell. Biochem. (1997) 67:528–540.
  • CHANG DJ, JI C, KIM KK, CASINGHINO S, McCARTHY TL, CENTRELLA M: Reduction in transforming growth factor 13 receptor I expression and transcription factor CBFal on bone cells by glucocorticoid.. Chem. (1998) 273:4892–4896.
  • SHI XM, BLAIR HC, YANG X, McDONALD JM, GAO X: Tandem repeat of C/EBP binding sites mediates PPARy2 gene transcription in glucocorticoid-induced adipocyte differentiation. J. Cell. Biochem. (2000) 76:518–527.
  • McCULLOCH CA, TENENBAUM HC: Dexamethasone induces proliferation and terminal differentiation of osteogenic cells in tissue culture. Anat. Rec. (1986) 215:397–402.
  • GRONOWICZ GA, DEROME ME: Synthetic peptide containing Arg-Gly-Asp inhibits bone formation and resorption in a mineralizing organ culture system of fetal rat parietal bones. J. Bone Miner. Res. (1994) 9:193–201.
  • GOHEL AR, HAND AR, GA: Immunogold localization of 01-integrin in bone: effect of glucocorticoids and insulin-like growth factor I on integrins and osteocyte. J. Histochem. Cytochem. (1995) 43:1085–1096.
  • DEFRANCO DJ, LIAN JB, J: Differential effects of glucocorticoid on recruitment and activity of osteoclasts induced by normal and osteocalcin-deficient bone implanted in rats. Endocrinology (1992)131:114–121.
  • HOFBAUER LC, KHOSLA S, CR, LACEY DL, BOYLE WJ, RIGGS BL: The roles of osteoprotegerin and osteoprotegerin ligand in the paracrine regulation of bone resorption. J. Bone Miner. Res. (2000) 15:2–12.
  • SASAKI N, KUSANO E, ANDO Y, YANO K, TSUDA E, ASANO Y: Glucocorticoid decreases circulating osteoprotegerin (OPG): possible mechanism for glucocorticoid induced osteoporosis. Nephrol. Dial. Transplant. (2001) 16:479–482.
  • MORRISON NA, SHINE J, FRAGONAS JC, VERKEST V, McMENEMY ML, EISMAN JA: 1,25-dihydroxyvitamin D-responsive element and glucocorticoid repression in the osteocalcin gene. Science (1989) 246:1158–1161.
  • DELANY AM, GABBITAS BY, CANALIS E: Cortisol downregulates osteoblast al (I) procollagen mRNA by transcriptional and posttranscriptional mechanisms. J. Cell. Biochem. (1995) 57:488–494.
  • SUBRAMANIAM M, COLVARD D, KEETING PE, RASMUSSEN K, RIGGS BL, SPELSBERG TC: Glucocorticoid regulation of alkaline phosphatase, osteocalcin, and proto-oncogenes in normal human osteoblast-like cells. J. Cell. Biochem. (1992) 50:411–424.
  • GRONOWICZ GA, DEROME ME, McCARTHY MB: Glucocorticoids inhibit fibronectin synthesis and messenger ribonucleic acid levels in cultured fetal rat parietal bones. Endocrinology (1991) 128:1107–1114.
  • DOHERTY WJ, DEROME ME, McCARTHY MB, GRONOWICZ GA: The effect of glucocorticoids on osteoblast function. The effect of corticosterone on osteoblast expression of131 integrins. J. Bone Joint Surg Am. (1995) 77:396–404.
  • ABBADIA Z, AMIRAL J, MC, DELMAS PD, CLEZARDIN P: The growth-supportive effect of thrombospondin (TSP1) and the of TSP1 by human MG-63 osteoblastic cells are both inhibited by dexamethasone. FEBS Lett. (1993) 335:161–166.
  • WEINSTEIN RS, MANOLAGAS SC: Apoptosis and osteoporosis. Am. J. Med. (2000) 108:153–164.
  • REID IR, VEALE AG, FRANCE JT: Glucocorticoid osteoporosis. J. Asthma (1994) 31:7–18.
  • MARTENS HF, SHEETS PK, TENOVER JS, DUGOWSON CE, BREMNER WJ, STARKEBAUM G: Decreased testosterone levels in men with rheumatoid arthritis: effect of low dose prednisone therapy. J. RheumatoL (1994) 21:1427–1431.
  • WIMALAWANSA SJ: Prevention and treatment of osteoporosis: efficacy of combination of hormone replacement therapy with other antiresorptive agents.. Densitom. (2000) 3:187–201.
  • HAHN TJ, HALSTEAD LR, BARAN DT: Effects off short term glucocorticoid administration on intestinal calcium absorption and circulating vitamin D metabolite concentrations in man. J. Clin. Endocrinol. Metab. (1981) 52:111–115.
  • AARDEN EM, BURGER EH, NUWEIDE PJ: Function of osteocytes in bone. J. Cell. Biochem. (1994) 55:287–299.
  • ZAMAN G, PITSILLIDES AA, SC et al.: Mechanical strain stimulates nitric oxide production by rapid activation of endothelial nitric oxide synthase in osteocytes. J. Bone Miner. Res. (1999) 14:1123–1131.
  • CHANG CC, GREENSPAN A, GERSHWIN ME: Osteonecrosis: current perspectives on pathogenesis and treatment. Semin. Arthritis Rheum. (1993) 23:47–69.
  • CHERNETSKY SG, MONT Mk LAPORTE DM, JONES LC, HUNGERFORD DS, McCARTHY EF: Pathologic features in steroid and nonsteroid associated osteonecrosis. Clin. Orthop. (1999):149–161.
  • MANKIN HJ: Nontraumatic necrosis of bone (osteonecrosis). N Engl. J. Med. (1992) 326:1473–1479.
  • WARMAN M, BOSKEY AL: Effect of high levels of corticosteroids on the lipids of the long bones of the mature rabbit.. Bone Dis. Relat. Res. (1983) 4:319–324.
  • WEINSTEIN RS, NICHOLAS RW, MANOLAGAS SC: Apoptosis of osteocytes in glucocorticoid-induced osteonecrosis of the hip. J. Clin. EndocrinoL Metab. (2000) 85:2907–2912.
  • EBERHARDT AW, YEAGER-JONES A, BLAIR HC: Regional trabecular bone matrix degeneration and osteocyte death in femora of glucocorticoid- treated rabbits. Endocrinology (2001) 142:1333–1340.
  • ISHIDA Y, HEERSCHE JN:-induced osteoporosis: both in vivo and in vitro concentrations of glucocorticoids higher than physiological levels attenuate osteoblast differentiation. J. Bone Miner. Res. (1998) 13:1822–1826.
  • WEINSTEIN RS, JILKA RL, AM, MANOLAGAS SC: Inhibition of osteoblastogenesis and promotion of apoptosis of osteoblasts and osteocytes by glucocorticoids. Potential mechanisms of their deleterious effects on bone. J. Clin. Invest. (1998) 102:274–282.
  • KIM CH, CHENG SL, KIM GS: Effects of dexamethasone on proliferation, activity, and cytokine secretion of normal human bone marrow stromal cells: possible mechanisms of glucocorticoid-induced bone loss. J. EndocrinoL (1999) 162:371–379.
  • MINER JN, YAMAMOTO KR: Regulatory crosstalk at composite response elements. Trends Biochem. Sci. (1991) 16:423–426.
  • DIAMOND MI, MINER JN, YOSHINAGA SK, YAMAMOTO KR: Transcription factor interactions: selectors of positive or negative regulation from a single DNA element. Science (1990) 249:1266–1272.
  • MINER JN, YAMAMOTO KR: The basic region of AP-1 specifies glucocorticoid receptor activity at a composite response element. Genes Dev. (1992) 6:2491–2501.
  • MINER JN, DIAMOND MI, KR: Joints in the regulatory lattice: composite regulation by steroid receptor-AP1 complexes. Cell Growth Differ. (1991) 2:525–530.
  • McKAY LI, CIDLOWSKI JA: Cross-talk between nuclear factor-KB and the steroid hormone receptors: mechanisms of mutual antagonism. MoL EndocrinoL (1998) 12:45–56.
  • BARNES PJ, ADCOCK IM: How do corticosteroids work in asthma?. Intern. Med. (2003) 139:359–370.
  • JIN JY, ALMON RR, DUBOIS DC, JUSKO WJ: Modeling of corticosteroid pharmacogenomics in rat liver using gene microarrays. J. PharmacoL Exp. Ther. (2003) 307:93–109.
  • ALLAN GF, TSAI SY, O'MALLEY BW, TSAI MJ: Steroid hormone receptors and in vitro transcription. Bioessays (1991) 13:73–78.
  • HONG H, DARIMONT BD, MA H, YANG L, YAMAMOTO KR, STALLCUP MR: An additional region of coactivator GRIP1 required for interaction with the hormone-binding domains of a subset of nuclear receptors. J. Biol. Chem. (1999) 274:3496–3502.
  • SMITH CL, ONATE SA, TSAI MJ, O'MALLEY BW: CREB binding protein acts synergistically with steroid receptor coactivator-1 to enhance steroid receptor-dependent transcription. Proc. NatL Acad. Sci. USA (1996) 93:8884–8888.
  • DARIMONT BD, WAGNER RL, APRILETTI JW et al.: Structure and specificity of nuclear receptor-coactivator interactions. Genes Dev. (1998) 12:3343–3356.
  • LIU J, DEFRANCO DB: Chromatin recycling of glucocorticoid receptors: implications for multiple roles of heat shock protein 90. Mol. Endocrinol. (1999) 13:355–365.
  • PHILLIPS SJ: Physiology of wound healingand surgical wound care. Asaio. J. (2000) 46:S2–S5.
  • MOEHREN U, ECKEY M, BANIAHMAD A: Gene repression by nuclear hormone receptors. Essays Biochem. (2004) 40:89–104.
  • ••Thorough review of repressionmechanisms.
  • BARNES PJ: Anti-inflammatory actions of: molecular mechanisms. Clin. Sci. (1998) 94:557–572.
  • •Excellent overview of the anti-inflammatory activity of GR.
  • DE BOSSCHER K, SCHMITZ ML, VANDEN BERGHE W, PLAISANCE S, FIERS W, HAEGEMAN G: Glucocorticoid-mediated repression of nuclear factor-KB-dependent transcription involves direct interference with transactivation. Proc. Natl. Acad. Sci. USA (1997) 94:13504–13509.
  • REICHARDT HM, KAESTNER KH, TUCKERMANN J et al.: DNA binding of the glucocorticoid receptor is not essential survival [see comments]. Cell (1998) 93:531–541.
  • •Genetic test of activation/repression model.
  • ZHOU XF, SHEN XQ, L: Ligand-activated retinoic acid receptor inhibits AP-1 transactivation by disrupting c-Jun/c-Fos dimerization. MoL Endocrinol. (1999) 13:276–285.
  • MEYER T, GUSTAFSSON JA, CARLSTEDT-DUKE J: Glucocorticoid-dependent transcriptional repression of the osteocalcin gene by competitive binding at the TATA box. DNA Cell Biol. (1997) 16:919–927.
  • DE LANGE P, KOPER JW, HUIZENGA NA et al.: Differential hormone-dependent transcriptional activation and - repression by naturally occurring human glucocorticoid receptor variants. MoL Endocrinol. (1997) 11:1156–1164.
  • DE BOSSCHER K, BERGHE W, HAEGEMAN G: Glucocorticoid repression of AP-1 is not mediated by competition for nuclear coactivators. MoL Endocrinol. (2001) 15:219–227.
  • HECK S, BENDER K, KULLMANN M, GOTTLICHER M, HERRLICH P, CATO AC: I KB a-independent downregulation of NF-KB activity by glucocorticoid receptor. EMBO J. (1997) 16:4698–4707.
  • RAY A. SIEGEL MD, KE, RAY P: Anti-inflammation: direct physical association and functional antagonism between transcription factor NF-KB and the glucocorticoid receptor. Chest (1995) 107:139S.
  • GOTTLICHER M, HECK S, P: Transcriptional cross-talk, the second mode of steroid hormone receptor action. J. Mot Med. (1998) 76:480–489.
  • NISSEN RM, YAMAMOTO KR: The glucocorticoid receptor inhibits NFKB by interfering with serine-2 phosphorylation of the RNA polymerase II carboxy-terminal domain. Genes Dev. (2000) 14:2314–2239.
  • KASSEL 0, SCHNEIDER S, HEILBOCK C, LITFIN M, GOTTLICHER M, HERRLICH P: A nuclear isoform of the focal adhesion LIM-domain protein Trip6 integrates and repressing signals at AP-1-and NF-KB-regulated promoters. Genes Dev. (2004) 18:2518–2528.
  • McNALLY JG, MULLER WG, D, WOLFORD R, HAGER GL: The glucocorticoid receptor: rapid exchange with regulatory sites in living cells. Science (2000) 287:1262–1265.
  • ROGATSKY I, ZAREMBER KA, YAMAMOTO KR: Factor recruitment and TIF2/GRIP1 corepressor activity at a collagenase-3 response element that mediates regulation by phorbol esters and hormones. EMBO J. (2001) 20:6071–6083.
  • •Demonstration that GR co-opts co-activators for repression purposes.
  • BRUNA A, NICOLAS M, MUNOZ A, KYRIAKIS JM, CAELLES C: Glucocorticoid receptor-JNK interaction mediates inhibition of the JNK pathway by glucocorticoids. EMBOJ. (2003) 22:6035–6044.
  • MALCHOFF CD, MALCHOFF DM: Glucocorticoid resistance and hypersensitivity. Endocrinol. Metab. Clin. North Am. (2005) 34:315–326.
  • KIM MY, BUYON JP, PETRI M, SKOVRON ML, SHORE RE: Equivalence trials in SLE research: issues to consider. Lupus (1999) 8:620–626.
  • CHAVASSIEUX PM, ARLOT ME, ROUX JP et al.: Effects of alendronate on bone quality and remodeling in glucocorticoid- induced osteoporosis: a histomorphometric analysis of transiliac biopsies. J. Bone Miner. Res. (2000) 15:754–762.
  • NIEMAN LK, CHROUSOS GP, KELLNER C et al.: Successful treatment of Cushing's syndrome with the glucocorticoid antagonist RU 486.1 Clin. Endocrinol. Metab. (1985) 61:536–540.
  • SCHULTE HM, CHROUSOS GP, GOLD PW et al.: Continuous administration of synthetic ovine corticotropin-releasing factor in man. Physiological and pathophysiological implications. J. Clin. Invest. (1985) 75:1781–1785.
  • BJORNTORP P, ROSMOND R: Hypothalamic origin of the metabolic syndrome X. Ann. IVY Acad. Sci. (1999) 892:297–307.
  • KATSUMATA M, GUPTA C, BAKER MK, SUSSDORF CE, GOLDMAN AS: Diphenylhydantoin: an alternative ligand of a glucocorticoid affecting prostaglandin generation in A/J mice. Science (1982) 218:1313–1315.
  • SCHMIDT TJ, MILLER-DIENER A, LITWACK G: X-lapachone, a specific competitive inhibitor of ligand binding to the glucocorticoid receptor. J. Biol. Chem. (1984) 259:9536–9543.
  • MINER JN, TYREE C, HU J et al.: A nonsteroidal glucocorticoid receptor antagonist. MoL EndocrinoL (2003) 17(1):117–127.
  • TU N, LINK JT, SORENSEN BK et aL: Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator. Bioorg-. Med. Chem. Lett. (2004) 14:4179–4183.
  • JACOBSON PB, VON GELDERN TW, OHMAN Let al.: Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of Type 2 diabetes. J. PharmacoL Exp. Ther. (2005) 314(1):191–200.
  • •Novel approach to a SeGRA.
  • EINSTEIN M, GREENLEE M, G et al.: Selective glucocorticoid receptor nonsteroidal ligands completely antagonize the dexamethasone mediated induction of enzymes involved in gluconeogenesis and glutamine metabolism. J. Steroid Biochem. MoL Biol. (2004) 92:345–356.
  • ROUSSEAU GG, BAXTER JD, TOMKINS GM: Glucocorticoid receptors: relations between steroid binding and biological effects. J. MoL Biol. (1972) 67:99–115.
  • MARKHAM A, BRYSON HM:. A review of its pharmacological properties and therapeutic efficacy. Drugs (1995) 50:317–333.
  • KROGSGAARD MR, LUND B, JOHNSSON B: A longterm prospective study of the equipotency between deflazacort and prednisolone in the treatment of patients with polymyalgia rheumatica. j Rheumatol. (1995) 22:1660–1662.
  • CALLEJA C, PASCUSSI JM, MANI JC, MAUREL P, VILAREM MJ: The antibiotic rifampicin is a nonsteroidal ligand and activator of the human glucocorticoid receptor. Nat. Med. (1998) 4:92–96.
  • VISSER J, HILLEBRANDS JL, J: No evidence that rifampicin has glucocorticoid-like immunosuppressive leading to suppression of rat- proliferation in vitro. Antimicrob. Chemother. (2001) 47:894–895.
  • PROCOPIOU PA, BIGGADIKE K, ENGLISH AF et al.: Novel glucocorticoid antedrugs possessing a 1713-(y-lactone) ring. J. Med. Chem. (2001) 44:602–612.
  • •Review on a new glucocorticoid.
  • BODOR N: Recent advances in retrometabolic design approaches. J. Control Release (1999) 62:209–222.
  • BODOR N, VARGA M: Effect of a novel soft steroid on the wound healing of rabbit cornea. Exp. Eye Res. (1990) 50:183–187.
  • METSELAAR JM, WAUBEN MH, WAGENAAR-HILBERS JP, OC, STORM G: Complete remission of experimental arthritis by joint targeting of glucocorticoids with long-circulating liposomes. Arthritis Rheum. (2003) 48:2059–2066.
  • •Review on a new glucocorticoid.
  • PAUL-CLARK MJ, GILROY DW, WILLIS D, WILLOUGHBY DA, TOMLINSON A: Nitric oxide synthase inhibitors have opposite effects on acute inflammation depending on their route of administration. J. Immunol. (2001) 166:1169–1177.
  • PAUL-CLARK M, DEL SOLDATO P, FIORUCCI S, FLOWER RJ, M: 21-NO-prednisolone is a novel nitric oxide-releasing derivative of prednisolone with enhanced anti-inflammatory properties. Br. J. PharmacoL (2000) 131:1345–1354.
  • •Review on a new glucocorticoid.
  • PAUL-CLARK MJ, MANCINI L, DEL SOLDATO P, FLOWER RJ, PERRETTI M: Potent antiarthritic properties of a glucocorticoid derivative, NCX-1015, in an experimental model of arthritis. Proc. Natl. Acad. Sci. USA (2002) 99:1677–1682.
  • •Review on a new glucocorticoid.
  • ALLAN GF, LENG X, TSAI SY et ell.: Hormone and antihormone induce distinct conformational changes which are central to steroid receptor activation. J. Biol. Chem. (1992) 267:19513–19520.
  • FENG W, RIBEIRO RC, WAGNER RL et al.: Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors. Science (1998) 280:1747–1749.
  • APRILETTI JW, RIBEIRO RC, WAGNER RL et al.: Molecular and structural biology of thyroid hormone. Clin. Exp. PharmacoL PhysioL Suppl. (1998) 25:S2–S11.
  • COSMAN F, LINDSAY R: Selective estrogen receptor modulators: clinical spectrum. Endocr. Rev. (1999) 20:418–434.
  • NEGRO-VILAR A: Selective androgen receptor modulators (SARMs): a novel approach to androgen therapy for the new millennium. J. Clin. Endocrinol. Metab. (1999) 84:3459–3462.
  • McDONNELL DP, NORRIS JD: Analysis of the molecular pharmacology of estrogen receptor agonists and antagonists provides insights into the mechanism of action of estrogen in bone. Osteoporos. Int. (1997) 1\(Suppl. 7):S29–S34.
  • TSAI MJ, O'MALLEY BW: Molecular mechanisms of action of steroid/thyroid receptor superfamily members.. Rev. Biochem. (1994) 63:451–486.
  • REICHARDT HM, TRONCHE F, BERGER S, KELLENDONK C, SCHUTZ G: New insights into glucocorticoid and mineralocorticoid signaling: lessons from gene targeting. Adv. PharmacoL (2000) 47:1–21.
  • •Review of GR and MR knockouts and mutants.
  • VAYSSIERE BM, DUPONT S, CHOQUART A et aL: Synthetic glucocorticoids that dissociate transactivation and AP-1 transrepression exhibit antiinflammatory activity in vivo. MoL EndocrinoL (1997) 11:1245–255.
  • VANDEN BERGHE W, E, DE BOSSCHER K, RESCHE-RIGON M, HAEGEMAN G: Dissociated glucocorticoids with anti-inflammatory potential repress interleukin-6 gene expression by a nuclear factor-KB-dependent mechanism. MoL PharmacoL (1999) 56:797–806.
  • BELVISI MG, WICKS SL, CH et al.: Therapeutic benefit of a dissociated glucocorticoid and the relevance of in vitro separation of transrepression from transactivation activity.. (2001) 166: 1975-1982.
  • ELMORE SW, PRATT JK, MJ et al.: Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators. Bioorg-. Med. Chem. Lett. (2004) 14:1721–1727.
  • •Review on SGRMs.
  • LIN CW, NAKANE M, STASHKO M aL: trans-Activation and repression of the novel nonsteroid glucocorticoid receptor ligand 2,5-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethy1-5-(1-methylcyclohexen-3-y 1)-1H- pyrano13,4-fiquinoline (A276575) and its four stereoisomers. MoL PharmacoL (2002) 62:297–303.
  • COGHLAN MJ, JACOBSON PB, LANE B et al.: A novel antiinflammatory maintains glucocorticoid efficacy with reduced side effects. MoL Endocrinol. (2003) 17:860–869.
  • MINER JN: Designer glucocorticoids. Biochem. PharmacoL (2002) 64:355–361.
  • SCHACKE H, SCHOTTELIUS A, DOCKE WD et al.: Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. Proc. NatL Acad. Sci. USA (2004) 101:227–232.
  • •Review on a SeGRA.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.