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1. Full Text Selective glucocorticoid receptor agonists: Glucocorticoid therapy with no regrets?
by Cooper, Mark S and Zhou, Hong and Seibel, Markus J
Journal of Bone and Mineral Research, ISSN 0884-0431, 11/2012, Volume 27, Issue 11, pp. 2238 - 2241
Therapeutic glucocorticoids were first developed in the 1950s to treat rheumatoid arthritis. super((1)) Since then the use of these potent anti-inflammatory... 
INDUCED OSTEOPOROSIS | DNA-BINDING | BONE LOSS | CARDIAC TRANSPLANTATION | ORAL CORTICOSTEROIDS | TRANSACTIVATION | ENDOCRINOLOGY & METABOLISM | INDUCED ARTHRITIS | PREVENTION | LIGAND | T-CELLS | Receptors, Glucocorticoid - metabolism | Animals | Bone Density | Humans | Physiological aspects | Corticosteroids | Steroids | Obesity | Antiinflammatory agents | Glucocorticoids | Diabetes mellitus | Cushing's syndrome | Glucocorticoid receptors | Atrophy | Glucose tolerance | Osteoporosis | Side effects | Skin | Bone | Myopathy
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2. Full Text Molecular mechanisms of glucocorticoid action and selective glucocorticoid receptor agonists
by Stahn, Cindy and Löwenberg, Mark and Hommes, Daniel W and Buttgereit, Frank
Molecular and Cellular Endocrinology, ISSN 0303-7207, 2007, Volume 275, Issue 1, pp. 71 - 78
Glucocorticoids (GC) are the most common used anti-inflammatory and immunosuppressive drugs in the treatment of rheumatic and other inflammatory diseases.... 
Mechanisms of action | SEGRA | Non-genomic | mGCR | Glucocorticoid | cGCR | Genomic | RHEUMATOID-ARTHRITIS | TRANSREPRESSION | glucocorticoid | ACTIVATION | BLOOD MONONUCLEAR-CELLS | mechanisms of action | CELL BIOLOGY | DISSOCIATION | genomic | LCK | TRANSACTIVATION | ENDOCRINOLOGY & METABOLISM | FYN | EXPRESSION | non-genomic | T-CELLS | Animals | Anti-Inflammatory Agents - pharmacology | Humans | Glucocorticoids - pharmacology | Immunosuppressive Agents - pharmacology | Cell Membrane - drug effects | Receptors, Glucocorticoid - agonists
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3. Full Text Design and X-Ray Crystal Structures of High-Potency Nonsteroidal Glucocorticoid Agonists Exploiting a Novel Binding Site on the Receptor
by Keith Biggadike and Randy K. Bledsoe and Diane M. Coe and Tony W. J. Cooper and David House and Marie A. Iannone and Simon J. F. MacDonald and Kevin P. Madauss and Iain M. McLay and Tracy J. Shipley and Simon J. Taylor and Thuy B. Tran and Iain J. Uings and Victoria Weller and Shawn P. Williams and Argonne National Lab. (ANL), Argonne, IL (United States)
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 10/2009, Volume 106, Issue 43, pp. 18114 - 18119
Crystallography and computer modeling have been used to exploit a previously unexplored channel in the glucocorticoid receptor (GR). Highly potent,... 
Receptors | Glucocorticoids | Drug interactions | Agonists | Ligands | Amides | Pharmacology | Drug design | Glucocorticoid receptors | Crystal structure | AlleGrow | Intranasal glucocorticoid | Glucocorticoid modulation | TRANSREPRESSION | DOMAIN | drug design | MODULATORS | TRANSACTIVATION | MULTIDISCIPLINARY SCIENCES | intranasal glucocorticoid | LIGAND | FLUTICASONE FUROATE | glucocorticoid modulation | DISCOVERY | Protein Structure, Tertiary | Humans | Models, Molecular | Crystallography, X-Ray | NF-kappa B - metabolism | Receptors, Glucocorticoid - metabolism | Receptors, Glucocorticoid - agonists | Drug Design | Amides - chemistry | Cell Line, Tumor | Amides - metabolism | Binding Sites | Receptors, Glucocorticoid - chemistry | X-ray crystallography | Evaluation | Corticosteroids | Crystals | Properties | Structure | Methods | Binding sites (Biochemistry) | OCCUPATIONS | DESIGN | GLUCOCORTICOIDS | COMPUTERS | INDAZOLES | CRYSTAL STRUCTURE | CRYSTALLOGRAPHY | MATERIALS SCIENCE | SIMULATION | PYRROLIDONES | ACCURACY | AMIDES | Biological Sciences | Physical Sciences
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4. Full Text Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics
by Riether, Doris and Harcken, Christian and Razavi, Hossein and Kuzmich, Daniel and Gilmore, Thomas and Bentzien, Jörg and Pack, Edward J and Souza, Donald and Nelson, Richard M and Kukulka, Alison and Fadra, Tazmeen N and Zuvela-Jelaska, Ljiljana and Pelletier, Josephine and Dinallo, Roger and Panzenbeck, Mark and Torcellini, Carol and Nabozny, Gerald H and Thomson, David S
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2010, Volume 53, Issue 18, pp. 6681 - 6698
Syntheses and structure activity relationships (SA R) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole... 
RESPONSES | SIDE | CHEMISTRY, MEDICINAL | REPRESSION | TRANSCRIPTION | RECEPTOR MODULATORS | LIGAND-BINDING DOMAIN | INTERNAL ALKYNES | DISCOVERY | RAY CRYSTAL-STRUCTURE | MOLECULAR-MECHANISMS | Arthritis, Experimental - drug therapy | Interleukin-6 - antagonists & inhibitors | Aromatase Inhibitors - pharmacology | Stereoisomerism | Humans | Transcriptional Activation | Biological Availability | Structure-Activity Relationship | Insulin - blood | Anti-Inflammatory Agents, Non-Steroidal - pharmacology | Receptors, Glucocorticoid - agonists | Aromatase - genetics | Pyridines - adverse effects | Pyrroles - adverse effects | Female | Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis | Steroids - chemistry | Interleukin-6 - genetics | Cells, Cultured | Pyridines - chemical synthesis | Aromatase - biosynthesis | Enzyme Induction | Models, Molecular | Rats | Rats, Sprague-Dawley | Interleukin-1 - pharmacology | Pyrroles - pharmacology | Animals | Anti-Inflammatory Agents, Non-Steroidal - adverse effects | Pyrroles - chemical synthesis | Hydrogen Bonding | Interleukin-6 - biosynthesis | Mice | Mice, Inbred BALB C | Pyridines - pharmacology | Adipose Tissue - drug effects
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5. Full Text Systemic and Intra-Amygdala Administration of Glucocorticoid Agonist and Antagonist Modulate Extinction of Conditioned Fear
by Yang, Yi-Ling and Chao, Po-Kuan and Lu, Kwok-Tung
Neuropsychopharmacology, ISSN 0893-133X, 05/2006, Volume 31, Issue 5, pp. 912 - 924
We examined the effect of glucocorticoid agonists on the extinction of conditioned fear in rats by using fear-potentiated startle. Systemic injection of... 
Amygdala | Conditioned fear | Extinction | Glucocorticoid | PSYCHOSOCIAL TREATMENT | POSTTRAUMATIC-STRESS-DISORDER | glucocorticoid | amygdala | CORTICOSTERONE | BEHAVIORAL-INHIBITION | PSYCHIATRY | conditioned fear | POTENTIATED STARTLE | D-CYCLOSERINE | NEUROSCIENCES | PREFRONTAL CORTEX | extinction | MEMORY | PREWEANLING RAT | PHARMACOLOGY & PHARMACY | BRAIN | Amygdala - drug effects | Extinction, Psychological - drug effects | Fear - drug effects | Male | Receptors, Glucocorticoid - metabolism | Fear - physiology | Dexamethasone - pharmacology | Reflex, Startle - drug effects | Anxiety Disorders - metabolism | Anxiety Disorders - drug therapy | Receptors, Glucocorticoid - drug effects | Reflex, Startle - physiology | Extinction, Psychological - physiology | Disease Models, Animal | Conditioning (Psychology) - drug effects | Conditioning (Psychology) - physiology | Rats | Avoidance Learning - physiology | Rats, Sprague-Dawley | Hormone Antagonists - pharmacology | Animals | Glucocorticoids - antagonists & inhibitors | Avoidance Learning - drug effects | Mifepristone - pharmacology | Amygdala - physiology | Glucocorticoids - agonists | Anxiety Disorders - physiopathology
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6. Full Text X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain
by Biggadike, Keith and Bledsoe, Randy K and Hassell, Anne M and Kirk, Barrie E and McLay, Iain M and Shewchuk, Lisa M and Stewart, Eugene L and Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Journal of Medicinal Chemistry, ISSN 0022-2623, 06/2008, Volume 51, Issue 12, pp. 3349 - 3352
An X-ray crystal structure is reported for the novel enhanced-affinity glucocorticoid agonist fluticasone furoate (FF) in the ligand binding domain of the... 
CHEMISTRY, MEDICINAL | SEASONAL ALLERGIC RHINITIS | SERIES | NASAL SPRAY | MOMETASONE FUROATE | ESTERS | Androstadienes - chemistry | Humans | Models, Molecular | Crystallography, X-Ray | Protein Conformation | Nuclear Receptor Coactivator 2 - chemistry | Binding Sites | Receptors, Glucocorticoid - chemistry | Receptors, Glucocorticoid - agonists | DEXAMETHASONE | GLUCOCORTICOIDS | LIGANDS | CRYSTAL STRUCTURE | RECEPTORS | 60 APPLIED LIFE SCIENCES
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7. Full Text Efficacy of selective mineralocorticoid and glucocorticoid agonists in canine septic shock
by Hicks, Caitlin W and Sweeney, Daniel A and Danner, Robert L and Eichacker, Peter Q and Suffredini, Anthony F and Feng, Jing and Sun, Junfeng and Behrend, Ellen N and Solomon, Steven B and Natanson, Charles
Critical Care Medicine, ISSN 0090-3493, 01/2012, Volume 40, Issue 1, pp. 199 - 207
Objective: Corticosteroid regimens that stimulate both mineralocorticoid and glucocorticoid pathways consistently reverse vasopressor-dependent hypotension in... 
Infection | Sepsis | Models | Corticosteroids | Animal | UNITED-STATES | models | infection | METAANALYSIS | RECEPTOR | CRITICALLY-ILL | MECHANISMS | HYDROCORTISONE | corticosteroids | animal | HYPERRENINEMIC HYPOALDOSTERONISM | ALDOSTERONE | sepsis | SEVERE SEPSIS | CRITICAL CARE MEDICINE | Blood Volume - drug effects | Shock, Septic - prevention & control | Water-Electrolyte Balance - drug effects | Central Venous Pressure - drug effects | Interleukin-6 - blood | Shock, Septic - drug therapy | Desoxycorticosterone - administration & dosage | Heart - physiopathology | Water-Electrolyte Balance - physiology | Dexamethasone - administration & dosage | Blood Volume - physiology | Central Venous Pressure - physiology | Lung - physiopathology | Shock, Septic - physiopathology | Desoxycorticosterone - therapeutic use | Serum Albumin - analysis | Sodium - blood | Mineralocorticoids - agonists | Dexamethasone - therapeutic use | Pneumonia, Staphylococcal - drug therapy | Animals | Platelet Count | Lung - drug effects | Dogs | Heart - drug effects | Glucocorticoids - agonists
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8. Full Text Synthetic progestins used in HRT have different glucocorticoid agonist properties
by Koubovec, Dominique and Ronacher, Katharina and Stubsrud, Elisabeth and Louw, Ann and Hapgood, Janet Patricia
Molecular and Cellular Endocrinology, ISSN 0303-7207, 2005, Volume 242, Issue 1, pp. 23 - 32
The synthetic progestins, medroxyprogesterone acetate (MPA) and norethisterone acetate (NET-EN or NET-A), are widely used as female contraceptive agents and in... 
Medroxyprogesterone | Agonist potency | Phosphorylation | Hormone replacement therapy | Norethisterone | Glucocorticoid receptor | glucocorticoid receptor | IMMUNE CELLS | SELECTIVE PROGESTIN | RECEPTOR | FACTOR-KAPPA-B | medroxyprogesterone | CELL BIOLOGY | BREAST-CANCER | norethisterone | agonist potency | INTRAMUSCULAR INJECTION | INTERLEUKIN-8 GENE | ENDOCRINOLOGY & METABOLISM | hormone replacement therapy | HORMONE-REPLACEMENT THERAPY | MEDROXYPROGESTERONE ACETATE PROVERA | POSTMENOPAUSAL WOMEN | phosphorylation | Cell Line | Humans | Transcriptional Activation - drug effects | Medroxyprogesterone Acetate - pharmacology | Rats | Receptors, Glucocorticoid - metabolism | Medroxyprogesterone Acetate - metabolism | Trypsin - metabolism | Hormone Replacement Therapy | Norethindrone - analogs & derivatives | Receptors, Glucocorticoid - agonists | Animals | Transfection | Norethindrone - pharmacology | Progesterone Congeners - pharmacology | Glucocorticoids - pharmacology | Phosphorylation - drug effects | Progesterone Congeners - metabolism | Glucocorticoids - agonists | Norethindrone - metabolism | Genes, Reporter
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9. Full Text Widespread Negative Response Elements Mediate Direct Repression by Agonist- Liganded Glucocorticoid Receptor
by Surjit, Milan and Ganti, Krishna Priya and Mukherji, Atish and Ye, Tao and Hua, Guoqiang and Metzger, Daniel and Li, Mei and Chambon, Pierre
Cell, ISSN 0092-8674, 2011, Volume 145, Issue 2, pp. 224 - 241
The glucocorticoid (GC) receptor (GR), when liganded to GC, activates transcription through direct binding to simple (+)GRE DNA binding sequences (DBS).... 
ATOPIC-DERMATITIS | GENE PROMOTER | MOUSE KERATINOCYTES | BIOCHEMISTRY & MOLECULAR BIOLOGY | GROWTH | REV-ERB-ALPHA | MICE | MECHANISMS | BINDING | THYMIC STROMAL LYMPHOPOIETIN | BETA | CELL BIOLOGY | Promoter Regions, Genetic | Animals | Cytokines | Response Elements | Humans | Gene Expression Regulation | Transcription, Genetic | Mice | Dermatitis, Atopic - metabolism | Repressor Proteins - metabolism | Receptors, Glucocorticoid - agonists | Corticosteroids | Steroids
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10. Full Text Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores
by Betageri, Raj and Gilmore, Thomas and Kuzmich, Daniel and Kirrane, Thomas M and Bentzien, Jörg and Wiedenmayer, Dieter and Bekkali, Younes and Regan, John and Berry, Angela and Latli, Bachir and Kukulka, Alison J and Fadra, Tazmeen N and Nelson, Richard M and Goldrick, Susan and Zuvela-Jelaska, Ljiljana and Souza, Don and Pelletier, Josephine and Dinallo, Roger and Panzenbeck, Mark and Torcellini, Carol and Lee, Heewon and Pack, Edward and Harcken, Christian and Nabozny, Gerald and Thomson, David S
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2011, Volume 21, Issue 22, pp. 6842 - 6851
We report a SAR of non-steroidal glucocorticoid mimetics that utilize indoles as A-ring mimetics. A detailed SAR is discussed with a focus on improving PR and... 
Dissociated activity | Non-steroidal glucocorticoid agonist | Function-regulating pharmacophore | TRANSREPRESSION | CHEMISTRY, MEDICINAL | CRYSTAL-STRUCTURE | CHEMISTRY, ORGANIC | MECHANISMS | DISCOVERY | MAMMARY-TUMOR VIRUS | IN-VITRO | TRANSACTIVATION | RECEPTOR MODULATORS | BINDING | EXPRESSION | Animals | Humans | Glucocorticoids - chemistry | Glucocorticoids - pharmacology | Models, Molecular | Indoles - pharmacology | Mice | Receptors, Glucocorticoid - metabolism | Structure-Activity Relationship | HeLa Cells | Indoles - chemistry | Receptors, Glucocorticoid - agonists | Corticosteroids | Analysis | Prednisolone | Steroids
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11. Full Text Nonsteroidal glucocorticoid agonists: Tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (Transrepression/Transactivation) efficacy selectivity
by Biggadike, Keith and Boudjelal, Mohamed and Clackers, Margaret and Coe, Diane M and Demaine, Derek A and Hardy, George W and Humphreys, Davina and Inglis, Graham G. A and Johnston, Michael J and Jones, Haydn T and House, David and Loiseau, Richard and Needham, Deborah and Skone, Philip A and Uings, Iain and Veitch, Gemma and Weingarten, Gordon G and McLay, Iain M and Macdonald, Simon J. F
Journal of Medicinal Chemistry, ISSN 0022-2623, 12/2007, Volume 50, Issue 26, pp. 6519 - 6534
The synthesis and biological activity of tetrahydronaphthalene derivatives coupled to various heterocycles are described. These compounds are potent... 
SUBSTITUTION | DESIGN | CHEMISTRY, MEDICINAL | IN-VITRO PROFILE | MODULATORS | RECEPTOR-LIGAND | LEADS | VIVO ACTIVITY | MECHANISMS | LIGAND-BINDING DOMAIN | Cell Line | Transcription, Genetic - drug effects | Receptors, Glucocorticoid - antagonists & inhibitors | Drug Partial Agonism | Stereoisomerism | Humans | Tetrahydronaphthalenes - chemical synthesis | Transcriptional Activation - drug effects | Models, Molecular | Anti-Inflammatory Agents, Non-Steroidal - chemistry | Structure-Activity Relationship | Anti-Inflammatory Agents, Non-Steroidal - pharmacology | Receptors, Glucocorticoid - agonists | Molecular Mimicry | NF-kappa B - genetics | Tetrahydronaphthalenes - chemistry | Tetrahydronaphthalenes - pharmacology | Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis | Mammary Tumor Virus, Mouse - genetics | Binding Sites
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12. Full Text 2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists
by Chantigny, Yves A and Murray, John C and Kleinman, Edward F and Robinson, Ralph P and Plotkin, Michael A and Reese, Matthew R and Buckbinder, Leonard and McNiff, Patricia A and Millham, Michele L and Schaefer, Jean F and Abramov, Yuriy A and Bordner, Jon
Journal of Medicinal Chemistry, ISSN 0022-2623, 03/2015, Volume 58, Issue 6, pp. 2658 - 2677
A significant improvement in agonist activity of the previously described 2-aryloctahydrophenanthrene-2,3,7-triol series of dissociated glucocorticoid receptor... 
CHEMISTRY, MEDICINAL | DISCOVERY | Cell Line | Anti-Inflammatory Agents - pharmacology | Humans | Matrix Metalloproteinase 13 - genetics | Tumor Necrosis Factor-alpha - blood | Models, Molecular | Crystallography, X-Ray | Receptors, Glucocorticoid - metabolism | Receptors, Glucocorticoid - agonists | Up-Regulation - drug effects | Phenanthrenes - chemistry | Phenanthrenes - pharmacology | Animals | Dexamethasone - pharmacology | Interleukin-1 - immunology | Tumor Necrosis Factor-alpha - immunology | Mice | Mammary Tumor Virus, Mouse - genetics
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13. Full Text Discovery of New non-steroidal selective glucocorticoid receptor agonists
by Potamitis, Constantinos and Siakouli, Dimitra and Papavasileiou, Konstantinos D and Boulaka, Athina and Ganou, Vassiliki and Roussaki, Marina and Calogeropoulou, Theodora and Zoumpoulakis, Panagiotis and Alexis, Michael N and Zervou, Maria and Mitsiou, Dimitra J
Journal of Steroid Biochemistry and Molecular Biology, ISSN 0960-0760, 02/2019, Volume 186, pp. 142 - 153
Glucocorticoids (GCs) are widely used as potent anti-inflammatory drugs; however, GC therapy is often accompanied by adverse side effects. The... 
Virtual screening | MD simulations | Selective agonists | Anti-Inflammatory action | Pharmacophore model | Glucocorticoid receptor | HORMONE | LIGANDS | BIOCHEMISTRY & MOLECULAR BIOLOGY | ENDOCRINOLOGY & METABOLISM | EXPRESSION | NF-κB protein | Side effects | Inflammation | Antiinflammatory agents | Glucocorticoids | Benzothiazole
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14. Full Text Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists
by Regan, John and Lee, Thomas W and Zindell, Renée M and Bekkali, Younes and Bentzien, Jörg and Gilmore, Thomas and Hammach, Abdelhakim and Kirrane, Thomas M and Kukulka, Alison J and Kuzmich, Daniel and Nelson, Richard M and Proudfoot, John R and Ralph, Mark and Pelletier, Josephine and Souza, Donald and Zuvela-Jelaska, Lijiljana and Nabozny, Gerald and Thomson, David S
Journal of Medicinal Chemistry, ISSN 0022-2623, 12/2006, Volume 49, Issue 26, pp. 7887 - 7896
We report on the nuclear receptor binding affinities, cellular activities of transrepression and transactivation, and anti-inflammatory properties of a... 
TRANSREPRESSION | RESPONSES | CHEMISTRY, MEDICINAL | TRANSACTIVATION | MODULATORS | IN-VIVO | TRANSCRIPTION | RECEPTOR LIGAND | BINDING | FIBROBLASTS | MOLECULAR-MECHANISMS | Humans | Transcriptional Activation | Aromatase - metabolism | Anti-Inflammatory Agents, Non-Steroidal - chemistry | Quinolones - pharmacology | Trans-Activators - chemistry | Anti-Inflammatory Agents, Non-Steroidal - pharmacology | Molecular Mimicry | Dexamethasone - pharmacology | Quinolones - chemistry | Quinolones - chemical synthesis | Female | Trans-Activators - pharmacology | Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis | Fibroblasts - metabolism | Trans-Activators - chemical synthesis | Animals | Fibroblasts - drug effects | Lipopolysaccharides - pharmacology | Fibroblasts - cytology | Mice | Mice, Inbred BALB C | HeLa Cells | Glucocorticoids - agonists | Receptors, Cytoplasmic and Nuclear - metabolism
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15. Full Text Non-steroidal glucocorticoid agonists—The discovery of aryl pyrazoles as A-ring mimetics
by Clackers, Margaret and Coe, Diane M and Demaine, Derek A and Hardy, George W and Humphreys, Davina and Inglis, Graham G.A and Johnston, Michael J and Jones, Haydn T and House, David and Loiseau, Richard and Minick, Doug J and Skone, Philip A and Uings, Iain and McLay, Iain M and Macdonald, Simon J.F
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2007, Volume 17, Issue 17, pp. 4737 - 4745
Based on a modelling and iterative approach, a potent dissociated glucocorticoid agonist was discovered where the benzoxazinone is replaced with an aryl... 
Aryl pyrazole | Agonist | Glucocorticoid | Non-steroidal | Dissociated | Tetrahydronaphthalene | glucocorticoid | DESIGN | CHEMISTRY, MEDICINAL | MODULATORS | CHEMISTRY, ORGANIC | RECEPTOR | agonist | MECHANISMS | dissociated | IN-VITRO | aryl pyrazole | LIGANDS | non-steroidal | tetrahydronaphthalene | Chemistry, Pharmaceutical - methods | Models, Chemical | Stereoisomerism | Molecular Conformation | Receptors, Glucocorticoid - agonists |