Academic literature on the topic 'Glucocorticoid receptor modulator'

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Journal articles on the topic "Glucocorticoid receptor modulator"

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Gossye, V., D. Elewaut, K. Van Beneden, P. Dewint, G. Haegeman, and K. De Bosscher. "A plant-derived glucocorticoid receptor modulator attenuates inflammation without provoking ligand-induced resistance." Annals of the Rheumatic Diseases 69, no. 01 (2009): 291–96. http://dx.doi.org/10.1136/ard.2008.102871.

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Background:Acquired resistance to glucocorticoids constitutes a major clinical challenge, often overlooked in the search for improved alternatives to classic steroids. We sought to unravel how two glucocorticoid receptor-activating compounds, dexamethasone and Compound A, influence glucocorticoid receptor levels and how this can be correlated to their gene regulatory potential.Methods:Compound A and dexamethasone were applied in a short-term and long-term treatment protocol. By quantitative PCR analysis in fibroblast-like synoviocytes (FLS) the gene regulatory potential of both compounds in th
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Small, Benjamin, Charles E. F. Millard, Edwina P. Kisanga, et al. "The Selective Progesterone Receptor Modulator Ulipristal Acetate Inhibits the Activity of the Glucocorticoid Receptor." Journal of Clinical Endocrinology & Metabolism 105, no. 3 (2019): 716–34. http://dx.doi.org/10.1210/clinem/dgz139.

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Abstract Context The selective progesterone modulator ulipristal acetate (ulipristal) offers a much-needed therapeutic option for the clinical management of uterine fibroids. Although ulipristal initially passed safety evaluations in Europe, postmarketing analysis identified cases of hepatic injury and failure, leading to restrictions on the long-term use of ulipristal. One of the factors potentially contributing to significant side effects with the selective progesterone modulators is cross-reactivity with other steroid receptors. Objective To determine whether ulipristal can alter the activi
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Atucha, Erika, Ioannis Zalachoras, José K. van den Heuvel, et al. "A Mixed Glucocorticoid/Mineralocorticoid Selective Modulator With Dominant Antagonism in the Male Rat Brain." Endocrinology 156, no. 11 (2015): 4105–14. http://dx.doi.org/10.1210/en.2015-1390.

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Adrenal glucocorticoid hormones are potent modulators of brain function in the context of acute and chronic stress. Both mineralocorticoid (MRs) and glucocorticoid receptors (GRs) can mediate these effects. We studied the brain effects of a novel ligand, C118335, with high affinity for GRs and modest affinity for MRs. In vitro profiling of receptor-coregulator interactions suggested that the compound is a “selective modulator” type compound for GRs that can have both agonistic and antagonistic effects. Its molecular profile for MRs was highly similar to those of the full antagonists spironolac
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Wang, Liu, Tae Gyu Oh, Jason Magida, et al. "Bromodomain containing 9 (BRD9) regulates macrophage inflammatory responses by potentiating glucocorticoid receptor activity." Proceedings of the National Academy of Sciences 118, no. 35 (2021): e2109517118. http://dx.doi.org/10.1073/pnas.2109517118.

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In macrophages, homeostatic and immune signals induce distinct sets of transcriptional responses, defining cellular identity and functional states. The activity of lineage-specific and signal-induced transcription factors are regulated by chromatin accessibility and other epigenetic modulators. Glucocorticoids are potent antiinflammatory drugs; however, the mechanisms by which they selectively attenuate inflammatory genes are not yet understood. Acting through the glucocorticoid receptor (GR), glucocorticoids directly repress inflammatory responses at transcriptional and epigenetic levels in m
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Liang, Yuan, Tiehua Zhang, Jingqi Zhao, et al. "Glucocorticoid receptor-mediated alleviation of inflammation by berberine: in vitro, in silico and in vivo investigations." Food & Function 12, no. 23 (2021): 11974–86. http://dx.doi.org/10.1039/d1fo01612a.

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Jones, Amanda, Dong-Jin Hwang, Ramesh Narayanan, Duane D. Miller, and James T. Dalton. "Effects of a Novel Selective Androgen Receptor Modulator on Dexamethasone-Induced and Hypogonadism-Induced Muscle Atrophy." Endocrinology 151, no. 8 (2010): 3706–19. http://dx.doi.org/10.1210/en.2010-0150.

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Glucocorticoids are the most widely used antiinflammatory drugs in the world. However, prolonged use of glucocorticoids results in undesirable side effects such as muscle wasting, osteoporosis, and diabetes. Skeletal muscle wasting, which currently has no approved therapy, is a debilitating condition resulting from either reduced muscle protein synthesis or increased degradation. The imbalance in protein synthesis could occur from increased expression and function of muscle-specific ubiquitin ligases, muscle atrophy F-box (MAFbx)/atrogin-1 and muscle ring finger 1 (MuRF1), or decreased functio
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Nemoto, Takahiro, and Yoshihiko Kakinuma. "Prenatal and Postnatal Methyl-Modulator Intervention Corrects the Stress-Induced Glucocorticoid Response in Low-Birthweight Rats." International Journal of Molecular Sciences 22, no. 18 (2021): 9767. http://dx.doi.org/10.3390/ijms22189767.

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Low body weight at birth has been shown to be a risk factor for future metabolic disorders, as well as stress response abnormalities and depression. We showed that low-birthweight rats had prolonged high blood corticosterone levels after stress exposure, and that an increase in Gas5 lncRNA, a decoy receptor for glucocorticoid receptors (GRs), reduces glucocorticoid responsiveness. Thus, we concluded that dampened pituitary glucocorticoid responsiveness disturbed the glucocorticoid feedback loop in low-birthweight rats. However, it remains unclear whether such glucocorticoid responsiveness is s
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Bungard, Christopher J., George D. Hartman, Jesse J. Manikowski, et al. "Discovery of selective glucocorticoid receptor modulator MK-5932." Bioorganic & Medicinal Chemistry 19, no. 24 (2011): 7374–86. http://dx.doi.org/10.1016/j.bmc.2011.10.054.

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Ayroldi, Emira, Antonio Macchiarulo, and Carlo Riccardi. "Targeting glucocorticoid side effects: selective glucocorticoid receptor modulator or glucocorticoid‐induced leucine zipper? A perspective." FASEB Journal 28, no. 12 (2014): 5055–70. http://dx.doi.org/10.1096/fj.14-254755.

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Polari, Lauri, Santeri Anttila, Terhi Helenius, et al. "Novel Selective Estrogen Receptor Modulator Ameliorates Murine Colitis." International Journal of Molecular Sciences 20, no. 12 (2019): 3007. http://dx.doi.org/10.3390/ijms20123007.

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Estrogen-receptor-mediated signaling has been suggested to decrease the inflammatory response in monocyte macrophages. Previously, we showed that a novel selective estrogen receptor modulator (SERM2) promotes anti-inflammatory phenotype of monocytes in vitro. In this study, we demonstrate the potential of SERM2 in amelioration of colitis. We utilized a dextran sodium sulfate (DSS)-induced colitis model in FVB/n mice to demonstrate the effects of orally administered SERM2 on the clinical status of the mice and the histopathological changes in the colon, as well as proportion of Mrc-1 positive m
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Dissertations / Theses on the topic "Glucocorticoid receptor modulator"

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Thiele, Sylvia. "Bone-sparing and anti-inflammatory potential of the novel selective glucocorticoid receptor modulator, compound A." Doctoral thesis, Saechsische Landesbibliothek- Staats- und Universitaetsbibliothek Dresden, 2013. http://nbn-resolving.de/urn:nbn:de:bsz:14-qucosa-114824.

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Rheumatoid arthritis (RA) is a common chronic inflammatory disease that affects about 1% of the Western population. Glucocorticoids (GC) are widely used for the treatment of RA and other immune-mediated diseases, such as asthma, but their use is associated with adverse effects on bone metabolism. Because of that, new selective GC receptor (GR) agonists (SEGRAs) with the potential for an improved risk/benefit profile have been developed. Compound A (CpdA) is a novel SEGRA, which showed an improved risk/benefit profile concerning glucose metabolism, however the effects on bone are not well inves
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Zein, Naïmah. "“CpdX”, a non-steroidal Selective Glucocorticoid Receptor Agonistic Modulator (SEGRAM) selectively triggers the beneficial anti-inflammatory activity of glucocorticoids, but not their long-term debilitating effects." Thesis, Strasbourg, 2018. http://www.theses.fr/2018STRAJ088.

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Lors de la liaison d’un glucocorticoïde (GC) naturel ou synthétique (par exemple, la Dexaméthasone) au récepteur des glucocorticoïdes (GR), les GCs régulent l’expression de gènes cibles soit par (i) transactivation par liaison ‘’directe’’ à un élément de liaison à l’ADN de type ‘’(+)GRE’’, (ii) transrépression ‘’directe’’ par liaison à un élément de type ‘’nGRE’’ ou (iii) transrépression ‘’indirecte’’ par interaction physique directe avec des facteurs de transcription pro-inflammatoires tels que AP-1 et NF-κB. Les effets anti-inflammatoires bénéfiques des GCs sont généralement attribués à la t
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Thiele, Sylvia [Verfasser], Lorenz C. [Akademischer Betreuer] Hofbauer, Günter [Akademischer Betreuer] Vollmer, and Lorenz [Akademischer Betreuer] Hofbauer. "Bone-sparing and anti-inflammatory potential of the novel selective glucocorticoid receptor modulator, compound A / Sylvia Thiele. Gutachter: Günter Vollmer ; Lorenz Hofbauer. Betreuer: Lorenz C. Hofbauer." Dresden : Saechsische Landesbibliothek- Staats- und Universitaetsbibliothek Dresden, 2013. http://d-nb.info/1068152702/34.

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McInnes, Kerry J. "Hepatic 5α-reduced glucocorticoids : modulators of glucocorticoid receptor activation in obesity". Thesis, University of Edinburgh, 2003. http://hdl.handle.net/1842/24946.

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In obese versus lean Zucker rats, hepatic 5α-reductase type 1 mRNA expression and protein levels were increased. They also had increased activity of hepatic 5β-reductase activity. By contrast, 3α-hydroxysteroid dehydrogenase mRNA expression was unchanged in obesity. Greater inactivation of B by A-ring reductases in liver may decrease local corticosterone (B) concentrations in these sites, and increase the metabolic clearance rate of glucocorticoids, thus increasing drive to the hypothalamic-pituitary-adrenal axis (HPA). To investigate whether 5α-reduced metabolites of corticosterone are glucoc
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Tilborg, Marc van. "The glucocorticoid receptor DNA binding domain : structure and allosteric modulation = het DNA binded domein van de glucocorticoide receptor /." [S.l. : s.n.], 1998. http://www.gbv.de/dms/bs/toc/250860244.pdf.

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Tran, Thuyet Van. "Modulation of Folate Receptor-alpha by Glucocorticoid Receptor and Progesterone Receptor." University of Toledo Health Science Campus / OhioLINK, 2005. http://rave.ohiolink.edu/etdc/view?acc_num=mco1104777244.

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Tran, Thuyet Van. "Modulation of folate receptor-[alpha] by glucocorticoid receptor and progesterone receptor." Connect to full-text via OhioLINK ETD Center, 2004. http://rave.ohiolink.edu/etdc/view?acc%5Fnum=mco1104777244.

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Thesis (Ph. D.)--Medical College of Ohio, 2004.<br>"In partial fulfillment of the requirements for the degree of Doctor of Philosophy in Medical Sciences." Major advisor: Manohar Ratnam. Includes abstract. Document formatted into pages: iii, 293 p. Title from title page of PDF document. Includes bibliographical references (p. 175-281).
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Kuipa, Michael. "Antiretroviral drugs differentially modulate glucocorticoid activity via the glucocorticoid receptor in vitro." Master's thesis, Faculty of Science, 2019. http://hdl.handle.net/11427/31426.

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Concurrent use of anti-retroviral drugs (ARVs) and progestin-based hormonal contraceptives is widespread. During times of stress and during glucocorticoid (GC) therapy, intracellular ARVs are in the presence of high concentrations of GCs, which regulate all aspects of immunity and inflammation via the glucocorticoid receptor (GR). However, the reciprocal modulation of ARV and steroid intracellular functions is relatively unexplored. In this study, the effects of the ARVs tenofovir disoproxil fumarate (TDF), dapivirine (DPV), and maraviroc (MVC) on activation of the GR and GR-regulated mRNA exp
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Osman, Waffa. "Modulation of nuclear receptor function by interacting proteins /." Stockholm : Karolinska institutet, 2007. http://diss.kib.ki.se/2007/978-91-7357-264-4/.

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Heeley, Robert P. "The phenotypic consequences of genetic variation in the modulatory domain of the rat glucocorticoid receptor." Thesis, University of Glasgow, 1998. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.241738.

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Books on the topic "Glucocorticoid receptor modulator"

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Hobson, Adrian. The Medicinal Chemistry of Glucocorticoid Receptor Modulators. Springer Nature Switzerland, 2023. http://dx.doi.org/10.1007/978-3-031-28732-9.

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Hobson, Adrian. Medicinal Chemistry of Glucocorticoid Receptor Modulators. Springer, 2023.

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Henter, Ioline D., and Rodrigo Machado-Vieira. Novel therapeutic targets for bipolar disorder. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780198748625.003.0030.

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The long-term course of bipolar disorder (BD) comprises recurrent depressive episodes and persistent residual symptoms for which standard therapeutic options are scarce and often ineffective. Glutamate is the major excitatory neurotransmitter in the central nervous system, and glutamate and its cognate receptors have consistently been implicated in the pathophysiology of mood disorders and in the development of novel therapeutics for these disorders. Since the rapid and robust antidepressant effects of the N-methyl-D-aspartate (NMDA) antagonist ketamine were first observed in 2000, other NMDA
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Elder, Grahame J. Metabolic bone disease after renal transplantation. Edited by Jeremy R. Chapman. Oxford University Press, 2015. http://dx.doi.org/10.1093/med/9780199592548.003.0288.

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Patients who undergo kidney transplantation have laboratory, bone, and soft tissue abnormalities that characterize chronic kidney disease mineral and bone disorder (CKD-MBD). After successful transplantation, abnormal values of parathyroid hormone, fibroblast growth factor 23, calcium, phosphate, vitamin D sterols, and sex hormones generally improve, but abnormalities often persist. Cardiovascular risk remains high and is influenced by prevalent vascular calcification, and fracture risk increases due to a combination of abnormal bone ‘quality’, compounded by immunosuppressive drugs and reducti
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Book chapters on the topic "Glucocorticoid receptor modulator"

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Hobson, Adrian. "Selective Glucocorticoid Receptor Modulators." In SpringerBriefs in Molecular Science. Springer Nature Switzerland, 2023. http://dx.doi.org/10.1007/978-3-031-28732-9_5.

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Tashiro, Fumio, Shigeru Morimura, Nobuo Horikoshi, Kazuko Kato, and Yoshio Ueno. "Deregulation of c-myc Gene and Modulation of Glucocorticoid Receptor by Aflatoxin B1." In Microbial Toxins in Foods and Feeds. Springer US, 1990. http://dx.doi.org/10.1007/978-1-4613-0663-4_44.

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Živadinović, Dragoslava, Željko Džakula, and Radoslav K. Andjus. "Temperature Modulation of Glucocorticoid-receptor Affinity in a Hibernator, the European Ground Squirrel, and a Non-Hibernator, the Rat." In Life in the Cold. Springer Berlin Heidelberg, 2000. http://dx.doi.org/10.1007/978-3-662-04162-8_30.

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H. Check, Jerome, and Diane L. Check. "Progesterone and Glucocorticoid Receptor Modulator Mifepristone (RU-486) as Treatment for Advanced Cancers." In Repurposed Drugs for Cancer [Working Title]. IntechOpen, 2020. http://dx.doi.org/10.5772/intechopen.93545.

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Rauner, Martina, Sylvia Thiele, Claudia Goettsch, Elena Tsourdi, and Lorenz C. Hofbauer. "Compound A Is a Selective Glucocorticoid Receptor Modulator with Potent Anti-Inflammatory Effects and Bone-Sparing Potential." In The Endocrine Society's 93rd Annual Meeting & Expo, June 4–7, 2011 - Boston. The Endocrine Society, 2011. http://dx.doi.org/10.1210/endo-meetings.2011.part1.p1.p1-19.

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Nixon, Mark, Rodger Duffin, Adriano G. Rossi, Brian R. Walker, and Ruth Andrew. "5α-Reduced Glucocorticoids as Endogenous Selective Glucocorticoid Receptor Modulators." In The Endocrine Society's 93rd Annual Meeting & Expo, June 4–7, 2011 - Boston. The Endocrine Society, 2011. http://dx.doi.org/10.1210/endo-meetings.2011.part1.p1.p1-18.

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Nunez, B. Scott, and Wayne V. Vedeckis. "Monitoring nuclear receptor function." In Receptors: Structure and function. Oxford University PressOxford, 2001. http://dx.doi.org/10.1093/oso/9780199638819.003.0011.

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Abstract The glucocorticoid receptor (GR), one of the first nuclear receptors to be characterized and to have its gene cloned, serves to illustrate the complexity of nuclear receptor function. The expression of the GR gene is regulated by at least three different promoters and the resulting mRNAs can be differentially spliced into several transcriptional variants (1-3). Following the translation of these transcripts into protein, the activity and/or subcellular distribution of the GR protein may be modified by post-translational modifications such as phosphorylation (4). In the absence of liga
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Coghlan, Michael J., Steven W. Elmore, Philip R. Kymt, and Michael E. Kort. "Chapter 17. Selective glucocorticoid receptor modulators." In Annual Reports in Medicinal Chemistry. Elsevier, 2002. http://dx.doi.org/10.1016/s0065-7743(02)37018-0.

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Zhang, Yanmin, Hui Sheng, Jinshun Qi, Bei Ma, and Xin Ni. "Glucocorticoids Rapidly Modulate NMDA Receptor Activity Via Multiple Signaling Pathways in Hippocampal Neurons." In BASIC/TRANSLATIONAL - Glucocorticoid Disease & Physiology. The Endocrine Society, 2011. http://dx.doi.org/10.1210/endo-meetings.2011.part4.p5.p3-508.

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"Modulation of IL1 Receptor Expression by IL1, Prostaglandins and Glucocorticoids." In Lymphocyte Activation and Differentiation. De Gruyter, 1988. http://dx.doi.org/10.1515/9783110850253-024.

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Conference papers on the topic "Glucocorticoid receptor modulator"

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Lesovaya, Ekaterina A., Kirill I. Kirsanov, Irina V. Budunova, and Marianna G. Yakubovskaya. "Abstract 214: Anticancer effect of Compound A, a novel modulator of the glucocorticoid receptor, in acute leukemia cells." In Proceedings: AACR 101st Annual Meeting 2010‐‐ Apr 17‐21, 2010; Washington, DC. American Association for Cancer Research, 2010. http://dx.doi.org/10.1158/1538-7445.am10-214.

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Chupp, G. L., K. M. Beeh, A. Jauhiainen, et al. "Results of a Phase 2b Dose Finding Study of Velsecorat, an Inhaled Non-Steroidal, Selective Glucocorticoid Receptor Modulator in Asthma (GRANIT)." In American Thoracic Society 2021 International Conference, May 14-19, 2021 - San Diego, CA. American Thoracic Society, 2021. http://dx.doi.org/10.1164/ajrccm-conference.2021.203.1_meetingabstracts.a1202.

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Necander, S., S. Lawrence, L. Thurman, et al. "Design of a Phase 1 Virtual Hybrid Study of AZD7594, an Inhaled Non-Steroidal, Selective Glucocorticoid Receptor Modulator, in Adolescents with Asthma." In American Thoracic Society 2020 International Conference, May 15-20, 2020 - Philadelphia, PA. American Thoracic Society, 2020. http://dx.doi.org/10.1164/ajrccm-conference.2020.201.1_meetingabstracts.a3733.

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Chupp, G. L., M. N. Brown, K. M. Beeh, et al. "Design of a Phase 2b Dose Finding Study of AZD7594, an Inhaled Non-Steroidal, Selective Glucocorticoid Receptor Modulator, for the Treatment of Asthma." In American Thoracic Society 2019 International Conference, May 17-22, 2019 - Dallas, TX. American Thoracic Society, 2019. http://dx.doi.org/10.1164/ajrccm-conference.2019.199.1_meetingabstracts.a1315.

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Hegelund Myrbäck, T., S. Prothon, M. Dearman, et al. "SAT0251 Selective glucocorticoid receptor modulator shows potent anti-inflammatory effect with improved metabolic profile in a phase i study supported by in vitro data." In Annual European Congress of Rheumatology, EULAR 2018, Amsterdam, 13–16 June 2018. BMJ Publishing Group Ltd and European League Against Rheumatism, 2018. http://dx.doi.org/10.1136/annrheumdis-2018-eular.5451.

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Pinkerton, J. W., B. Dekkak, D. Zervas, et al. "Velsecorat (AZD7594), a Selective Glucocorticoid Receptor Modulator (SGRM) Demonstrates Favorable Pre-Clinical Efficacy vs Safety Profile Compared to Current Clinical Inhaled Steroid, Fluticasone Furoate." In American Thoracic Society 2021 International Conference, May 14-19, 2021 - San Diego, CA. American Thoracic Society, 2021. http://dx.doi.org/10.1164/ajrccm-conference.2021.203.1_meetingabstracts.a1418.

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Adeel, Z., K. Kaczmarek, P. Ramos-Ramirez, and O. Tliba. "Non-Genomic Effects of Glucocorticoids Differentially Modulate Glucocorticoid Receptor Site-Specific Phosphorylation." In American Thoracic Society 2020 International Conference, May 15-20, 2020 - Philadelphia, PA. American Thoracic Society, 2020. http://dx.doi.org/10.1164/ajrccm-conference.2020.201.1_meetingabstracts.a2375.

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Hendrickx, R., T. Hegelund-Myrbäck, M. Dearman, et al. "SAT0245 Azd9567: a novel oral selective glucocorticoid receptor modulator, demonstrated to have an improved therapeutic ratio compared to prednisolone in pre-clinical studies, is safe and well tolerated in first clinical study." In Annual European Congress of Rheumatology, EULAR 2018, Amsterdam, 13–16 June 2018. BMJ Publishing Group Ltd and European League Against Rheumatism, 2018. http://dx.doi.org/10.1136/annrheumdis-2018-eular.6360.

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Safy, M., MJ De Hair, JW Jacobs, F. Buttgereit, MC Kraan, and JM van Laar. "AB0428 A systematic review on efficacy and safety of selective glucocorticoid receptor modulators in comparison to glucocorticoids in arthritis." In Annual European Congress of Rheumatology, 14–17 June, 2017. BMJ Publishing Group Ltd and European League Against Rheumatism, 2017. http://dx.doi.org/10.1136/annrheumdis-2017-eular.3254.

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Ramos-Ramirez, P., Z. Adeel, K. Kaczmarek, and O. Tliba. "Glucocorticoid Receptor (GR)-Beta Modulates PDGF-Induced Airway Smooth Muscle Proliferation." In American Thoracic Society 2020 International Conference, May 15-20, 2020 - Philadelphia, PA. American Thoracic Society, 2020. http://dx.doi.org/10.1164/ajrccm-conference.2020.201.1_meetingabstracts.a4410.

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