Discovery and Optimization of N-Acyl-6-sulfonamide-tetrahydroquinoline Derivatives as Novel Non-Steroidal Selective Glucocorticoid Receptor Modulators.
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DOI: 10.1021/acs.jmedchem.2c01082
Abstract: Selective glucocorticoid receptor modulators (SGRMs), which can dissociate the transactivation from the transrepression of the glucocorticoid receptor (GR), are regarded as very promising therapeutics for inflammatory and autoimmune diseases. We previously discovered a SGRM HP-19… read more here.
Keywords: glucocorticoid; receptor modulators; glucocorticoid receptor; acyl sulfonamide ... See more keywords
Discovery of a novel nonsteroidal selective glucocorticoid receptor modulator by virtual screening and bioassays
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DOI: 10.1038/s41401-021-00855-6
Abstract: Synthetic glucocorticoids (GCs) have been widely used in the treatment of a broad range of inflammatory diseases, but their clinic use is limited by undesired side effects such as metabolic disorders, osteoporosis, skin and muscle… read more here.
Keywords: glucocorticoid receptor; glucocorticoid; screening bioassays; selective glucocorticoid ... See more keywords
Safety, Pharmacokinetics and Pharmacodynamics of the Selective Glucocorticoid Receptor Modulator Velsecorat (AZD7594) Following Inhalation in Healthy Volunteers
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DOI: 10.2147/dddt.s334960
Abstract: Introduction Velsecorat (AZD7594) is a non-steroidal, selective, glucocorticoid receptor modulator (SGRM), being developed for the treatment of asthma. This article reports the initial, first-in-human, single and repeat dose-escalating study in healthy male volunteers. Methods The… read more here.
Keywords: velsecorat azd7594; glucocorticoid receptor; receptor modulator; velsecorat ... See more keywords
Relacorilant, a Selective Glucocorticoid Receptor Modulator, Induces Clinical Improvements in Patients With Cushing Syndrome: Results From A Prospective, Open-Label Phase 2 Study
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Endocrinology"
DOI: 10.3389/fendo.2021.662865
Abstract: Introduction/Purpose Relacorilant is a selective glucocorticoid receptor modulator (SGRM) with no progesterone receptor activity. We evaluated the efficacy and safety of relacorilant in patients with endogenous Cushing syndrome (CS). Materials and Methods A single-arm, open-label,… read more here.
Keywords: glucocorticoid receptor; relacorilant selective; cushing syndrome; receptor ... See more keywords