(+)-ZK 216348 - CAS 669073-68-1
Category: Inhibitor
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Glucocorticoid Receptor
(+)-ZK 216348 is a selective nonsteroidal glucocorticoid receptor (GR) agonist for the treatment of experimental colitis (IC50 values of 20, 20, and 80 nM for GR, Progesterone (PR) and Mineralocorticoid (MR) receptors, respectively). (+)-ZK 216348 exhibits antiinflammatory activity for both systemic and topical application, and shows no negative effects on intestinal epithelial migration or proliferation.
Brife Description:
glucocorticoid receptor (GR) agonist
ZK-216348; 4-(2,3-dihydro-1-benzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamide
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1.Effects of dissociated glucocorticoids on OPG and RANKL in osteoblastic cells.
Humphrey EL;Williams JH;Davie MW;Marshall MJ Bone. 2006 May;38(5):652-61. Epub 2005 Nov 17.
Glucocorticoids are effective anti-inflammatory and immunosuppressive agents, but their use is often associated with debilitating side effects such as glucocorticoid-induced osteoporosis. Newly developed glucocorticoid analogues such as the so-called dissociated glucocorticoids are potent immunosuppressants and have the potential for fewer side effects. The effects of these new analogues on osteoprotegerin (OPG) and receptor activator of NF-kappaB ligand (RANKL) in osteoblastic cells have not been studied. OPG and RANKL are osteoblast-derived proteins pivotal to the regulation of bone mass. RANKL stimulates bone resorption by increasing osteoclast differentiation, activation and survival. OPG is the decoy receptor for RANKL and thus inhibits bone resorption. Here, we show that dexamethasone, prednisolone, deflazacort and the dissociated glucocorticoids, RU24858, RU40066, RU24782, AL438-F1 and ZK216348 significantly inhibit OPG production in two human osteoblastic cell lines (MG63 and hFOB). The potency for OPG inhibition was ligand and cell-type specific. In both cell types, dexamethasone and prednisolone were the most potent ligands inhibiting OPG production with IC(50)s of approximately 0.
2.Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects.
Schäcke H;Schottelius A;Döcke WD;Strehlke P;Jaroch S;Schmees N;Rehwinkel H;Hennekes H;Asadullah K Proc Natl Acad Sci U S A. 2004 Jan 6;101(1):227-32. Epub 2003 Dec 23.
Glucocorticoids (GCs) are the most commonly used antiinflammatory and immunosuppressive drugs. Their outstanding therapeutic effects, however, are often accompanied by severe and sometimes irreversible side effects. For this reason, one goal of research in the GC field is the development of new drugs, which show a reduced side-effect profile while maintaining the antiinflammatory and immunosuppressive properties of classical GCs. GCs affect gene expression by both transactivation and transrepression mechanisms. The antiinflammatory effects are mediated to a major extent via transrepression, while many side effects are due to transactivation. Our aim has been to identify ligands of the GC receptor (GR), which preferentially induce transrepression with little or no transactivating activity. Here we describe a nonsteroidal selective GR-agonist, ZK 216348, which shows a significant dissociation between transrepression and transactivation both in vitro and in vivo. In a murine model of skin inflammation, ZK 216348 showed antiinflammatory activity comparable to prednisolone for both systemic and topical application. A markedly superior side-effect profile was found with regard to increases in blood glucose, spleen involution, and, to a lesser extent, skin atrophy; however, adrenocorticotropic hormone suppression was similar for both compounds.
3.Discovery of quinolines as selective glucocorticoid receptor agonists.
Jaroch S;Berger M;Huwe C;Krolikiewicz K;Rehwinkel H;Schäcke H;Schmees N;Skuballa W Bioorg Med Chem Lett. 2010 Oct 1;20(19):5835-8. doi: 10.1016/j.bmcl.2010.07.125. Epub 2010 Aug 3.
The dissociated glucocorticoid receptor (GR) agonist ZK 216348 is rendered GR-selective over other nuclear hormone receptors through replacing the methylbenzoxazine with a quinoline moiety. Compounds were shown to be efficacious in cell assays with respect to inflammation endpoints, along with reduced activity in a transactivation assay, hinting at an improved therapeutic window over corticosteroids.
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CAS 669073-68-1 (+)-ZK 216348

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