670242-76-9Relevant academic research and scientific papers
An AKAP-Lbc-RhoA interaction inhibitor promotes the translocation of aquaporin-2 to the plasma membrane of renal collecting duct principal cells
Schrade, Katharina,Tr?ger, Jessica,Eldahshan, Adeeb,Zühlke, Kerstin,Abdul Azeez, Kamal R.,Elkins, Jonathan M.,Neuenschwander, Martin,Oder, Andreas,Elkewedi, Mohamed,Jaksch, Sarah,Andrae, Karsten,Li, Jinliang,Fernandes, Joao,Müller, Paul Markus,Grunwald, Stephan,Marino, Stephen F.,Vuki?evi?, Tanja,Eichhorst, Jenny,Wiesner, Burkhard,Weber, Marcus,Kapiloff, Michael,Rocks, Oliver,Daumke, Oliver,Wieland, Thomas,Knapp, Stefan,Von Kries, Jens Peter,Klussmann, Enno
, (2018/02/06)
Stimulation of renal collecting duct principal cells with antidiuretic hormone (arginine-vasopressin, AVP) results in inhibition of the small GTPase RhoA and the enrichment of the water channel aquaporin-2 (AQP2) in the plasma membrane. The membrane inser
Nonpeptidic Selective Inhibitors of the Chymotrypsin-Like (β5 i) Subunit of the Immunoproteasome
Sosi?, Izidor,Gobec, Martina,Brus, Boris,Knez, Damijan,?ivec, Matej,Konc, Janez,Le?nik, Samo,Ogrizek, Mitja,Obreza, Ale?,?igon, Du?an,Jane?i?, Du?anka,Mlinari?-Ra??an, Irena,Gobec, Stanislav
, p. 5745 - 5748 (2016/05/09)
Elevated expression of the immunoproteasome has been associated with autoimmune diseases, inflammatory diseases, and various types of cancer. Selective inhibitors of the immunoproteasome are not only scarce, but also almost entirely restricted to peptide-based compounds. Herein, we describe nonpeptidic reversible inhibitors that selectively block the chymotrypsin-like (β5i) subunit of the human immunoproteasome in the low micromolar range. The most potent of the reversibly acting compounds were then converted into covalent, irreversible, nonpeptidic inhibitors that retained selectivity for the β5i subunit. In addition, these inhibitors discriminate between the immunoproteasome and the constitutive proteasome in cell-based assays. Along with their lack of cytotoxicity, these data point to these nonpeptidic compounds being suitable for further investigation as β5i-selective probes for possible application in noncancer diseases related to the immunoproteasome.
PSORALEN DERIVATIVES AS NON-PEPTIDIC INHIBITORS OF CHYMOTRYPSIN-LIKE ACTIVITY OF THE IMMUNOPROTEASOME
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, (2016/10/11)
This invention relates to new inhibitors of chymothrypsin-like activity of the immunoproteasome (inhibitors of β5? or LMP7 subunit) with the general formula (I), where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the treatment of diseases where immunoproteasome activity is increased.
Synthesis of modified psoralen analogues
Garazd,Garazd,Ogorodniichuk,Khilya
, p. 291 - 300 (2007/10/03)
Substituted 3-(5-methyl-7-oxofuro[3,2-g]chromen-6-yl)propanoic acids analogous to psoralen were synthesized by linear annulation of a furan moiety to the coumarin system.
