Estrogen receptors (ER) are nuclear hormone which responsible for sex signaling in women. A series of (1,4-disubstituted)-1,2,3-triazoles 5–21 were prepared by reaction azidophenols with terminal alkynes under Fokin conditions. The products purified column chromatography or recrystallization and characterized NMR HRMS. compounds tested binding to ERβ via a ligand displacement assay, 1-(4-hydrox...

PDZ (PSD-95, DiscsLarge, ZO1) domains function in nature as protein binding domains within scaffold and membrane-associated proteins. They comprise ∼90 residues and make specific, high affinity interactions with complementary C-terminal peptide sequences, with other PDZ domains, and with phospholipids. We hypothesized that the specific, strong interactions of PDZ domains with their ligands woul...

Colicin Ia, a 626-residue bactericidal protein, consists of three domains, with the carboxy-terminal domain (C domain) responsible for channel formation. Whole colicin Ia or C domain added to a planar lipid bilayer membrane forms voltage-gated channels. We have shown previously that the channel formed by whole colicin Ia has four membrane-spanning segments and an approximately 68-residue segmen...

The Drosophila melanogaster ecdysone receptor (EcR) is produced in three isoforms, which mediate developmental processes such as metamorphosis. These isoforms were expressed in Saccharomyces cerevisiae to elucidate aspects of receptor transcription activity in a highly defined genetic model system. All three EcR isoforms showed ligand-independent transcriptional activation of an ecdysone report...

The CXCR4 chemokine receptor is a G protein-coupled receptor that plays an important role in leukocyte homing, cancer metastasis, and human immunodeficiency virus infection. In response to ligand stimulation, chemokine receptors undergo endocytosis through clathrin-coated vesicle (CCV). Uncoating of CCV, a process involving heat shock cognate protein and several other proteins, is critical for ...

Reprint requests to Dr. B. Kersting. E-mail: [email protected] Z. Naturforsch. 55 b, 1179-1187 (2000); received August 17, 2000 Cobalt Complexes, Amine-Thiolate Ligands, Sulfinate Complexes The reactivity of Co111 amine-thiolate complexes with terminal and bridging thiolate func­ tions towards oxidizing agents has been investigated. The mononuclear Co N3S3 complex [Coni(L1)] (2)...

High resolution structural studies of models of glutamate receptors (GluRs) have been limited to monomeric models of the ligand-binding site. To obtain oligomeric models of glutamate receptors that can reveal more complete structural information, we examined the assembly and ligand binding properties of two truncated versions of the GluR1 subunit. The first version, GluR1-WS, consisted of only ...

The asymmetric unit of the title complex, [Co(NCS)2(C7H9N)2(CH3OH)2], comprises of one CoII cation located on a centre of inversion, one thio-cyanate ligand, one methanol ligand and one 3,5-di-methyl-pyridine ligand. The CoII cation is octa-hedrally coordinated by two terminal N-bonding thio-cyanate anions, two methanol mol-ecules and two 3,5-di-methyl-pyridine ligands into a discrete complex. ...

BRD4 (bromodomain-containing protein 4) is an epigenetic reader that realizes histone proteins and promotes the transcription of genes linked to cancer progression non-cancer diseases such as acute heart failure severe inflammation. The highly conserved N-terminal bromodomain (BD1) recognizes acylated lysine residues organize expression genes. As such, BD1 essential for disrupting interactions ...

Abstract The reactions of [Fe2Cp2(CO)4] with a series isocyanides, CNR, were conducted in acetonitrile and afforded, after thermal treatment, the mono-isocyanide derivatives [Fe2Cp2(CO)3(CNR)] [R = 1H-indol-5-yl, 1; CH2P(O)(OEt)2, 2; Cy = C6H11, 3; 4-C6H4OMe, 4; Xyl = 2,6-C6H3Me2, 5; Me, 6; 2-naphthyl, 7; Bn = CH2Ph, 8]. In order to avoid multiple substitution, diiron reactant was used molar ex...