Results 51 to 60 of about 81,174 (219)

Further Structure‐Activity Relationship of G Protein‐Gated Inwardly Rectifying Potassium Channels 1/2 Activators: Synthesis and Biological Characterization of In Vitro Tool Compounds

ChemMedChem, EarlyView.
Work presented here details the design and characterize novel G protein‐gated inwardly rectifying potassium channels (GIRK)1/2 activators. A new 4,4‐difluorocyclohexylpyrazole have been identified that confers improved potency and selectivity for GIRK1/2 versus GIRK1/4.
Sumaiya Nahid, Fahad Imtiaz Rahman, Yu Du, Brittany D. Spitznagel, Sandeep K. Singh, Yashpal S. Chhonker, Daryl J. Murry, C. David Weaver, Corey R. Hopkins   +8 more
wiley   +1 more source

New Pyridobenothiazolone Derivatives Display Nanomolar Pan‐Serotype Anti‐Dengue Virus Activity

ChemMedChem, EarlyView.
A ligand‐based strategy is employed, starting from hit compound 2, to develop the C‐2 modified pyridobenzothiazolone 19 as a pan‐serotype nanomolar DENV‐1‐4 inhibitor. Investigations of the mechanism reveal the peculiar ability to abolish the infectivity of virions in a second infection.
Tommaso Felicetti, Chin Piaw Gwee, Kitti Wing Ki Chan, Giacomo Pepe, Ciro Milite, Pietro Campiglia, Satoru Watanabe, Muhammad Danial Bin Mohd Mazlan, Stefano Sabatini, Serena Massari, Oriana Tabarrini, Gianluca Sbardella, Subhash G. Vasudevan, Giuseppe Manfroni   +13 more
wiley   +1 more source

Do Flame Retardants Promote Vitamin D Deficiency? [PDF]

, 2014
Vitamin D deficiency in the Unites States has become more prevalent in recent years. Research has shown that environmental chemicals such as flame-retardants induce hepatic enzymes in the cytochrome P450 family such as CYP24 and CYP3A that are important ...
Petteruti, Audrey
core   +2 more sources

Scientific Opinion on Flavouring Group Evaluation 302 (FGE.302): N-(2-methylcyclohexyl)-2,3,4,5,6-pentafluoro-benzamide from Chemical Group 30 [PDF]

, 2017
Publisher ...
Anastassiadou, Maria, Bolognesi, Claudia, Brimer, Leon, Castle, Laurence, Cravedi, Jean-Pierre, de Fátima Tavares Poças, Maria, EFSA Panel on Food Contact Materials, Enzymes, Flavourings and Processing Aids (CEF), Engel, Karl-Heinz, Fowler, Paul, Franz, Roland, Grob, Konrad, Gürtler, Rainer, Husøy, Trine, Kärenlampi, Sirpa, Mennes, Wim, Mulder, Gerard, Penninks, André, Rosaria Milana, Maria, Silano, Vittorio, Smith, Andrew, Sundh, Ulla Beckman, Tlustos, Christina, Wölfle , Detlef, Zorn, Holger, Zugravu, Corina-Aurelia   +24 more
core   +2 more sources

Novel Para‐Phenylenediamine‐Based Derivatives as Receptor Tyrosine Kinase‐like Orphan Receptor 1 (ROR1) Inhibitors: An In Vitro Preliminary Characterization

ChemMedChem, EarlyView.
ROR1 represents a promising target for the development of novel antiproliferative compounds, giving its high expression in different cancer cell lines. The present study describes the workflow leading to the design, synthesis, and characterization of a series of para‐phenylenediamine‐based compounds able to interact with the target kinase, inhibiting ...
Gerardina Smaldone, Maria Rosaria Miranda, Francesca Di Matteo, Valeria Napolitano, Michela Aliberti, Simona Musella, Veronica Di Sarno, Gianluigi Lauro, Giuseppe Bifulco, Giacomo Pepe, Giovanna Aquino, Mario Felice Tecce, Isabel Maria Gomez‐Monterrey, Pietro Campiglia, Carmine Ostacolo, Alessia Bertamino, Vincenzo Vestuto, Tania Ciaglia   +17 more
wiley   +1 more source

Synthesis and biological characterization of 4,4‐difluoro‐3(phenoxymethyl)piperidine scaffold as dopamine 4 receptor (D4R) antagonist in vitro tool compounds

ChemMedChem, Accepted Article.
We report the discovery and characterization of a novel series of 4,4‐difluoropiperidine etherbased dopamine D4 receptor antagonists. Structure‐activity relationship studies led to the identification of compound 14a, which displays exceptional binding affinity for the D4 receptor (Ki = 0.3 nM) and remarkable selectivity over other dopamine receptor ...
Saeedeh Saeedi, Sumaiya Nahid, Anish Vadukoot, Corey R Hopkins   +3 more
wiley   +1 more source

Molecular biomarkers and toxic consequences of impact by organic pollution in aquatic organisms [PDF]

, 1994
Organic contaminants are readily bioaccumulated by aquatic organisms. Exposure to and toxic effects of contaminants can be measured in terms of the biochemical responses of the organisms (i.e. molecular biomarkers).
Förlin, L., George, S.G., Livingston, D.R.   +2 more
core  

Changes in Protein Expression of Renal Drug Transporters and Drug‐Metabolizing Enzymes in Autosomal Dominant Polycystic Kidney Disease Patients

Clinical Pharmacology &Therapeutics, EarlyView.
Autosomal dominant polycystic kidney disease is the most prevalent inherited kidney disease and leads to bilateral kidney enlargement and progressive loss of renal function, often over decades. Comorbidities include hypertension, flank pain, and bacterial infections. The condition often necessitates prolonged multidrug therapy.
Annika C. Tillmann, Dorien J. M. Peters, Amin Rostami‐Hodjegan, Patricia Wilson, Jill Norman, Jill Barber, Zubida M. Al‐Majdoub   +6 more
wiley   +1 more source

Protein retention in yeast rough endoplasmic reticulum: expression and assembly of human ribophorin I. [PDF]

, 1990
The RER retains a specific subset of ER proteins, many of which have been shown to participate in the translocation of nascent secretory and membrane proteins. The mechanism of retention of RER specific membrane proteins is unknown.
Crowe, JS, Meyer, DI, Sanderson, CM
core  

Targeting of the master receptor MOM19 to mitochondria [PDF]

, 1991
The targeting of proteins to mitochondria involves the recognition of the precursor proteins by receptors on the mitochondrial surface followed by insertion of the precursors into the outer membrane at the general insertion site GIP.
Dietmeier, Klaus A., Eckerskorn, Christoph, Lottspeich, Fritz, Neupert, Walter, Pfanner, Nikolaus, Schneider, Helmut, Söllner, Thomas, Trülzsch, Barbara   +7 more
core   +1 more source