Cited by 123
The natural product prodigiosin 1, often described as an H+/Cl- symport cotransporter, can transport Cl- across lipid vesicles via an anion exchange (or antiport) mechanism.
University of Maryland, College Park
Publishes on Crystallization and Solubility Studies, X-ray Diffraction in Crystallography, Molecular Sensors and Ion Detection. 15 papers and 434 citations.
Add your photo, update your bio, and get notified when your ranking changes.
The natural product prodigiosin 1, often described as an H+/Cl- symport cotransporter, can transport Cl- across lipid vesicles via an anion exchange (or antiport) mechanism.
The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification of 1 (AMG319), a compound with an IC50 of 16 nM in a human whole blood assay (HWB), excellent selectivity over a large panel of protein kinases, and a high level of in vivo efficacy as measured by two rodent disease models of inflammation.
Self-assembled transporter: Self-association of a partial-cone calixarene amide provides membrane-active aggregates that enable the transport of chloride anions across phospholipid membranes (see picture). Additionally, a regulatory system is described, wherein an inactive calixarene analogue inhibits the active chloride transporter. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2006/z504489_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
Structure-based rational design led to the synthesis of a novel series of potent PI3K inhibitors. The optimized pyrrolopyridine analogue 63 was a potent and selective PI3Kβ/δ dual inhibitor that displayed suitable physicochemical properties and pharmacokinetic profile for animal studies. Analogue 63 was found to be efficacious in animal models of inflammation including a keyhole limpet hemocyanin (KLH) study and a collagen-induced arthritis (CIA) disease model of rheumatoid arthritis. These studies highlight the potential therapeutic value of inhibiting both the PI3Kβ and δ isoforms in the treatment of a number of inflammatory diseases.