Concept

Hit to lead

Publications associées (69)

Functionalized pyrrolidine inhibitors of human alpha- mannosidases II in cancer: optimizing the fit to the active site

Refining the chemical structure of functionalized pyrrolidine-based inhibitors of Golgi α- mannosidase II (GMII) to optimize binding affinity provided a lead molecule that demonstrated nanomolar competitive inhibition of α-mannosidases II and an optimal fi ...

2008

A new synthetic access to furo[3,2-f]chromene analogues of an antimycobacterial

Stewart Cole

From the structure of 3,3-dimethyl-3H-benzofuro[3,2-f][1]-benzopyran, a selective in vitro inhibitor of mycobacterial growth, we have undertaken a structure-activity relationship investigation. We wish to report here our results on the use of [2+3] cycload ...

2008

A novel drug discovery concept for tuberculosis: inhibition of bacterial and host cell signalling

Stewart Cole, Edina Rita Székely, Gabor Nemeth

The Mycobacterium tuberculosis genome encodes for eleven eukaryotic-like Ser/Thr protein kinases. At least three of these (PknA, PknB and PknG) are essential for bacterial growth and survival. PknG is secreted by pathogenic mycobacteria, in macrophages to ...

2008

Dual-color Total Internal Reflection Fluorescence Fluctuation Spectroscopy

Theo Lasser, Marcel Leutenegger

We developed a dual-color total internal reflection fluorescence (TIRF) system for single molecule imaging and fluorescence fluctuation spectroscopy (FFS). For a performance analysis, we measured a synthetic binding assay with dual-color global fluorescenc ...

2006

Dual-color Total Internal Reflection Fluorescence Fluctuation Spectroscopy

Theo Lasser, Marcel Leutenegger

2006

High Relaxivity Confined to a Small Molecular Space: A Metallostar-Based, Potential MRI Contrast Agent

André Merbach, Alain Borel, Eva Jakab Toth, Joao Bruno Livramento Fig.

Good things come in small packages: For its moderate molecular weight, the metallostar complex [Fe{Gd2L(H2O)4}3]4− (see picture; L is a bipyridine–poly(aminocarboxylate) derivative) displays exceptionally high proton relaxivity, which is explained in terms ...

2005

Processing along the way: forwarding vs. coding

Christina Fragouli

We consider a source that transmits to a receiver by routing the information packets over a communication network and examine rate benefits that finite complexity processing at the intermediate nodes may offer. We show that the processing capabilities of t ...

2004

Protein kinases as drug targets in parasitic protozoa

The importance of protein kinases in cell signaling and cell cycle control has led to detailed structural and functional studies in various eukaryotes, and hence to the synthesis of specific chemical inhibitors for managing disease. Here, the current progr ...

Elsevier2002

Structure-Lipophilicity Relationships of Neutral and Protonated β-Blockers, Part I, Intra- and Intermolecular Effects in Isotropic Solvent Systems

Hubert Girault, Pierre-Alain Carrupt

The objectives of this study were to validate new experimental techniques used to measure the log P of protonated drugs, and to investigate the inter- and intramolecular forces influencing the partitioning behavior of β-blockers in isotropic biphasic solve ...

1999

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