Combinatorial Screening for Specific Drug Solubilizers with Switchable Release Profiles

À propos
Confidentialité
Mentions légales

Graph Chatbot

Publications associées (30)

A novel cell-based sensor detecting the activity of individual basic proprotein convertases

Daniel Constam, Karin Irmgard Löw, Stefan Kunz

The basic proprotein convertases (PCs) furin, PC1/3, PC2, PC5/6, PACE4, PC4, and PC7 are promising drug targets for human diseases. However, developing selective inhibitors remains challenging due to overlapping substrate recognition motifs and limited str ...

WILEY2019

Extrapolating the Fragment-Based Approach to Inorganic Drug Discovery

Paul Joseph Dyson, Lucinda Kate Batchelor

The fragment-based approach is a well-established strategy for organic drug discovery. Recent studies have shown that this approach also has considerable potential in medicinal inorganic chemistry, and yet the approach has not been formally described. Here ...

ELSEVIER2019

Nickel-Catalyzed Regioselective Hydroalkylation and Hydroarylation of Alkenyl Boronic Esters

Xile Hu, Srikrishna Bera

Metal hydride catalyzed hydrocarbonation reactions of alkenes are an efficient approach to construct new carbon-carbon bonds from readily available alkenes. However, the regioselectivity of hydrocarbonation remains challenging to be controlled. In nickel h ...

Wiley-VCH Verlag GmbH2019

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK

Stewart Cole

Mycobacterium tuberculosis, the etiological agent of the infectious disease tuberculosis, kills approximately 1.5 million people annually, while the spread of multidrug-resistant strains is of great global concern. Thus, continuous efforts to identify new ...

Nature Research2018

Novel probes for the non-invasive bioluminescence imaging of mitochondrial membrane potential and dipeptidylpeptidase-4 activity in living animals

Arkadiy Bazhin

Current thesis summarizes the work on development of novel bioluminescent probes for measurement of activity of dipeptidylpep-tidase-4 (DPP-4) and for quantification of mitochondrial membrane potential (MMP). DPP-4 enzyme plays critical role in develop-men ...

EPFL2018

Electrostatic spray ionization from 384-well microtiter plates for mass spectrometry analysis based enzyme assay and drug metabolism screening

Hubert Girault, Liang Qiao, Elena Tobolkina, Tzu-En Lin, Xiaoqin Zhong, Yan Deng, Emna Belghith

We have realized the direct ionization of samples from wells of microtiter plates under atmospheric conditions for mass spectrometry analysis without any liquid delivery system or any additional interface. The microtiter plate is a commercially available 3 ...

American Chemical Society2017

Ligand-Protein Affinity Studies Using Long-Lived States of Fluorine-19 Nuclei

Geoffrey Bodenhausen, Roberto Buratto, Daniele Mammoli, Estel Canet Martinez

The lifetimes T-LLS of long-lived states or T-LLC of long-lived coherences can be used for the accurate determination of dissociation constants of weak protein ligand complexes. The remarkable contrast between signals derived from LLS or LLC in free and bo ...

American Chemical Society2016

Homogeneous time-resolved G protein-coupled receptor-ligand binding assay based on fluorescence cross-correlation spectroscopy

Luc Henry

G protein-coupled receptors (GPCRs) mediate many important physiological functions and are considered as one of the most successful therapeutic target classes for a wide spectrum of diseases. Drug discovery projects generally benefit from a broad range of ...

Academic Press Inc Elsevier Science2016

Inhibiting Mycobacterium tuberculosis within and without

Stewart Cole

Tuberculosis remains a scourge of global health with shrinking treatment options due to the spread of drug-resistant strains of Mycobacterium tuberculosis. Intensive efforts have been made in the past 15 years to find leads for drug development so that bet ...

Royal Soc2016

The Principles of Ligand Specificity on beta-2-adrenergic receptor

Shuguang Yuan

G protein-coupled receptors are recognized as one of the largest families of membrane proteins. Despite sharing a characteristic seven-transmembrane topology, G protein-coupled receptors regulate a wide range of cellular signaling pathways in response to v ...

Nature Research2016

Page 2 sur 2