Publications related to Receptor antagonist

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

Stewart Cole, Neeraj Dhar, Florence Pojer, Ruben Hartkoorn, Gaëlle Séraphine Kolly, Joao Pedro De Almeida Neres

Phenotypic screening of a quinoxaline library against replicating Mycobacterium tuberculosis led to the identification of lead compound Ty38c (3-((4-methoxybenzyl)amino)-6-(trifluoromethyl)quinoxaline-2-carboxylic acid). With an MIC99 and MBC of 3.1 mu M, ...

American Chemical Society2015

Reversible Local and Global Switching in Multicomponent Supramolecular Networks: Controlled Guest Release and Capture at the Solution/Solid Interface

Magalí Alejandra Lingenfelder, Fernando Pablo Cometto

Dynamically switchable supramolecular systems offer exciting possibilities in building smart surfaces, the structure and thus the function of which can be controlled by using external stimuli. Here we demonstrate an elegant approach where the guest binding ...

Amer Chemical Soc2015

Exploring Weak Ligand-Protein Interactions by Long-Lived NMR States: Improved Contrast in Fragment-Based Drug Screening

Geoffrey Bodenhausen, Daniele Mammoli, Roberto Buratto

Ligands that have an affinity for protein targets can be screened very effectively by exploiting favorable properties of long-lived states (LLS) in NMR spectroscopy. In this work, we describe the use of LLS for competitive binding experiments to measure ac ...

Wiley-Blackwell2014

Towards a new combination therapy for tuberculosis with next generation benzothiazinones

Paul Joseph Dyson, Stewart Cole, Florence Pojer, Ruben Hartkoorn, Anthony Vocat, Ming Zhang, Joao Pedro De Almeida Neres, Thierry Buclin, Benoit Lechartier

The benzothiazinone lead compound, BTZ043, kills Mycobacterium tuberculosis by inhibiting the essential flavo-enzyme DprE1, decaprenylphosphoryl-beta-D-ribose 2-epimerase. Here, we synthesized a new series of piperazine-containing benzothiazinones (PBTZ) a ...

2014

Drug concentration prediction and delivery

Giovanni De Micheli, Alena Simalatsar, Wenqi You Dubout

In medical practice, the decision-making process regarding drug dose is critical to patients’ health and recovery. For drugs with narrow therapeutic ranges, the medical doctor decides the quantity (dose amount) and frequency (dose interval) on the basis of ...

2014

Mixtures of Chemical Pollutants at European Legislation Safety Concentrations: How Safe Are They?

Kristin Schirmer

The risk posed by complex chemical mixtures in the environment to wildlife and humans is increasingly debated, but has been rarely tested under environmentally relevant scenarios. To address this issue, two mixtures of 14 or 19 substances of concern (pesti ...

Oxford University Press2014

Chemical Modification of Graphene via Hyperthermal Molecular Reaction

Klaus Kern, Marko Burghard, Stephan Rauschenbach, Sabine Abb, Gordon Rinke

Chemical functionalization of graphene is achieved by hyperthermal reaction with azopyridine molecular ions. The one-step, room temperature process takes place in high vacuum (10(7) mbar) using an electrospray ion beam deposition (ES-IBD) setup. For ion su ...

Amer Chemical Soc2014

Regulation of Steatohepatitis and PPARγ Signaling by Distinct AP-1 Dimers

Johan Auwerx, Evan Graehl Williams

Nonalcoholic fatty liver disease (NAFLD) affects up to 30% of the adult population in Western societies, yet the underlying molecular pathways remain poorly understood. Here, we identify the dimeric Activator Protein 1 as a regulator of NAFLD. Fos-related ...

Elsevier2014

Large scale expression and purification of the mouse 5-HT3 receptor

Horst Vogel, Cédric Deluz, Ghérici Hassaïne, Menno Berend Tol

Receptors of the Cys-loop family are central to neurotransmission and primary therapeutic targets. In order to decipher their gating and modulation mechanisms, structural data is essential. However, structural studies require large amounts of pure, functio ...

Elsevier Science Bv2013

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Receptor antagonist

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

Reversible Local and Global Switching in Multicomponent Supramolecular Networks: Controlled Guest Release and Capture at the Solution/Solid Interface

Exploring Weak Ligand-Protein Interactions by Long-Lived NMR States: Improved Contrast in Fragment-Based Drug Screening

Towards a new combination therapy for tuberculosis with next generation benzothiazinones

Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR

Drug concentration prediction and delivery

Mixtures of Chemical Pollutants at European Legislation Safety Concentrations: How Safe Are They?

Chemical Modification of Graphene via Hyperthermal Molecular Reaction

Regulation of Steatohepatitis and PPARγ Signaling by Distinct AP-1 Dimers

Large scale expression and purification of the mouse 5-HT3 receptor

Graph Chatbot

Chat with Graph Search

Towards a new combination therapy for tuberculosis with next generation benzothiazinones

Drug concentration prediction and delivery

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

Reversible Local and Global Switching in Multicomponent Supramolecular Networks: Controlled Guest Release and Capture at the Solution/Solid Interface

Exploring Weak Ligand-Protein Interactions by Long-Lived NMR States: Improved Contrast in Fragment-Based Drug Screening

Mixtures of Chemical Pollutants at European Legislation Safety Concentrations: How Safe Are They?

Regulation of Steatohepatitis and PPARγ Signaling by Distinct AP-1 Dimers

Chemical Modification of Graphene via Hyperthermal Molecular Reaction

Large scale expression and purification of the mouse 5-HT3 receptor

Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR