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Amides are ubiquitous molecules in nature and in synthetic chemistry. Here we report a convenient and efficient method to synthesize N-aryl amides via amidation of esters with nitroarenes. In the presence of manganese metal, this amidation proceeded smooth ...
ROYAL SOC CHEMISTRY2019
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In a typical high-throughput drug screening (HTS) process, up to millions of chemical compounds are applied to cells cultured in well plates, aiming to find molecules that exhibit a robust dose-response, as evidenced for example by a fluorescence signal. I ...
Royal Soc Chemistry2017
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 ...
2018
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 ...
Sortases are transpeptidase enzymes that anchor surface proteins, including virulence factors, to the cell wall of Gram-positive bacteria, and they are potential targets for the development of anti-infective agents. While several large compound libraries w ...
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 ...
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 ...
Cyclic peptide ligands are a promising molecular format for the development of therapeutics. They combine some of the advantages of large protein therapeutics (high affinity and specificity) and of small molecule drugs (accessibility to chemical synthesis ...
Screening drugs on patient biopsies from solid tumours has immense potential, but is challenging due to the small amount of available material. To address this, we present here a plug-based microfluidics platform for functional screening of drug combinatio ...
Integer programs (IPs) are one of the fundamental tools used to solve combinatorial problems in theory and practice. Understanding the structure of solutions of IPs is thus helpful to argue about the existence of solutions with a certain simple structure, ...
