Concept

Mechanism of action

Related publications (51)

Deconvolution of ex-vivo drug screening data and bulk tissue expression predicts the abundance and viability of cancer cell subpopulations

Ex-vivo drug sensitivity screening (DSS) allows the prediction of cancer treatment effectiveness in a personalized fashion. However, it only provides a readout on mixtures of cells, potentially occulting important information on clinically relevant cell su ...

EPFL2024

Toxic Effects of Koumine on the Early-Life Development Stage of Zebrafish

Yao Tian

Koumine is one of the most abundant alkaloids found in Gelsemium elegans, and it has a wide range of pharmacological effects including antitumor, anti-inflammatory, analgesic treatment effects, and antianxiety. However, its high toxicity and unclear mechan ...

Basel2023

Energy transfer and charge transfer between semiconducting nanocrystals and transition metal dichalcogenide monolayers

Michele Ghini

Nowadays, as a result of the emergence of low-dimensional hybrid structures, the scientific community is interested in their interfacial carrier dynamics, including charge transfer and energy transfer. By combining the potential of transition metal dichalc ...

ROYAL SOC CHEMISTRY2023

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Henning Paul-Julius Stahlberg, Dongchun Ni

ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...

NATURE RESEARCH2021

Can Precision Electrophile Signaling Make a Meaningful and Lasting Impression in Drug Design?

Yimon Aye, Amogh Kulkarni

For several years, drugs with reactive electrophilic appendages have been developed. These units typically confer prolonged residence time of the drugs on their protein targets, and may assist targeting shallow binding sites and/or improving the drug-prote ...

WILEY-V C H VERLAG GMBH2021

Synthesis of diphenoxyadamantane alkylamines with pharmacological interest

Stewart Cole, Anthony Vocat

In this work, the synthesis and the pharmacological evaluation of diphenoxyadamantane alkylamines Ia-f and IIa-f is described. The new diphenoxy-substituted adamantanes share structural features present in trypanocidal and antitubercular agents. 1-Methylpi ...

PERGAMON-ELSEVIER SCIENCE LTD2019

Multimodal imaging and high-throughput image-processing for drug screening on living organisms on-chip

Michaël Unser, Johan Auwerx, Martinus Gijs, Matteo Cornaglia, Laurent Mouchiroud, Daniel Migliozzi, Virginie Sophie Uhlmann

A major step for the validation of medical drugs is the screening on whole organisms, which gives the systemic information that is missing when using cellular models. Caenorhabditis elegans is a soil worm that catches the interest of researchers who study ...

2019

Synthesis, biology, computational studies and in vitro controlled release of new isoniazid-based adamantane derivatives

Stewart Cole, Anthony Vocat

Aim: There is a necessity for new drugs to be more efficient than today's standard due to the emergence of drug-resistant strains of Mycobacterium tuberculosis (Mtb) Results/methodology: 12 new isoniazid-based adamantane derivatives were synthesized and te ...

FUTURE SCI LTD2019

Analysis of cellular and drug action mechanisms in the malaria parasites using systems biology approaches

Anush Chiappino-Pepe

Malaria puts at risk of infection half of the world population and still kills around half a million people every year. The rapid and worrisome rise of drug-resistant malaria parasites hinders the treatment of malaria and calls for a global collaboration t ...

EPFL2018

Generation and Characterization of Anti-VGLUT Nanobodies Acting as Inhibitors of Transport

Andrea Volterra

The uptake of glutamate by synaptic vesicles is mediated by vesicular glutamate transporters (VGLUTs). The central role of these transporters in excitatory neurotransmission underpins their importance as pharmacological targets. Although several compounds ...

Amer Chemical Soc2017

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