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Concept

Drug class

Related publications (15)

Harnessing the Membrane Translocation Properties of AB Toxins for Therapeutic Applications

Françoise Gisou van der Goot Grunberg, Oksana Andrei Sergeeva, Numa Piot

Over the last few decades, proteins and peptides have become increasingly more common as FDA-approved drugs, despite their inefficient delivery due to their inability to cross the plasma membrane. In this context, bacterial two-component systems, termed AB ...

2021

Enhancing the Signaling of GPCRs via Orthosteric Ions

Horst Arthur Vogel, Shuguang Yuan

G protein-coupled receptors play essential roles in cellular processes such as neuronal signaling, vision, olfaction, tasting, and metabolism. As GPCRs are the most important drug targets, understanding their interactions with ligands is of utmost importan ...

AMER CHEMICAL SOC2020

The Investigation of Flory-Huggins Interaction Parameters for Amorphous Solid Dispersion Across the Entire Temperature and Composition Range

Esther Amstad

Amorphous solid dispersion (ASD) is one of the most promising enabling formulations featuring significant water solubility and bioavailability enhancements for biopharmaceutical classification system (BCS) class II and IV drugs. An accurate thermodynamic u ...

2019

Towards Light-Activated Ruthenium-Arene (RAPTA-Type) Prodrug Candidates

Paul Joseph Dyson, Rosario Scopelliti, Patrycja Nowak-Sliwinska, Felix Daniel Bobbink, Anna Katherine Renfrew

Cancer is currently one of the deadliest diseases worldwide. Based on the high incidence of this disease, the side effects associated with current chemotherapies and the appearance of drug resistance, considerable efforts have been directed towards the dev ...

WILEY-V C H VERLAG GMBH2019

Dual-responsive polyphosphazene as a common platform for highly efficient drug self-delivery

For clinical applications, simplicity, high efficiency, and low toxicity are key issues in the design of anti-tumor drugs. In this work, a novel dual-responsive drug self-framed delivery system (DSFDS) with high drug delivery efficiency is proposed based o ...

Royal Society of Chemistry2019

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

Rapid Production of Submicron Drug Substance Particles by Supersonic Spray Drying

Esther Amstad

Many newly developed active pharmaceutical ingredients (APIs) are poorly soluble in water and thus have a dissolution-limited bioavailability. The bioavailability of Biopharmaceutical Classification System (BCS) class II APIs increases if they dissolve fas ...

Amer Chemical Soc2017

Does Proton Conduction in the Voltage-Gated H+ Channel hHv1 Involve Grotthuss-Like Hopping via Acidic Residues?

Ursula Röthlisberger, Siri Camee van Keulen, Lucie Monique Françoise Delemotte

Hv1s are ubiquitous highly selective voltage-gated proton channels involved in male fertility, immunology, and the invasiveness of certain forms of breast cancer. The mechanism of proton extrusion in Hv1 is not yet understood, while it constitutes the firs ...

2016

Development of mass spectrometric methods to understand the mechanism of action of transition metal-based anticancer compounds

Fook Seng Ronald Lee

Metal based anti-cancer drugs (metallodrugs) such as cisplatin are a cornerstone of cancer chemotherapy. However, development of this class of compound has been hindered by our lack of understanding of how they function. This is mainly because existing met ...

EPFL2016

The Molecular Mechanism of P2Y 1 Receptor Activation

Horst Arthur Vogel, Shuguang Yuan

Human purinergic Gprotein-coupled receptor P2Y(1) (P2Y(1)R) is activated by adenosine 5'-diphosphate (ADP) to induce platelet activation and thereby serves as an important antithrombotic drug target. Crystal structures of P2Y(1)R revealed that one ligand ( ...

Wiley-Blackwell2016

Next-generation antimicrobials: from chemical biology to first-in-class drugs

Paul Murima

The global emergence of multi-drug resistant bacteria invokes an urgent and imperative necessity for the identification of novel antimicrobials. The general lack of success in progressing novel chemical entities from target-based drug screens have prompted ...

Pharmaceutical Soc Korea2015

Cognitive Enhancers (Nootropics). Part 3: Drugs Interacting with Targets other than Receptors or Enzymes. Disease-Modifying Drugs. Update 2014

Andrea Pfeifer

Scientists working in the field of Alzheimer's disease and, in particular, cognitive enhancers, are very productive. The review "Drugs interacting with Targets other than Receptors or Enzymes. Disease-modifying Drugs" was accepted in October 2012. In the l ...

Ios Press2014

Detection of Drug-Protein Interactions with an Improved Yeast Three-Hybrid System

Cindy Fellay

The identification of the targets of therapeutic drugs is one of the major challenges for pharmaceutical companies. The main target responsible for drug action is often known, but most drugs also bind other targets, either causing deleterious side effects ...

EPFL2013

Cognitive Enhancers (Nootropics). Part 3: Drugs Interacting with Targets other than Receptors or Enzymes. Disease-modifying Drugs

Andrea Pfeifer

Cognitive enhancers (nootropics) are drugs to treat cognition deficits in patients suffering from Alzheimer's disease, schizophrenia, stroke, attention deficit hyperactivity disorder, or aging. Cognition refers to a capacity for information processing, app ...

Ios Press2013

Endogenous Myc maintains the tumor microenvironment

Douglas Hanahan

The ubiquitous deregulation of Myc in human cancers makes it an intriguing therapeutic target, a notion supported by recent studies in Ras-driven lung tumors showing that inhibiting endogenous Myc triggers ubiquitous tumor regression. However, neither the ...

2011