Concept

Selective receptor modulator

Related publications (13)

Non-invasive stimulation of the human striatum disrupts reinforcement learning of motor skills

Friedhelm Christoph Hummel, Takuya Morishita, Pierre Theopistos Vassiliadis, Elena Beanato, Esra Neufeld, Fabienne Windel, Maximilian Jonas Wessel, Traian Popa, Julie Duqué

Reinforcement feedback can improve motor learning, but the underlying brain mechanisms remain underexplored. In particular, the causal contribution of specific patterns of oscillatory activity within the human striatum is unknown. To address this question, ...

Nature Portfolio2024

Phonon-Driven Selective Modulation of Exciton Oscillator Strengths in Anatase TiO2Nanoparticles

Majed Chergui, Edoardo Baldini, Enrico Pomarico, Thomas Charles Henry Rossi, Malte Oppermann, Tania Palmieri, Gerald Auböck

The way nuclear motion affects electronic responses has become a very hot topic in materials science. Coherent acoustic phonons can dynamically modify optical, magnetic, and mechanical properties at ultrasonic frequencies, with promising applications as se ...

2018

The FDA-approved natural product dihydroergocristine reduces the production of the Alzheimer's disease amyloid-beta peptides

Patrick Fraering, Jianhua Liu, Jing Yu

Known gamma-secretase inhibitors or modulators display an undesirable pharmacokinetic profile and toxicity and have therefore not been successful in clinical trials for Alzheimer's disease (AD). So far, no compounds from natural products have been identifi ...

Nature Publishing Group2015

Potential of Cycloaddition Reactions To Generate Cytotoxic Metal Drugs In Vitro

Paul Joseph Dyson, Sviatlana Siankevich, Benjamin Samuel Murray, Stéphanie Crot

Severe general toxicity issues blight many chemotherapeutics utilized in the treatment of cancers, resulting in the need for more selective drugs able to exert their biological activity at only the required location(s). Toward this aim, we report the devel ...

Amer Chemical Soc2014

Identification of genetic determinants and pharmacological modulators of mitochondrial function

Pénélope Andreux

Increased life expectancy goes hand in hand with a higher incidence of age-related diseases that affect the nervous and metabolic systems, such as type 2 diabetes, cancer, Parkinson’s and Alzheimer’s disease. These complex diseases are a product of the com ...

EPFL2013

The Receptor TGR5 Mediates the Prokinetic Actions of Intestinal Bile Acids and Is Required for Normal Defecation in Mice

Kristina Schoonjans

BACKGROUND & AIMS: Abnormal delivery of bile acids (BAs) to the colon as a result of disease or therapy causes constipation or diarrhea by unknown mechanisms. The G protein-coupled BA receptor TGR5 (or GPBAR1) is expressed by enteric neurons and endocrine ...

W B Saunders Co-Elsevier Inc2013

Balancing bistable perception during self-motion

Olaf Blanke, Michiel van Elk

In two experiments we investigated whether bistable visual perception is influenced by passive own body displacements due to vestibular stimulation. For this we passively rotated our participants around the vertical (yaw) axis while observing different rot ...

Springer2012

Cyclin D1 Enhances the Response to Estrogen and Progesterone by Regulating Progesterone Receptor Expression

Cathrin Brisken

Estrogen and progesterone are the defining hormones of normal female development, and both play critical roles in breast carcinogenesis. Cyclin D1 is a breast cancer oncogene whose amplification is linked to poor prognosis in estrogen and progesterone rece ...

American Society for Microbiology2010

Discovery of 6alpha-Ethyl-23(S)-methylcholic Acid (S-EMCA, INT-777) as a Potent and Selective Agonist for the TGR5 Receptor, a Novel Target for Diabesity

Johan Auwerx, Kristina Schoonjans

In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C(23)(S)-methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic acid (6-ECDCA, INT-747) affords s ...

2009

Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies

Johan Auwerx, Kristina Schoonjans

TGR5, a metabotropic receptor that is G-protein-coupled to the induction of adenylate cyclase, has been recognized as the molecular link connecting bile acids to the control of energy and glucose homeostasis. With the aim of disclosing novel selective modu ...

2008

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