Publication

Phage selection of peptide macrocycles against b-catenin to interfere with Wnt signaling

Publications associées (30)

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

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 GMBH2022

The E protein-TCF1 axis controls gamma delta T cell development and effector fate

Freddy Radtke

TCF1 plays a critical role in T lineage commitment and the development of alpha beta lineage T cells, but its role in gamma delta T cell development remains poorly understood. Here, we reveal a regulatory axis where T cell receptor (TCR) signaling controls ...

2021

Reprogramming G Protein-Coupled Receptor Structure, Function And Signaling By Computational Design

Dániel Kéri

G protein-coupled receptors (GPCRs) are 7-transmembrane alpha-helical integral membrane proteins on which cells heavily rely to receive information regarding their external environment. These receptors are able to transfer information to intracellular down ...

EPFL2021

Evolutionary history expands the range of signaling interactions in hybrid multikinase networks

Mohamed Barakat, Anne-Florence Raphaëlle Bitbol

Two-component systems (TCSs) are ubiquitous signaling pathways, typically comprising a sensory histidine kinase (HK) and a response regulator, which communicate via intermolecular kinase-to-receiver domain phosphotransfer. Hybrid HKs constitute non-canonic ...

NATURE RESEARCH2021

Wnt5a promotes hippocampal postsynaptic development and GluN2B-induced expression via the eIF2 alpha HRI kinase

Eva Ramos Fernandez

Wnt signaling plays a key role in neurodevelopment and neuronal maturation. Specifically, Wnt5a stimulates postsynaptic assemblies, increases glutamatergic neurotransmission and, through calcium signaling, generates nitric oxide (NO). Trying to unveil the ...

Nature Research2021

An Oculus to Profile and Probe Target Engagement In Vivo: How T-REX Was Born and Its Evolution into G-REX

Chloé Rogg, Yimon Aye

Here we provide a personal account of innovation and design principles underpinning a method to interrogate precision electrophile signaling that has come to be known as "REX technologies". This Account is framed in the context of trying to improve methods ...

AMER CHEMICAL SOC2021

TBX3 acts as tissue-specific component of the Wnt/beta-catenin transcriptional complex

Michel Aguet, Andreas Eduard Moor

BCL9 and PYGO are beta-catenin cofactors that enhance the transcription of Wnt target genes. They have been proposed as therapeutic targets to diminish Wnt signaling output in intestinal malignancies. Here we find that, in colorectal cancer cells and in de ...

2020

Targeting the oncogenic signaling of the transcription factor STAT3 with potent and selective monobody inhibitors

Grégory La Sala

Many targeted cancer therapies fail to improve the overall survival of patients. Limitations involve low drug selectivity and the rapid development of resistance. Moreover, the majority of oncogenic drivers presently remain considered as undruggable as th ...

EPFL2020

Antiangiogenic immunotherapy suppresses desmoplastic and chemoresistant intestinal tumors in mice

Matthias Lütolf, Mauro Delorenzi, Laureline Wetterwald, Sina Nassiri, Michele De Palma, Mario Leonardo Squadrito, Nikolche Gjorevski, Alan Nicolas Thierry Guichard, Simone Ragusa, Borja Prat Luri

Mutations in APC promote colorectal cancer (CRC) progression through uncontrolled WNT signaling. Patients with desmoplastic CRC have a significantly worse prognosis and do not benefit from chemotherapy, but the mechanisms underlying the differential respon ...

2020

Multi-color Molecular Visualization of Signaling Proteins Reveals How C-Terminal Src Kinase Nanoclusters Regulate T Cell Receptor Activation

Juliette Griffie

Elucidating the mechanisms that controlled T cell activation requires visualization of the spatial organization of multiple proteins on the submicron scale. Here, we use stoichiometrically accurate, multiplexed, single-molecule super-resolution microscopy ...

CELL PRESS2020