Concept

Sirolimus

Related publications (25)

Everolimus for Children With Recurrent or Progressive Low-Grade Glioma: Results From the Phase II PNOC001 Trial

PURPOSE The PNOC001 phase II single-arm trial sought to estimate progression-free survival (PFS) associated with everolimus therapy for progressive/recurrent pediatric low-grade glioma (pLGG) on the basis of phosphatidylinositol 3-kinase (PI3K)/AKT/mammali ...

2023

Generating macrocyclic inhibitors of protein-protein interactions

Gontran Sangouard

Protein-protein interactions (PPIs) play important roles in many diseases and their modulation is an attractive strategy for developing new therapeutics. However, the relatively large and often flat binding surfaces of PPIs makes the development of inhibit ...

EPFL2022

Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale

Christian Heinis, Gerardo Turcatti, Julien Bortoli Chapalay, Alessandro Angelini, Manuel Leonardo Merz, Sevan Mleh Habeshian, Jonathan Patrice Vesin, Mischa Schüttel, Ganesh Kumar Mothukuri, Gontran Sangouard, Cristina Diaz Perlas, Zsolt Bognár

Macrocycles have excellent potential as therapeutics due to their ability to bind challenging targets. However, generating macrocycles against new targets is hindered by a lack of large macrocycle libraries for high-throughput screening. To overcome this, ...

2022

Akt Is S-Palmitoylated: A New Layer of Regulation for Akt

Françoise Gisou van der Goot Grunberg, Laurence Gouzi Abrami

The protein kinase Akt/PKB participates in a great variety of processes, including translation, cell proliferation and survival, as well as malignant transformation and viral infection. In the last few years, novel Akt posttranslational modifications have ...

FRONTIERS MEDIA SA2021

Endothelial Calcineurin Signaling Restrains Metastatic Outgrowth by Regulating Bmp2

Nadine Fournier, Mauro Delorenzi, Sina Nassiri, Borja Prat Luri, Laureline Wetterwald

Calcineurin/NFAT signaling is active in endothelial cells and is proposed to be an essential component of the tumor angiogenic response. Here, we investigated the role of endothelial calcineurin signaling in vivo in physiological and pathological angiogene ...

CELL PRESS2019

Applying a Trojan Horse Strategy to Ruthenium Complexes in the Pursuit of Novel Antibacterial Agents

Paul Joseph Dyson, Lucinda Kate Batchelor, Quentin François Antoine Laurent

Siderophores are iron chelators secreted by bacteria to scavenge iron(III) from their surrounding environment. They possess their own internalization pathway that is sufficiently unselective to be hijacked, making them suitable for Trojan Horse strategy ap ...

2018

Genetic and epigenetic inactivation of SESTRIN1 controls mTORC1 and response to EZH2 inhibition in follicular lymphoma

Elisa Oricchio, Natalya Katanayeva, Elena Battistello, Stephanie Jocelyne Sungalee, Maria Christine Donaldson, Giovanni Ciriello

Follicular lymphoma (FL) is an incurable form of B cell lymphoma. Genomic studies have cataloged common genetic lesions in FL such as translocation t(14;18), frequent losses of chromosome 6q, and mutations in epigenetic regulators such as EZH2 Using a focu ...

American Association for the Advancement of Science2017

Acidic tumor microenvironment abrogates the efficacy of mTORC1 inhibitors

Anne Planche, Tania Santoro

Background: Blocking the mechanistic target of rapamycin complex-1 (mTORC1) with chemical inhibitors such as rapamycin has shown limited clinical efficacy in cancer. The tumor microenvironment is characterized by an acidic pH which interferes with cancer t ...

Biomed Central Ltd2016

Injectable cryogel-based whole-cell cancer vaccines

Thomas Michael Braschler, Sidi Ahmed Bencherif

A biomaterial-based vaccination system that uses minimal extracorporeal manipulation could provide in situ enhancement of dendritic cell (DC) numbers, a physical space where DCs interface with transplanted tumour cells, and an immunogenic context. Here we ...

Nature Publishing Group2015

Acute systemic rapamycin induces neurobehavioral alterations in rats

Raphaël Doenlen

Rapamycin is a drug with antiproliferative and immunosuppressive properties, widely used for prevention of acute graft rejection and cancer therapy. It specifically inhibits the activity of the mammalian target of rapamycin (mTOR), a protein kinase known t ...

Elsevier Science Bv2014

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