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Inhibitor-conjugated harmonic nanoparticles targeting fibroblast activation protein

Publications associées (30)

AMP-activated Protein Kinase (AMPK): New molecular insights and novel downstream targets

AMP-activated Protein Kinase (AMPK) is a central regulator of energy homeostasis and a promising drug target for metabolic disorders. It exists as complexes of three subunits, a catalytic alpha, and two regulatory beta and gamma subunits. The regulation of ...

EPFL2022

Protein Engineering for Personalized therapy and diagnosis

Lixia Wei

Protein Engineering, especially protein post-translational modification (PTM), ex-tends proteomes in a more complex way than one can expect from analysis of their encod-ing genomes. It can activate or deactivate certain catalytic functions, add new desired ...

EPFL2022

Regulation of Src tumor activity by its N-terminal intrinsically disordered region

Florence Armand, Romain Hamelin

The membrane-anchored Src tyrosine kinase is involved in numerous pathways and its deregulation is involved in human cancer. Our knowledge on Src regulation relies on crystallography, which revealed intramolecular interactions to control active Src conform ...

SPRINGERNATURE2022

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

Apelin-13 Protects Corpus Cavernosum Against Fibrosis Induced by High-Fat Diet in an MMP-Dependent Mechanism

Nikolaos Stergiopoulos, Rafaela Fernandes Da Silva, Mikaël Nils Sturny, Fabiana Pereira Da Costa Fraga, Léa Liliane Colette Anguenot, Maiia Bragina, Augusto Martins Lima

Background: An increased fibrosis of the corpora cavernosa is a prevalent process that underlies most cases of erectile dysfunction. Apelin, an endogenous circulating peptide, has been documented as an important effector on cardiovascular homeostasis, cont ...

ELSEVIER SCI LTD2021

Metabolic and transcriptomic profiles of glioblastoma invasion revealed by comparisons between patients and corresponding orthotopic xenografts in mice

Lijing Xin, Cristina Ramona Cudalbu, Mario Gaetano Lepore, Marta Lai

The invasive behavior of glioblastoma, the most aggressive primary brain tumor, is considered highly relevant for tumor recurrence. However, the invasion zone is difficult to visualize by Magnetic Resonance Imaging (MRI) and is protected by the blood brain ...

2021

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

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

Cell-autonomous inflammation of BRCA1-deficient ovarian cancers drives both tumor-intrinsic immunoreactivity and immune resistance via STING

Christian Iseli, Julien Dorier, Mauro Delorenzi, Alizée Jéléna Grimm, Marco Mina, George Coukos, Alexandre Harari, Giovanni Ciriello

In this study, we investigate mechanisms leading to inflammation and immunoreactivity in ovarian tumors with homologous recombination deficiency (HRD). BRCA1 loss is found to lead to transcriptional reprogramming in tumor cells and cell-intrinsic inflammat ...

2021

Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist

Henning Paul-Julius Stahlberg, Nicolas Calo, Polina Isaikina

The human CC chemokine receptor 5 (CCR5) is a G protein-coupled receptor (GPCR) that plays a major role in inflammation and is involved in cancer, HIV, and COVID-19. Despite its importance as a drug target, the molecular activation mechanism of CCR5, i.e., ...

AMER ASSOC ADVANCEMENT SCIENCE2021