A5071465414- 14-3-3 protein interactions
- Cancer Treatment and Pharmacology
- Hernia repair and management
- Cell death mechanisms and regulation
- Synthetic Organic Chemistry Methods
- Pelvic floor disorders treatments
- Iron Metabolism and Disorders
- Marine Sponges and Natural Products
- Estrogen and related hormone effects
- Ovarian cancer diagnosis and treatment
- Neuroblastoma Research and Treatments
- Anorectal Disease Treatments and Outcomes
- Genetic factors in colorectal cancer
- Pelvic and Acetabular Injuries
- Synthesis of heterocyclic compounds
- Carbohydrate Chemistry and Synthesis
- Cardiac electrophysiology and arrhythmias
- Signaling Pathways in Disease
- Synthesis and Characterization of Heterocyclic Compounds
- Galectins and Cancer Biology
- Glycosylation and Glycoproteins Research
- Synthesis and Reactions of Organic Compounds
- Chemical Synthesis and Analysis
- Protein Kinase Regulation and GTPase Signaling
- Down syndrome and intellectual disability research
Abu Dhabi University
2021-2024
Centre National de la Recherche Scientifique
2011-2021
Station Biologique de Roscoff
2011-2021
Université Paris Sciences et Lettres
2018
Institut Curie
2018
ManRos Therapeutics (France)
2016-2017
DYRKs (dual specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like are implicated in the onset development of Alzheimer's disease Down syndrome. The marine sponge alkaloid leucettamine B was recently identified as an inhibitor DYRKs/CLKs. Synthesis analogues (leucettines) led to optimized product, leucettine L41. Leucettines were cocrystallized with DYRK1A, DYRK2, CLK3, PIM1, GSK-3β. selectivity L41 studied by activity interaction assays recombinant kinases affinity...
We here report on the synthesis, optimization, and biological characterization of leucettines, a family kinase inhibitors derived from marine sponge leucettamine B. Stepwise synthesis analogues starting natural structure, guided by activity testing eight purified kinases, led to highly potent CLKs DYRKs, two families kinases involved in alternative pre-mRNA splicing Alzheimer's disease/Down syndrome. Leucettine L41 was cocrystallized with CLK3. It interacts key residues located within...
// Sylvie Maubant 1, * , Tania Tahtouh Amélie Brisson 1 Virginie Maire Fariba Némati 2 Bruno Tesson 3 Mengliang Ye Guillem Rigaill 4, 5 Maïté Noizet Aurélie Dumont David Gentien 6 Bérengère Marty-Prouvost Leanne de Koning 7 Sardar Faisal Mahmood Didier Decaudin Francisco Cruzalegui 8 Gordon C. Tucker Sergio Roman-Roman 9 and Thierry Dubois Institut Curie, PSL Research University, Translational Department, Breast Cancer Biology Group, Paris, France Preclinical Investigation Laboratory, INSERM...
The protein kinase DYRK1A is involved in Alzheimer's disease, Down syndrome, diabetes, viral infections, and leukemia. Leucettines, a family of 2-aminoimidazolin-4-ones derived from the marine sponge alkaloid Leucettamine B, have been developed as pharmacological inhibitors DYRKs (dual specificity, tyrosine phosphorylation regulated kinases) CLKs (cdc2-like kinases). We report here on synthesis structure–activity relationship (SAR) 68 Leucettines. Leucettines were tested 11 purified kinases...
<title>Abstract</title> Objective To investigate the relationship between position of anterior mesh, measured by ultrasound through Bladder neck - Mesh Distance technique and surgical outcomes after laparoscopic sacrocolpopexy (SCP) for apical prolapse. Study design: Retrospective analysis prospectively collected data in a tertiary care hospital. Between January 2019 September 2019, 63 women who underwent SCP due to prolapse were included. was immediately surgery. The pelvic floor evaluated...
We here report on leucettines, a family of kinase inhibitors derived from the marine sponge leucettamine B. Stepwise synthesis analogues, followed by activity testing 8 purified kinases led to highly potent CLKs & DYRKs, two families involved in pre-mRNA splicing and Alzheimer's disease. Leucettine L41 was co-crystallized with DYRK1A, -2, CLK3 PIM1. inhibits phosphorylation pre-RNA regulating Ser/Arg-rich proteins. modulates alternative cellular systems. The selectivity extensively...
The "Journées Franco-Belges de Pharmacochimie" is a recognized annual meeting in organic and medicinal chemistry known for the quality of scientific exchange conviviality. Young researchers were encouraged to present their work share ideas with senior scientists. Abstracts plenary lectures, oral communications, posters presented during are collected this report.
Protein kinases catalyze the phosphorylation of proteins, one major mechanisms regulation cell life. Of 518 human kinases, families DYRKS (dual specificity, tyrosine activated kinases) and CLKS (cdc2-like are involved in alternative pre-mRNA splicing Alzheimer's disease/Down syndrome. We here report on synthesis, optimization biological characterization leucettines, a family kinase inhibitors derived from marine sponge natural product Leucettamine B. Stepwise synthesis analogues starting...