18 Papers
63 Citations
Pascal Dao is an academic researcher from Centre national de la recherche scientifique. The author has contributed to research in topics: Chemistry & Focal adhesion. The author has an hindex of 10, co-authored 17 publications. Previous affiliations of Pascal Dao include Paris Descartes University.
Chat about Author
Papers
Design, synthesis, and evaluation of novel imidazo[1,2-a][1,3,5]triazines and their derivatives as focal adhesion kinase inhibitors with antitumor activity.
Pascal Dao,Nikaïa Smith,Céline Tomkiewicz-Raulet,Expédite Yen-Pon,Marta Camacho-Artacho,Daniel Lietha,Jean-Phillipe Herbeuval,Xavier Coumoul,Christiane Garbay,Huixiong Chen,Huixiong Chen +10 more
TL;DR: Investigation demonstrated that these compounds strongly inhibited cell-matrix adhesion, migration, and invasion of U87-MG cells, and the best inhibitor showed IC50 value of 50 nM against FAK enzymatic activity.
58
Synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity
Pascal Dao,Rafika Jarray,Johanne Le Coq,Daniel Lietha,Ali Loukaci,Yves Lepelletier,Réda Hadj-Slimane,Christiane Garbay,Françoise Raynaud,Huixiong Chen,Huixiong Chen +10 more
TL;DR: The synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK (focal adhesion kinase) inhibitors and the evaluation of their anti-angiogenic activity on HUVEC cells revealed that the mode of interaction with the FAK kinase domain is highly similar to that observed in the complex of TAE-226.
57
Synthesis of novel 1,2,4-triazine scaffold as FAK inhibitors with antitumor activity.
TL;DR: A series of new compounds containing a 1,2,4-triazine core as novel scaffold for FAK inhibitors displayed 10-7M IC50 values, and the best one showed IC50 value of 0.23μM against FAK enzymatic activity.
48
Development of highly sensitive fluorescent probes for the detection of β-galactosidase activity – application to the real-time monitoring of senescence in live cells
TL;DR: βGal-1 exhibited an extremely fast response and over 200-fold fluorescence enhancement following the enzymatic cleavage of the β-d-galactopyranoside unit, which allowed the detection of senescence-associated β-Galactosidase (SA-β-gal) activity; a widely used biomarker ofsenescence.
Design, Synthesis, and Biological Evaluation of Covalent Inhibitors of Focal Adhesion Kinase (FAK) against Human Malignant Glioblastoma
Bo Li,Yongliang Li,Céline Tomkiewicz-Raulet,Pascal Dao,Daniel Lietha,Expédite Yen-Pon,Zhiyun Du,Xavier Coumoul,Christiane Garbay,Mélanie Etheve-Quelquejeu,Huixiong Chen +10 more
TL;DR: The structure-guided development of a series of covalent inhibitors of FAK showed highly potent inhibitory potency against FAK enzymatic activity with IC50 values in the nanomolar range, and demonstrated that these inhibitors may have the potential to offer a promising new targeted therapy for human glioblastomas.
32