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A Structural Explanation of the Effects of Dissociated Glucocorticoids on Glucocorticoid Receptor Transactivation
Overall, the findings provide some structural guidelines for the synthesis of potential new dissociated glucocorticoids with a better therapeutic ratio.
Targeting the DNA-binding activity of the human ERG transcription factor using new heterocyclic dithiophene diamidines
Data showed for the first time the ERG/DNA complex modulation, both in vitro and in cells, by a heterocyclic diamidine that specifically targets a portion of the ERg DNA recognition site.
GILZ inhibits the mTORC2/AKT pathway in BCR-ABL+ cells
It is demonstrated that the glucocorticoid-induced leucine zipper protein (GILZ) modulates imatinib and dasatinib resistance and suppresses tumor growth by inactivating the mammalian target of rapamycin complex-2 (mTORC2)/AKT signaling pathway.
A small-molecule P2RX7 activator promotes anti-tumor immune responses and sensitizes lung tumor to immunotherapy
- L. Douguet, Serena Janho Dit Hreich, V. Vouret-Craviari
- Biology, MedicineNature communications
- 28 January 2021
A chemical positive modulator of the purinergic P2RX7 receptor that potentiates αPD-1 treatment to effectively control the growth of lung tumors in transplantable and oncogene-induced mouse models and triggers long lasting antitumor immune responses.
Distinctly Different Dynamics and Kinetics of Two Steroid Receptors at the Same Response Elements in Living Cells
Comparing the recovery half time, binding site occupancy and the resulting temporal changes in transcription upon binding of two closely related steroid receptors, the androgen and glucocorticoid receptors (AR and GR), to their common hormone REs (HREs) is compared.
ZrCl4 as a new catalyst for ester amidation: an efficient synthesis of h-P2X7R antagonists
Enantioseparation of pyroglutamide derivatives on polysaccharide based chiral stationary phases by high-performance liquid chromatography and supercritical fluid chromatography: a comparative study.
Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease.
A dozen pyroglutamide-based P2X7 antagonists were shown to possess improved properties, among which inhibition of YO-PRO-1/TO- PRO-3 uptake and IL1β release upon BzATP activation of the receptor and dampening signs of DSS-induced colitis on mice, in comparison with reference antagonist GSK1370319A.
Discovery of highly functionalized scaffolds: Pyrroloimidazolediones as P2X7 receptor antagonists
Antagonists of the P2X7 receptor: Mechanism of enantioselective recognition using highly sulfated and sulfobutylether cyclodextrins by capillary electrokinetic chromatography
The linearity of the Van't Hoff plot, in the range of 288–303 K leading to negative enthalpy values, showed that the complexation phenomenon is enthalpically controlled and thermodynamically favored.