NEK kinases in cell cycle regulation, DNA damage response, and cancer progression

Tissue and Cell, Journal Year: 2025, Volume and Issue: 94, P. 102811 - 102811

Published: March 1, 2025

Language: Английский

---

NLRP3 as a therapeutic target in cyclophosphamide-associated toxicities

Molecular Biology Reports, Journal Year: 2025, Volume and Issue: 52(1)

Published: April 7, 2025

Language: Английский

---

Interface-driven structural evolution on diltiazem as novel uPAR inhibitors: from in silico design to in vitro evaluation

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: June 27, 2024

Language: Английский

---

Identification of a covalent NEK7 inhibitor to alleviate NLRP3 inflammasome-driven metainflammation

Cell Communication and Signaling, Journal Year: 2024, Volume and Issue: 22(1)

Published: Nov. 25, 2024

Aberrant activation of NLRP3 inflammasome is associated with a variety inflammatory diseases. Advances in understanding the molecular mechanisms have revealed that NEK7 an essential component for its activation, but development drugs specifically targeting remains challenging. Here we identify rociletinib (ROC), anticancer drug phase III clinical trial high safety profile, as highly potent and specific small-molecule antagonists NEK7. Mechanistically, ROC covalent binds to cysteine 79 through reactive α, β-unsaturated carbonyl group, thereby inhibiting interaction between NEK7, subsequent assembly inflammasome. Furthermore, alleviates pathological features metainflammation on mouse model type 2 diabetes (T2D). In summary, our results inhibitor demonstrates provides potential promising strategy treatment inflammasome-driven T2D.

Language: Английский

---

Exploration De L'Ouverture Du Pyranopyrazole Pour La Synthèse De Dérivés Pyrazoliques: Conception, Synthèse, Amarrage Moléculaire, Simulation Dynamique Moléculaire Et Analyses Dft

Published: Jan. 1, 2024

---