Related Experiment Video

Updated: Jun 30, 2025

Author Spotlight: A Selective Luciferase-Based Assay for Monitoring ATG4B 27 Activity in Cells
09:51

Author Spotlight: A Selective Luciferase-Based Assay for Monitoring ATG4B 27 Activity in Cells

Published on: June 30, 2023

826

NPS-2143 inhibit glioma progression by suppressing autophagy through mediating AKT-mTOR pathway

Jia-Li Nie1,2, Qi Li1,2, Hai-Tang Yin1,2

  • 1Department of Pharmacy, Affiliated Hospital of Guizhou Medical University, Guiyang, P.R. China.

Journal of Cellular and Molecular Medicine
|March 21, 2024
PubMed

Insights

NPS-2143, a calcium-sensing receptor antagonist, effectively suppresses glioma progression by inhibiting cell proliferation, inducing apoptosis, and blocking autophagy. This compound shows promise as an anti-glioma therapeutic agent.

Area of Science:

  • Neuro-oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Gliomas represent the most prevalent central nervous system tumors.
  • Identifying novel therapeutic compounds and understanding their mechanisms are crucial for effective glioma treatment.

Purpose of the Study:

  • To discover a potent anti-glioma compound.
  • To elucidate the molecular mechanisms underlying its anti-glioma effects.

Main Methods:

  • Cytotoxicity screening of 50 compounds on glioma cells using CCK-8 assay.
  • Investigated cell cycle, apoptosis, migration, invasion, and autophagy.
  • Utilized bioinformatic analysis and a nude mice xenograft model.

Main Results:

  • NPS-2143, a calcium-sensing receptor (CASR) antagonist, exhibited potent cytotoxicity against glioma cells.
  • NPS-2143 inhibited proliferation, induced G1 cell cycle arrest and apoptosis, and reduced migration/invasion.
  • NPS-2143 suppressed autophagy via the AKT-mTOR pathway and demonstrated in vivo tumor suppression.

Conclusions:

  • NPS-2143 effectively suppresses glioma progression by inhibiting autophagy.
  • CASR expression levels correlate with glioma patient prognosis, suggesting CASR as a potential therapeutic target.
Keywords:
GSEANPS‐2143autophagychemotherapyglioma

More Related Videos

Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment11:13

Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment

Published on: June 9, 2023

1.5K
Coculture Assays to Study Macrophage and Microglia Stimulation of Glioblastoma Invasion09:23

Coculture Assays to Study Macrophage and Microglia Stimulation of Glioblastoma Invasion

Published on: October 20, 2016

14.0K

Related Concept Videos

PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a...
3.5K
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
3.8K
Abnormal Proliferation02:23

Abnormal Proliferation

Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the...
4.5K
Interactions Between Signaling Pathways01:19

Interactions Between Signaling Pathways

Signaling cascades usually lack linearity. Multiple pathways interact and regulate one another, allowing cells to integrate and respond to diverse environmental stimuli.
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...
6.3K
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.0K
The JAK-STAT Signaling Pathway01:20

The JAK-STAT Signaling Pathway

Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as  SH2...
8.9K