MYCN acts as a direct co-regulator of p53 in MYCN amplified neuroblastoma

Saurabh Agarwal1, Giorgio Milazzo2, Kimal Rajapakshe3

  • 1Division of Hematology-Oncology, Department of Pediatrics, Baylor College of Medicine, Houston, Texas, USA.

Oncotarget
|May 15, 2018
PubMed

Insights

MYCN oncogenes directly bind to p53 in neuroblastoma, altering gene expression and promoting tumor growth. Targeting this interaction may improve chemotherapy effectiveness for high-risk neuroblastoma.

Area of Science:

  • Oncology
  • Molecular Biology
  • Genetics

Background:

  • MYC oncogenes and p53 play crucial roles in development and cancer.
  • MYCN amplification is common in high-risk neuroblastoma, but its impact on p53 function is unclear.
  • Neuroblastoma typically has wild-type p53, requiring p53 signaling repression for tumor development.

Purpose of the Study:

  • To investigate how MYCN amplification affects p53 transcriptional activity in neuroblastoma.
  • To elucidate the molecular mechanisms underlying MYCN's role in neuroblastoma tumorigenesis.

Main Methods:

  • Tested MYCN's direct binding to p53 using biochemical assays.
  • Analyzed MYCN-p53 co-localization at target gene promoters via chromatin analysis.
  • Quantified gene expression changes using RNA sequencing.

Main Results:

  • MYCN directly binds to the C-terminal domain of tetrameric p53, independent of MYCN/MAX heterodimers.
  • MYCN-p53 complex co-localizes at p53 response elements and E-boxes, modulating expression of DNA damage and cell cycle genes.
  • MYCN-p53 interaction regulates novel p53 targets involved in lipid metabolism, DNA repair, and apoptosis.

Conclusions:

  • MYCN acts as a transcriptional co-regulator of p53 in MYCN-amplified neuroblastoma, representing a novel oncogenic function.
  • Targeting the MYCN-p53 interaction could enhance p53-mediated responses and sensitize tumors to chemotherapy.

Related Concept Videos

Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
1.9K
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

Direct-Acting Cholinergic Agonists: Therapeutic Uses

Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren...
1.8K
Adrenergic Agonists: Direct-Acting Agents01:30

Adrenergic Agonists: Direct-Acting Agents

Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine.
These agents can be classified...
2.9K
Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...
2.4K
Negative Regulator Molecules01:23

Negative Regulator Molecules

Positive regulators allow a cell to advance through cell cycle checkpoints. Negative regulators have an equally important role as they terminate a cell’s progression through the cell cycle—or pause it—until the cell meets specific criteria.
38.6K
Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
These groups modify specific amino acids in a protein....
9.7K