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Endoscopic Endonasal Trans-sphenoidal Approach: Minimally Invasive Surgery for Pituitary Adenomas
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BRD4 as a therapeutic target for nonfunctioning and growth hormone pituitary adenoma

Chengzhang Shi1,2,3,4, Zhao Ye1,2,3,4, Jie Han5

  • 1Department of Neurosurgery, Huashan Hospital, Shanghai Medical College, Fudan University, Shanghai, China.

Neuro-Oncology
|April 5, 2020
PubMed
Abstract

Insights

Bromodomain-containing protein 4 (BRD4) is overexpressed in nonfunctioning and growth hormone pituitary adenomas. BRD4 inhibitors show promise in treating these pituitary tumors by reducing cell proliferation.

Area of Science:

  • Endocrinology
  • Oncology
  • Molecular Biology

Background:

  • Nonfunctioning pituitary adenoma (NFPA) and growth hormone pituitary adenoma (GHPA) are common pituitary adenomas (PAs).
  • Current treatments like surgical resection have limitations, and effective medical therapies are scarce.
  • Novel therapeutic targets are urgently needed for PA treatment.

Purpose of the Study:

  • To investigate the pathological role of Bromodomain-containing protein 4 (BRD4) in NFPA and GHPA.
  • To evaluate the efficacy of BRD4 inhibitors as a potential treatment for NFPA and GHPA.

Main Methods:

  • Detected BRD4 expression in PA tissues and cell lines using immunohistochemistry and real-time PCR.
  • Assessed BRD4 inhibitor efficacy in vitro (cell lines, patient-derived cells) and in vivo (mouse xenografts).
  • Investigated effects on cell cycle, apoptosis, and downstream gene expression via western blots and flow cytometry.

Main Results:

  • BRD4 was found to be overexpressed in NFPA and GHPA tissues.
  • The BRD4 inhibitor ZBC-260 significantly inhibited PA cell proliferation in vitro and in vivo.
  • ZBC-260 downregulated key oncogenes like c-Myc and Bcl2, crucial for pituitary tumorigenesis.

Conclusions:

  • BRD4 is pathologically overexpressed in NFPA and GHPA.
  • BRD4 inhibitors demonstrate significant anti-proliferative effects on PA cells.
  • BRD4 represents a promising therapeutic target for treating NFPA and GHPA.
Keywords:
BRD4GHPANFPAZBC-260target

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