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Transfer of Manipulated Tumor-associated Neutrophils into Tumor-Bearing Mice to Study their Angiogenic Potential In Vivo
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Targeting neurokinin-3 receptor: a novel anti-angiogenesis strategy for cancer treatment

Ting Wang1, Siwei Chen1, Shihui Wang1

  • 1School of Life Science, Zhengzhou University, Zhengzhou, 450001, P.R. China.

Oncotarget
|May 11, 2017
PubMed

Insights

Neurokinin receptor 3 (NK3R) agonists show anti-angiogenesis effects. Novel NK3R-A1 and NK3R-A2 analogues demonstrated potent anti-tumor activity with minimal side effects, suggesting NK3R as a promising cancer therapy target.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Angiogenesis is crucial for tumor growth and metastasis.
  • Current anti-angiogenic drugs have severe side effects, necessitating new therapeutic targets.
  • Neurokinin receptors (NK3R) are implicated in various physiological functions and are potential drug targets.

Purpose of the Study:

  • To investigate the anti-angiogenic effects mediated by neurokinin-3 receptor (NK3R).
  • To design and synthesize novel NK3R agonists with enhanced anti-angiogenic and anti-tumor properties.
  • To evaluate the efficacy and safety of these novel compounds in preclinical models.

Main Methods:

  • Synthesis and characterization of novel NK3R agonists, NK3R-A1 and NK3R-A2, incorporating a tumor angiogenesis homing sequence (NGR).
  • In vitro assessment of anti-migration effects on human umbilical vein endothelial cells (HUVECs) via NK3R activation.
  • In vivo evaluation of antitumor activity and side effects in relevant animal models.

Main Results:

  • A Neurokinin B (NKB) analogue, [Mephe7]NKB, demonstrated significant anti-angiogenic effects.
  • NK3R-A1 and NK3R-A2 exhibited enhanced anti-migration activity in HUVECs.
  • Both novel analogues displayed potent antitumor activity in vivo with no significant observed side effects.

Conclusions:

  • NK3R represents a potential novel target for anti-angiogenesis cancer therapy.
  • NK3R-A1 serves as a promising template for developing new anti-tumor drugs based on anti-angiogenesis strategies.
  • Targeting NK3R offers a potential pathway for developing effective cancer treatments with improved safety profiles.
Keywords:
anti-angiogenesisantitumor therapyneurokinin 3 receptorneurokinin B

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