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Regulation of Angiogenesis and Blood Supply01:24

Regulation of Angiogenesis and Blood Supply

Rapidly dividing tumors, embryos, and wounded tissues require more oxygen than usual, lowering the oxygen concentration in the blood. At low oxygen or hypoxic conditions, an oxygen-sensitive transcription factor called the hypoxia-inducible factor 1 or HIF1 is activated. HIF1 is a dimeric protein of alpha (ɑ) and beta (β) subunits.  Under optimal oxygen conditions, HIF1β is present in the nucleus while HIF1ɑ remains in the cytosol. HIF1ɑ is hydroxylated by prolyl hydroxylase and factor...
Mechanism of Angiogenesis01:10

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Blood vessel formation starts early during embryonic development, around day 7. In the extraembryonic yolk sac, mesodermal precursor cells called hemangioblast proliferate and differentiate into angioblast. Angioblasts express vascular endothelial growth factor receptor 2 or VEGFR2, which binds VEGF-A, a proangiogenic factor, guiding blood vessel formation. VEGF signaling promotes angioblasts to form a blood island in the developing embryo. Angioblasts further differentiate, giving rise to...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
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Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...
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Related Experiment Video

Updated: Jun 20, 2026

Modified In Vivo Matrix Gel Plug Assay for Angiogenesis Studies
09:03

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Published on: June 30, 2023

Endostatin derivative angiogenesis inhibitors.

Meng-jie Zheng1

  • 1Department of New Drug R&D, Jiangsu Simcere Pharmaceutical R&D Co., Ltd., Jiangsu, China. zhengmengjie@simcere.com

Chinese Medical Journal
|September 29, 2009
PubMed
Summary

Modified endostatin (ES) derivatives show enhanced anti-angiogenesis and anti-tumor activities. These novel ES molecular structures offer improved clinical relevance for future cancer therapeutic strategies.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Endostatin (ES) is a potent anti-angiogenesis factor.
  • Modifying ES molecular structure is crucial for enhancing its therapeutic efficacy.
  • Clinical application of native ES is limited by its short circulation half-life.

Purpose of the Study:

  • To review recent advancements in endostatin (ES) molecular structure modification.
  • To highlight the superior anti-angiogenesis activity of modified ES derivatives.
  • To assess the potential of novel ES derivatives in cancer therapy.

Main Methods:

  • Literature review of PubMed articles (1971-May 2008).
  • Search terms: "endostatin" and "angiogenesis".
  • Selection of articles on ES molecular structure modification and milestone studies.

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Main Results:

  • Modified ES derivatives with polyethylene glycol (PEG), low molecular weight heparin (LMWH), and IgG Fc domains demonstrated extended circulation half-life.
  • Recombinant ES variants exhibited more potent anti-tumor activity than native ES in mouse xenograft models.
  • Mutations in ES altered its anti-angiogenesis properties, suggesting tunable activity.

Conclusions:

  • Anti-angiogenesis therapy remains a promising strategy for tumor treatment.
  • Novel endostatin (ES) derivatives present a viable option for overcoming challenges in clinical ES application.
  • Further development of modified ES holds significant potential for effective cancer therapeutics.