New tricks for human farnesyltransferase inhibitor: cancer and beyond

Jingyuan Wang1, Xue Yao1, Jin Huang1

  • 1Shanghai Key Laboratory of New Drug Design , School of Pharmacy , East China University of Science and Technology , 130 Mei Long Road , Shanghai 200237 , China . Email: huangjin@ecust.edu.cn ; Tel: (+86)21 64253681.

Medchemcomm
|August 16, 2018
PubMed

Insights

Human protein farnesyltransferase (FTase) inhibitors are explored as anti-cancer agents by disrupting Ras protein farnesylation. FTIs also show therapeutic potential for diseases beyond cancer, including progeria and cardiovascular conditions.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Human protein farnesyltransferase (FTase) modifies proteins, including Ras superfamily members, via farnesylation.
  • Ras protein farnesylation is crucial for normal function and oncogenic transformation.
  • FTase substrates are implicated in various diseases like Hutchinson-Gilford progeria syndrome, chronic hepatitis D, and cardiovascular diseases.

Purpose of the Study:

  • To review the multifaceted roles of FTase in cancer progression.
  • To summarize the clinical advancements of FTase inhibitors (FTIs) in oncology.
  • To discuss the therapeutic potential of FTIs for non-cancerous human diseases.

Main Methods:

  • Literature review of FTase function and FTIs.
  • Analysis of FTase's role in tumor cell malignant transformation, proliferation, apoptosis, angiogenesis, and metastasis.
  • Examination of clinical trial data and research on FTIs for various diseases.

Main Results:

  • FTase plays significant roles in key cancer processes.
  • Several FTIs have advanced into cancer clinical trials.
  • FTIs demonstrate promise for treating conditions beyond cancer.

Conclusions:

  • FTase is a critical target in cancer therapy.
  • FTIs represent a promising therapeutic strategy for both oncological and non-oncological diseases.
  • Further research into FTIs could expand their clinical applications.

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