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Isoprenyl carboxyl methyltransferase inhibitors: a brief review including recent patents

Woo Seok Yang1, Seung-Gu Yeo2, Sungjae Yang1

  • 1Department of Genetic Engineering, Sungkyunkwan University, 2066 Seobu-ro, Jang-gu, Suwon, 16419, Republic of Korea.

Amino Acids
|June 21, 2017
PubMed

Insights

Inhibitors of isoprenyl carboxyl methyltransferase (ICMT) show promise as anti-cancer drugs by targeting Ras signaling. Further research is needed to optimize these ICMT inhibitors for clinical use.

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Oncology

Background:

  • Isoprenyl carboxyl methyltransferase (ICMT) is a key enzyme in the post-translational modification of Ras proteins.
  • Ras signaling pathway dysregulation is implicated in various cancers.
  • ICMT inhibition has demonstrated anti-cancer activity in preclinical studies.

Purpose of the Study:

  • To review patents and research articles (2009-2016) on ICMT inhibitors as potential chemotherapeutic agents.
  • To explore the development of novel anti-cancer drugs targeting Ras-related cancers via ICMT modulation.
  • To identify key chemical scaffolds and optimization strategies for ICMT inhibitors.

Main Methods:

  • Literature review of patents and research articles.
  • High-throughput screening for small-molecular ICMT inhibitors.
  • Chemical optimization of lead compounds.

Main Results:

  • Indole-based small-molecular ICMT inhibitors have been identified.
  • Cysmethynil is a prototypical ICMT inhibitor identified by Duke University researchers.
  • More potent analogs of cysmethynil were patented by Singapore University researchers.
  • Alternative non-indole based ICMT inhibitors were developed by researchers at Universidad Complutense De Madrid and Cancer Therapeutics CRC PTY Ltd.

Conclusions:

  • ICMT inhibitors represent a promising new class of anti-cancer drugs targeting Ras-related cancers.
  • Further chemical optimization is required to enhance drug-like properties (solubility, efficacy, safety) for clinical application.
  • Targeting functional groups in ICMT inhibitors is crucial for improving their therapeutic potential.
Keywords:
CancerCysmethynilICMT inhibitorMethylationRas

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