Tubulin Maytansine Site Binding Ligands and their Applications as MTAs and ADCs for Cancer Therapy

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Shuo Cao1, Yue-Hui Dong2, De-Feng Wang1

  • 1Department of Medicinal Chemistry, Faculty of Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

Current Medicinal Chemistry
|March 17, 2020
PubMed
Abstract

Insights

Maytansine site binding agents are potent Microtubule Targeting Agents (MTAs) for cancer chemotherapy. Antibody-Drug Conjugates (ADCs) using these agents show promise in targeted cancer therapy with improved selectivity and reduced side effects.

Area of Science:

  • Oncology
  • Pharmacology
  • Biochemistry

Background:

  • Microtubule Targeting Agents (MTAs) are crucial in cancer chemotherapy, disrupting tubulin dynamics to inhibit cell growth and induce apoptosis.
  • Maytansine site binding agents, a class of MTAs, are natural products that inhibit tubulin polymerization, showing significant antitumor activity.
  • These agents are utilized in Antibody-Drug Conjugates (ADCs) for targeted cancer treatment.

Purpose of the Study:

  • To review the role of Microtubule Targeting Agents (MTAs) in cancer chemotherapy.
  • To introduce maytansine, its binding site, and related ligands as potent MTAs.
  • To discuss the application of these ligands in Antibody-Drug Conjugates (ADCs) for cancer therapy.

Main Methods:

  • A literature search was conducted using SciFinder® to identify publications on maytansine, its derivatives, binding site, and applications as MTAs.
  • Publications were excluded if they were patents.
  • Recent clinical trial progress was gathered from clinical trial websites.

Main Results:

  • The article provides an overview of MTAs, focusing on maytansine and its binding site ligands.
  • It details the application of these ligands as MTAs and in ADCs for cancer therapy.
  • The review highlights the effectiveness of maytansine site binding agents in preclinical and clinical settings.

Conclusions:

  • Maytansine site binding agents are effective MTAs for cancer chemotherapy.
  • Maytansine site ligand-based ADCs are employed in clinical settings or trials for targeted cancer therapy, enhancing selectivity and reducing side effects.
  • Improving ADC delivery efficiency is crucial for patient benefit in targeted cancer therapy.
Keywords:
Microtubule targeting agentsantibody-drug conjugatesmaytansine binding siteplocabulinrhizoxintrastuzumab emtansine

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