ID-Checker Technology for the Highly Selective Macroscale Delivery of Anticancer Agents to the Cancer Cells

J Med Chem. 2022 Oct 13;65(19):12883-12894. doi: 10.1021/acs.jmedchem.2c00646. Epub 2022 Oct 4.

Abstract

Cancer cells deploy several glucose transport protein (GLUT) channels on the cell membranes to increase glucose uptake. Cancer cells die within 24 h in the absence of glucose. Thus, preventing the deployment of GLUT channels can deprive them of glucose, resulting in apoptosis within 24 h. Herein, we developed the ID-Checker with a glucose tag that ensures its highly specific macroscale delivery of anticancer agents to the cancer cells through the GLUT channels. ID-Checker presented here showed IC50 values of 0.17-0.27 and 3.34 μM in cancer and normal cell lines, respectively. ID-Checker showed a selectivity index of 12.5-20.2, which is about 10-20 times higher than that of known anticancer agents such as colchicine. ID-Checker inhibits the microtubule formation, which results in the prevention of the deployment of GLUT channels in 6 h and kills the cancer cells within 24 h without any damage to normal cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Colchicine
  • Glucose / metabolism
  • Glucose Transport Proteins, Facilitative / metabolism
  • Glucose Transporter Type 1
  • Neoplasms* / drug therapy
  • Technology

Substances

  • Antineoplastic Agents
  • Glucose Transport Proteins, Facilitative
  • Glucose Transporter Type 1
  • Glucose
  • Colchicine