PSMA-targeted low-molecular double conjugates for diagnostics and therapy

Eur J Med Chem. 2021 Dec 5:225:113752. doi: 10.1016/j.ejmech.2021.113752. Epub 2021 Aug 8.

Abstract

This review presents data on dual conjugates of therapeutic and diagnostic action for targeted delivery to prostate cancer cells. The works of the last ten years on this topic were analyzed. The mail attention focuses on low-molecular-weight conjugates directed to the prostate-specific membrane antigen (PSMA); the comparison of high and low molecular weight PSMA-targeted conjugates was made. The considered conjugates were divided in the review into two main classes: diagnostic bimodal conjugates (which are containing two fragments for different types of diagnostics), theranostic conjugates (containing both therapeutic and diagnostic agents); also bimodal high molecular weight therapeutic conjugates containing two therapeutic agents are briefly discussed. The data of in vitro and in vivo studies for PSMA-targeted double conjugates available by the beginning of 2021 have been analyzed.

Keywords: Anticancer drugs; Cancer diagnosis; Double conjugates; PSMA; Prostate cancer; Targeted delivery.

Publication types

  • Review

MeSH terms

  • Antigens, Surface / chemistry*
  • Antigens, Surface / metabolism
  • Antineoplastic Combined Chemotherapy Protocols / chemistry*
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Cytostatic Agents / chemistry*
  • Cytostatic Agents / pharmacology
  • Glutamate Carboxypeptidase II / antagonists & inhibitors
  • Glutamate Carboxypeptidase II / chemistry*
  • Glutamate Carboxypeptidase II / metabolism
  • Humans
  • Male
  • Molecular Structure
  • Molecular Weight
  • Prostatic Neoplasms / diagnosis*
  • Prostatic Neoplasms / drug therapy

Substances

  • Antigens, Surface
  • Cytostatic Agents
  • FOLH1 protein, human
  • Glutamate Carboxypeptidase II