Pharmaceutical applications of cyclotides

Drug Discov Today. 2019 Nov;24(11):2152-2161. doi: 10.1016/j.drudis.2019.09.010. Epub 2019 Sep 18.

Abstract

Cyclotides are cyclic peptides, present in several plant families, that show diverse biological properties. Structurally, cyclotides share a distinctive head-to-tail circular knotted topology of three disulfide bonds. This framework provides cyclotides with extraordinary resistance to thermal and chemical denaturation. There is increasing interest in the therapeutic potential of cyclotides, which combine several promising pharmaceutical properties, including binding affinity, target selectivity, and low toxicity towards healthy mammalian cells. Recently, cyclotides have been reported to be orally bioavailable and have proved to be amenable to modifications. Here, we provide an overview of the structure, properties, and pharmaceutical applications of cyclotides.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Computer Simulation
  • Cyclotides* / chemical synthesis
  • Cyclotides* / isolation & purification
  • Cyclotides* / pharmacology
  • Databases, Factual
  • Drug Discovery / methods*
  • Humans
  • Plants / chemistry

Substances

  • Cyclotides