Designed Parasite-Selective Rhomboid Inhibitors Block Invasion and Clear Blood-Stage Malaria

Shiv Gandhi, Rosanna P. Baker, Sangwoo Cho, Stancho Stanchev, Kvido Strisovsky, Siniša Urban

Research output: Contribution to journalArticlepeer-review

Abstract

Gandhi et al. combined substrate mapping, structural biology, and manually directed evolution to design potent peptidic inhibitors of the malaria rhomboid PfROM4 that do not target other rhomboid proteases. Treating malaria cultures revealed an essential role for PfROM4 only in invasion, and led to “tethered” parasites that die out.

Original languageEnglish (US)
Pages (from-to)1410-1424.e6
JournalCell Chemical Biology
Volume27
Issue number11
DOIs
StatePublished - Nov 19 2020

Keywords

  • Plasmodium
  • Ras-converting enzyme
  • Toxoplasma
  • apicomplexan parasites
  • malaria
  • presenilin
  • regulated intramembrane proteolysis
  • rhomboid protease
  • serine protease
  • site-2 protease

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry

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