Delving into the Latest Updates on Compound 49c(University of Geneva) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

PfPMX

Action

inhibitors

Mechanism

PfPMX inhibitors(Plasmodium falciparum plasmepsin X inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication

Malaria

Inactive Indication-

Originator Organization

University of Geneva

Active Organization

University of Geneva

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Regulated exocytosis by secretory organelles is important for malaria parasite invasion and egress. Many parasite effector proteins, including perforins, adhesins, and proteases, are extensively proteolytically processed both pre- and postexocytosis. Here we report the multistage antiplasmodial activity of the aspartic protease inhibitor hydroxyl-ethyl-amine-based scaffold compound 49c. This scaffold inhibits the preexocytosis processing of several secreted rhoptry and microneme proteins by targeting the corresponding maturases plasmepsins IX (PMIX) and X (PMX), respectively. Conditional excision of PMIX revealed its crucial role in invasion, and recombinantly active PMIX and PMX cleave egress and invasion factors in a 49c-sensitive manner.

100 Deals associated with Compound 49c(University of Geneva)

Login to view more data