Replenishing the malaria drug discovery pipeline; introduction of a new drug discovery workflow using a nanoluciferase malaria parasite

Malaria is a deadly disease, that affected over 240 million people in 2020, an increase over progress in previous years. Despite advances in malariology, the challenge of finding the right drugs to treat the illness is complex.
During this hourlong webinar, drug discovery experts Dr James Duffy (Medicines for Malaria Ventures (MMV)), Dr Koen Dechering (TropIQ) and Martijn Timmerman (Pivot Park Screening Center (PPSC)) will share:

• perspectives and strategies in antimalaria drug discovery
• the biology of the malaria models
• small molecule tactics and technical assay development
• a novel transgenic malaria reporter strain with excellent performance in high-throughput screening
• screening and hit generation of active compounds against the blood stage of the Plasmodium falciparum parasite
• triage of large compound libraries screening
  
  

Watch this webinar on 22 June 16.00 hrs. (CET)

 Register here.

Part 1: perspective on antimalarials and overall strategy
James Duffy will open the webinar by explaining that, despite advances in our understanding of the underlying molecular basis of malaria and there being several new combination therapies in clinical development, new, affordable and safe malaria medicines are urgently required to:

• overcome increasing resistance against artemisinin-based combination treatments to treat vulnerable populations
• interrupt the parasite life cycle by blocking transmission to the vectors
• prevent infection and target parasite species that remain dormant in the liver
  
  

part 2: Introduction to biology of malaria models
Koen Dechering will introduce a novel reporter parasite that was generated by integration of a nanoluciferase expression cassette into the parasite’s genome and demonstrate the reporter’s sensitivity and reproducibility in high throughput screening formats.
Furthermore, he will:

• discuss pros and cons of phenotypic versus target-based screening
• the life cycle of the malaria parasite and discuss the challenges in malaria drug discovery
  
  

Part 3: Small molecule tactics and technical assay development on malaria models
Martijn Timmerman will discuss:

• miniaturization and optimization of a 1536-well screening assay to screen the blood-stage of P. falciparum
• the importance of triaging after the screening of a 140,000-compound library
  
  

Part 4: Hit prioritization discussion
Lastly, James Duffy will present a new screening and selection cascade for hit generation of compounds active against the blood-stage of P. falciparum.