Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present)

2020 ◽  
Vol 63 (9) ◽  
pp. 4445-4467 ◽  
Author(s):  
Peter Mubanga Cheuka ◽  
Godwin Dziwornu ◽  
John Okombo ◽  
Kelly Chibale
2020 ◽  
Author(s):  
Sanaa Bardaweel

Recently, an outbreak of fatal coronavirus, SARS-CoV-2, has emerged from China and is rapidly spreading worldwide. As the coronavirus pandemic rages, drug discovery and development become even more challenging. Drug repurposing of the antimalarial drug chloroquine and its hydroxylated form had demonstrated apparent effectiveness in the treatment of COVID-19 associated pneumonia in clinical trials. SARS-CoV-2 spike protein shares 31.9% sequence identity with the spike protein presents in the Middle East Respiratory Syndrome Corona Virus (MERS-CoV), which infects cells through the interaction of its spike protein with the DPP4 receptor found on macrophages. Sitagliptin, a DPP4 inhibitor, that is known for its antidiabetic, immunoregulatory, anti-inflammatory, and beneficial cardiometabolic effects has been shown to reverse macrophage responses in MERS-CoV infection and reduce CXCL10 chemokine production in AIDS patients. We suggest that Sitagliptin may be beneficial alternative for the treatment of COVID-19 disease especially in diabetic patients and patients with preexisting cardiovascular conditions who are already at higher risk of COVID-19 infection.


2014 ◽  
Vol 14 (7) ◽  
pp. 941-951 ◽  
Author(s):  
Gregory Landelle ◽  
Armen Panossian ◽  
Frederic Leroux

2020 ◽  
Vol 42 (2) ◽  
pp. 25-25

Abstract The 2020 IUPAC-Richter Prize in Medicinal Chemistry has been awarded to John Macor, PhD, Global Head Integrated Drug Discovery, Sanofi.


2006 ◽  
Vol 11 (15-16) ◽  
pp. 708-716 ◽  
Author(s):  
Ryan T. Strachan ◽  
Gina Ferrara ◽  
Bryan L. Roth

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