Recent results in protein kinase inhibition for tropical diseases

• Published in: Bioorganic & medicinal chemistry letters Vol. 22; no. 22; pp. 6788 - 6793
• Main Author: Rotella, David P.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 15.11.2012; Elsevier
• Subjects: Biological and medical sciences; chemistry; drugs; genomics; human diseases; Humans; leishmaniasis; Leishmaniasis - drug therapy; malaria; Malaria - drug therapy; Medical sciences; Parasitic diseases; Parasitic Diseases - drug therapy; Pharmacology. Drug treatments; Plasmodium falciparum - enzymology; Protein kinase inhibitors; Protein Kinase Inhibitors - chemistry; Protein Kinase Inhibitors - therapeutic use; protein kinases; Protein Kinases - chemistry; Protein Kinases - metabolism; Protozoan Proteins - antagonists & inhibitors; Protozoan Proteins - metabolism; Protein kinase inhibitors; Parasitic diseases; Infection; Signal transduction; Enzyme; Tropical disease; Transferases; Non-specific serine/threonine protein kinase; Enzyme inhibitor; Parasitosis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2012.09.044

An image of the malarial kinase PfCDPK1 in cells infected by Plasmodium falciparum. Protein kinases are becoming widely investigated targets for treatment of protozoal parasitic tropical diseases such as malaria and leishmaniasis. The search for potent, selective inhibitors of these parasitic enzymes has been aided by the extensive variety of structures prepared for human diseases. Genomic approaches to target identification and validation have aided the search. Substantial progress has been made and research is continuing to expand in an effort to find safe, effective drug candidates for these difficult to treat and widespread diseases.