Inhibitors of Civ1 kinase belonging to 6-aminoaromatic-2-cyclohexyldiamino purine series as potent anti-fungal compounds.
There is today a blatant need for new antifungal agents, because of the recent increase in life-threatening infections involving an ever-greater number of fungal strains. Fungi make extensive use of kinases in the regulation of essential processes, in particular the cell cycle. Most fungal kinases, however, are shared with higher eukaryotes. Only the kinases which have no human homologs, such as the histidine kinases, can be used as targets for antifungal drugs design. This review describes efforts directed towards the discovery of drugs active against a novel target, the atypical cell cycle kinase, Civ1.
Bordon-Pallier
Florence
F
Infectious Diseases Group, Aventis Pharma, 102, route de Noisy, 93235 Romainville, France.
Jullian
Nathalie
N
Ferrari
Paul
P
Girard
Anne-Marie
AM
Bocquel
Marie-Thérèse
MT
Biton
Jacques
J
Bouquin
Nicolas
N
Haesslein
Jean-Luc
JL
D000595:Amino Acid Sequence; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology*; D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors; D018844:Cyclin-Dependent Kinases; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D005656:Fungal Proteins / Q000037:antagonists & inhibitors; D005658:Fungi / Q000187:drug effects / Q000201:enzymology / Q000502:physiology; D008958:Models, Molecular; D008969:Molecular Sequence Data; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011687:Purines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D000095043:Cyclin-Dependent Kinase-Activating Kinase
D000935:Antifungal Agents; D018797:Cell Cycle Proteins; D004791:Enzyme Inhibitors; D005656:Fungal Proteins; D011687:Purines; D017346:Protein Serine-Threonine Kinases; D018844:Cyclin-Dependent Kinases; C030985:purine; D000095043:Cyclin-Dependent Kinase-Activating Kinase