Latest findings on the role played by human isoform 5 of lactate dehydrogenase (hLDH5) in the promotion of glycolysis in invasive tumour cells are indicating this enzyme subtype as a promising therapeutic target for invasive cancer. Compounds able to selectively inhibit hLDH5 hold promise for the cure of neoplastic diseases. hLDH5 has so far been a rather unexplored target, since its importance in the promotion of cancer progression has been neglected for decades. This enzyme should also be considered as a challenging target due the high polar character (mostly cationic) of its ligand cavity. Recently, significant progresses have been reached with small-molecule inhibitors of hLDH5displaying remarkable potencies and selectivities. This review provides an overview of the newly developed hLDH5-inhibitors. The roles of hLDH isoforms will be briefly discussed, then the inhibitors will be grouped into chemical classes. Furthermore, general pharmacophore features will be emphasized throughout the structural subgroups analyzed.
|Autori:||Carlotta Granchi; Ilaria Paterni; Reshma Rani; Filippo Minutolo|
|Titolo:||Small-molecule inhibitors of human LDH5|
|Anno del prodotto:||2013|
|Digital Object Identifier (DOI):||10.4155/fmc.13.151|
|Appare nelle tipologie:||1.1 Articolo in rivista|