RT Journal Article
T1 Choline Kinase: An Unexpected Journey for a Precision Medicine Strategy in Human Diseases
A1 Lacal, Juan Carlos
A1 Zimmerman, Tahl
A1 Campos, Joaquín M.
K1 Phospholipids metabolism
K1 Choline kinase
K1 Bispyridinium compounds
K1 Bisquinolinium compounds
K1 QSAR
K1 Anticancer drugs
K1 Rheumatoid arthritis
K1 Parasites
K1 Pathogenic bacteria
K1 Inflammatory disease
K1 Phosphorylation
K1 Colina quinasa
K1 Relación estructura-actividad cuantitativa
K1 Antineoplásicos
K1 Artritis reumatoide
K1 Parásitos
K1 Fosforilcolina
K1 Fosforilación
AB Choline kinase (ChoK) is a cytosolic enzyme that catalyzes the phosphorylation of choline to form phosphorylcholine (PCho) in the presence of ATP and magnesium. ChoK is required for the synthesis of key membrane phospholipids and is involved in malignant transformation in a large variety of human tumours. Active compounds against ChoK have been identified and proposed as antitumor agents. The ChoK inhibitory and antiproliferative activities of symmetrical bispyridinium and bisquinolinium compounds have been defined using quantitative structure-activity relationships (QSARs) and structural parameters. The design strategy followed in the development of the most active molecules is presented. The selective anticancer activity of these structures is also described. One promising anticancer compound has even entered clinical trials. Recently, ChoKα inhibitors have also been proposed as a novel therapeutic approach against parasites, rheumatoid arthritis, inflammatory processes, and pathogenic bacteria. The evidence for ChoKα as a novel drug target for approaches in precision medicine is discussed.
PB MDPI
YR 2021
FD 2021-05-25
LK http://hdl.handle.net/10668/4203
UL http://hdl.handle.net/10668/4203
LA en
NO Lacal JC, Zimmerman T, Campos JM. Choline Kinase: An Unexpected Journey for a Precision Medicine Strategy in Human Diseases. Pharmaceutics. 2021 May 25;13(6):788
DS RISalud
RD Apr 5, 2025